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Angiogenesis Src

Src

Src kinase family is a family of non-receptor tyrosine kinases that includes nine members: Src, Yes, Fyn, and Fgr, forming the SrcA subfamily, Lck, Hck, Blk, and Lyn in the SrcB subfamily, and Frk in its own subfamily. Frk has homologs in invertebrates such as flies and worms, and Src homologs exist in organisms as diverse as unicellular choanoflagellates, but the SrcA and SrcB subfamilies are specific to vertebrates. Src family kinases contain six conserved domains: a N-terminal myristoylated segment, a SH2 domain, a SH3 domain, a linker region, a tyrosine kinase domain, and C-terminal tail.
Cat No. product name
T0152 BosutinibHOT Bosutinib is a synthetic quinolone derivative and dual kinase inhibitor that targets both Abl (IC50: 1 nM) and Src (IC50: 1.2 nM) kinases.
T10206 A 419259 A 419259 is a pyrrolo-pyrimidine inhibitor, designed to enhance selectivity towards the Src family (IC50s: 9 nM, <3 nM and <3 nM for Src, Lck and Lyn).
T10583 Bosutinib D8 Bosutinib D8 is a deuterium-labeled Bosutinib. Bosutinib (SKI-606) is a dual Src/Abl inhibitor (IC50s: 1.2 nM/1 nM).
T10784 CH6953755 CH6953755 is a potent, orally active and selective inhibitor of YES1 kinase (IC50: 1.8 nM). It inhibits YES1 kinase, leading to antitumor activity against YES1 ...
T11752 Keap1–Nrf2-IN-1 Keap1–Nrf2 IN-1 activates Nrf2-regulated cytoprotective response and antagonizes acetaminophen-induced liver injury both in cellular and in vivo models. Keap1...
T11916 Lyn-IN-1 Lyn-IN-1 is a selective and potent dual inhibitor of Bcr-Abl and Lyn
T13186 TL02-59 TL02-59 is an orally active inhibitor of Src-family kinase Fgr (IC50: 0.03 nM), and potently suppresses acute myelogenous leukemia (AML) cell growth.
T13186L TL02-59 dihydrochloride TL02-59 dihydrochloride is an orally active inhibitor of Src-family kinase Fgr (IC50: 0.03 nM).
T1448 DasatinibHOT Dasatinib is a potent inhibitor of the Bcr-Abl and Src family (IC50s: 0.6, 0.8, 79 and 37 nM for Abl, Src, c-Kit, and c-KitD816V, respectively).
T1448L Dasatinib monohydrate Dasatinib is an orally bioavailable synthetic small molecule-inhibitor of SRC-family protein-tyrosine kinases. Dasatinib binds to and inhibits the growth-promot...
T15674 Tirbanibulin dihydrochloride Tirbanibulin is an inhibitor of Src that targets the peptide substrate site of Src (GI50: 9-60 nM in cancer cell lines).
T15675 Tirbanibulin Mesylate Tirbanibulin Mesylate is an inhibitor of Src that targets the peptide substrate site of Src (GI50: 9-60 nM in cancer cell lines).
T1667 Tandutinib Tandutinib (MLN518, CT53518), an effective FLT3 antagonist (IC50: 0.22 μM), can also inhibit c-Kit and PDGFR, 15-20 fold higher potency for FLT3 versus CSF-1R ...
T16750 Rigosertib Rigosertib is a selective and non-ATP-competitive inhibitor of PLK1 (IC50: 9 nM). Rigosertib is a multi-kinase inhibitor and a selective anti-cancer agent, whic...
T16760 RK-24466 RK-24466 is a selective and potent inhibitor of Lck, inhibits Lck (64-509) and LckCD isoforms with IC50s of less than 1 and 2 nM, respectively.
T1754 ZM 306416 ZM 306416, a VEGFR1 inhibitor (IC50: 0.33 μM), can also inhibit EGFR (IC50<10 nM).
T1777 NintedanibHOT Nintedanib is an inhibitor of the receptor tyrosine kinases VEGFR/FGFR/PDGFR (IC50s: 13-34/37-610/59/65 nM for VEGFR1-3, FGFR1-4, and PDGFRα/β, respectively).
T1811 WH-4-023 WH-4-023 is a potent and orally active Lck/Src inhibitor. It also potently inhibits SIK.
T1812 KX1004 KX1-004, a potential protective drug for NIHL, is an effective small molecule inhibitor of Src-PTK.
T1835 IbrutinibHOT Ibrutinib is an irreversible inhibitor of BTK (IC50: 0.5 nM) that selectively blocks B cell activation.
T1985 WHI-P154 WHI-P154 is a potent JAK3 inhibitor.
T2070 CEP32496 CEP-32496 is a highly potent inhibitor of BRAF.
T22303 Dasatinib hydrochloride Dasatinib hydrochloride is a highly ATP competitive, potent, orally active inhibitor of dual Src/Bcr-Abl(with Ki values of 16 pM and 30 pM for Src and Bcr-Abl, ...
T22306 DGY-06-116 DGY-06-116 is an selective and irreversible covalent inhibitor of Src and FGFR1 with IC50 value of 3nM and 8340 nM, respectively.
T22306 DGY-06-116 DGY-06-116 is an selective and irreversible covalent inhibitor of Src and FGFR1 with IC50 value of 3nM and 8340 nM, respectively.
T23176 PP 3 PP 3 is a Negative control for the Src kinase inhibitor PP 2
T2327 Pelitinib Pelitinib (EKB-569) is an effective irreversible EGFR inhibitor (IC50: 38.5 nM).
T2341 KW2449 KW-2449 is a multiple-targeted inhibitor, mostly for Flt3 (IC50: 6.6 nM), modestly effective to Bcr-Abl, FGFR1, and Aurora A; little inhibitory on PDGFRβ, IGF-...
T2358 ENMD2076 ENMD-2076, a multi-targeted kinase inhibitor, has specific activity against Aurora A, Flt3, KDR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα.
T2372 PonatinibHOT Ponatinib is an orally available, multitargeted kinase inhibitor (IC50s: 0.37/1.1/1.5/2.2/5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively).
T2415 PP121 PP-121 is a multi-targeted inhibitor of PDGFR (IC50: 2 nM), Hck (IC50: 8 nM), mTOR (IC50: 10 nM), VEGFR2(IC50: 12 nM), Src (IC50: 14 nM) and Abl (IC50: 18 nM) ,...
T2603 Spebrutinib Spebrutinib is an orally bioavailable, selective inhibitor of Bruton's agammaglobulinemia tyrosine kinase (BTK), with potential antineoplastic activity.
T2608 CHIR98014 CHIR-98014 is a selective GSK3 inhibitor; potentiate insulin activation of glucose transport and utilization in vitro and in vivo.
T2609 Masitinib Masitinib is a tyrosine-kinase inhibitor used in the treatment of mast cell tumors in animals, specifically dogs. Since its introduction in November 2008 it has...
T2610 BMS 599626 BMS-599626 has been used in trials studying the treatment of Cancer, Metastases, and HER2 or EGFR Expressing Advanced Solid Malignancies.
T2624 OSI 930 OSI-930, an orally active inhibitor of c-Kit and the vascular endothelial growth factor receptor-2 (VEGFR-2), targets cancer cell proliferation and blood vessel...
T2642 PD173074 PD173074 is an effective FGFR1 inhibitor (IC50: 25 nM) and also inhibits VEGFR2 (IC50: 100-200 nM) in cell-free assays. The selectivity is higher ~1000-fold for...
T2696 PRT062607 hydrochlorideHOT PRT062607 (BIIB-057) is a selective inhibitor of Syk (IC50: 1 nM). It displays at least 80-fold selectivity for Syk over other kinases.
T2709 TAK901 TAK-901 has been used in trials studying the treatment of Lymphoma, Myelofibrosis, Multiple Myeloma, Myeloid Metaplasia, and Advanced Solid Tumors, among others...
T3063 PD173955 PD173955 is src family-selective tyrosine kinase inhibitor with IC50 of ~22 nM for Src, Yes and Abl kinase; less potent for FGFRα and no activity on InsR and P...
T3319 Scutellarein Scutellarein reduces inflammatory responses by inhibiting Src kinase activity.
T3593 Src Inhibitor 1 Src Inhibitor 1 is a potent and selective dual site Src tyrosine kinase inhibitor.
T3935 1-Naphthyl PP1 1-Naphthyl PP1 is a selective src inhibitor(v-Src and c-Fyn, c-Abl, CDK2 and CAMK II with IC50s of 1.0, 0.6, 0.6, 18 and 22 μM, respectively)
T4071 TPX0005 TPX-0005 is a potent ALK/ROS1/TRK inhibitor, with IC50 of 1.01 nM, 5.3 nM, 1.08 nM and 1.26 nM for WT ALK, SRC, ALK L1196M and ALK G1202R, respectively.
T4133 CCT196969 CCT196969 is a novel orally available, pan-RAF inhibitor with anti-SRC activity. It also inhibits SRC, LCK, and the p38 MAPKs.
T4301 AD80 AD80, a multikinase inhibitor, inhibits RET, RAF, SRCand S6K, with greatly reduced mTOR activity.
T4597 UM164 UM-164 is a highly potent inhibitor of c-Src with a Kd of 2.7 nM. UM-164 also potently inhibits p38α and p38β.
T4618 K 0859 BGG463 can inhibit c-ABL-T334I, BCR-ABL and BCR-ABL-T315I variants with a 50% inhibitory concentration (IC50) of 0.25 μM, 0.09 μM and 0.590 μM, respectively.
T6028 PF477736 PF-477736 is a specifc, effective and ATP-competitive Chk1 inhibitor (Ki: 0.49 nM ) and also inhibits FGFR3, Aurora-A, VEGFR2, Flt3, Fms (CSF1R), Ret and Yes.
T6077 ZM 447439 ZM 447439 is a selective and ATP-competitive inhibitor for Aurora A and Aurora B with IC50 of 110 nM and 130 nM, respectively. It is more than 8-fold selective ...
T6078 SaracatinibHOT Saracatinib (AZD0530) is an effective Src inhibitor (IC50: 2.7 nM), and effective to Lck, Fyn, Lyn, Blk, Fgr and c-Yes.
T6196 PP1 PP1, a specific and effective Src inhibitor, is with IC50 for Lck/Fyn is 5 nM/ 6 nM, respectively.
T6227 Benidipine hydrochloride Benidipine HCl, a hydrochloride salt form of benidipine, is used as a blocker of dihydropyridine calcium channel.
T6266 PP2 PP2 is a effective inhibitor of Lck/Fyn (IC50:4/5 nM) , ~100-fold less potent to EGFR, inactive for ZAP-70, PKA and JAK2.
T6311 Bafetinib Bafetinib (INNO-406) is an effective and specific dual Bcr-Abl/Lyn inhibitor (IC50: 5.8/19 nM), and no inhibition of the phosphorylation of the T315I mutant and...
T6315 MLN8054 MLN8054 is a potent and selective Aurora A kinase inhibitor with an IC50 of 4 nM.
T6321 Tofacitinib Tofacitinib is an oral, small molecule inhibitor of Janus kinases that is used to treat moderate-to-severe rheumatoid arthritis.
T6345 KX2-391 KX2-391 is a highly selective Src kinase inhibitor that has demonstrated efficacy in pre-Clinicalal animal models of colon, pancreatic, prostate and breast canc...
T6348 NVP-BHG712 NVP-BHG712 is a specific EphB4 inhibitor with ED50 of 25 nM that discriminates between VEGFR and EphB4 inhibition; also shows activity against c-Raf, c-Src and ...
T6350 CHIR124 CHIR-124 is an effective Chk1 inhibitor (IC50: 0.3 nM). It has 2, 000-fold selectivity against Chk2, 500- to 5, 000-fold less activity against Cdc2 and CDK2/4.
T6419 BMS536924 BMS-536924 is an ATP-competitive IGF-1R/IR inhibitor with IC50 of 100 nM/73 nM, modest activity for Mek, Fak, and Lck with very little activity for Akt1, MAPK1/...
T6427 Butein Butein, a plant polyphenol, is isolated from Rhus verniciflua. It can inhibit the activation of protein tyrosine kinase, NF-κB and STAT3, and also can inhibit ...
T6680 Staurosporine Staurosporine is a potent PKC inhibitor for PKCα/γ/η (IC50: 2/5/4 nM), less potent to PKCε (73 nM), PKCδ (20 nM) and little action to PKCζ (1086 nM).
T6730 WAY600 WAY-600 is a potent, ATP-competitive and selective inhibitor of mTOR with IC50 of 9 nM; blocks mTORC1/P-S6K(T389) and mTORC2/P-AKT(S473) but not P-AKT(T308); se...
T6732 WYE687 WYE-687 is an ATP-competitive and selective inhibitor of mTOR with IC50 of 7 nM; blocks mTORC1/pS6K(T389) and mTORC2/P-AKT(S473) but no effect observed on P-AKT...
T6886 MCB613 MCB-613 is an effective steroid receptor coactivator (SRC) stimulator.
T6896 Tolimidone MLR-1023 is a chemical compound which inhibits acid secretion in animal models and also acts as a bronchodilator in histamine-challenged animals.
T6920 ON123300 ON123300 is a potent and multi-targeted kinase inhibitor for CDK4/Ark5/PDGFRβ/FGFR1/RET/Fyn (IC50: 3.9/5/26/26/9.2/11 nM).
T6982 SGI7079 SGI-7079 is a new selective Axl inhibitor. SGI-7079 can be a dose-dependent manner inhibited growth of tumors. It is also a potential therapeutic target for EGF...
T6997 SU6656 SU 6656 is a selective inhibitor of Src family kinases, with IC50 of 280 nM, 20 nM, 130 nM, and 170 nM for Src, Yes, Lyn, and Fyn, respectively.
T7123 AMG-47a AMG-47a is a potent inhibitor of Lck and T cell proliferation. AMG-47a could promote the degradation of the KRAS oncoprotein. AMG-47a selectively reduced the ...
T7345 7-Hydroxy-4-chromone 7-Hydroxychromone is a Src kinase inhibitor (IC50 of <300 μM).
T7371 1-Naphthyl PP1 hydrochloride 1-Naphthyl PP1 hydrochloride is a selective inhibitor of src family kinases v-Src
T8499 eCF506 eCF506 is a potent and selective inhibitor of SRC (IC50 < 0.5 nM)
T8544 Masitinib mesylate Masitinib mesylate is a selective and orally bioavailable c-Kit inhibitor (IC50 of 200 nM,540/800 nM,510 nM for human recombinant c-Kit;PDGFRα/β;LynB,respecti...
T8995 NCGC00262650 NCGC00262650 is an inhibitor of AMA1-RON2 interaction and c-Src tyrosine kinase activity.
T9002 squarunkinA squarunkinA is a novel modulator of the UNC119-Cargo Interaction, potently and selectively inhibiting the binding of a myristoylated peptide representing the N-...
T9017 HPK1-IN-2 dihydrochloride HPK1-IN-2 dihydrochloride is a potent and orally active inhibitor of hematopoietic progenitor kinase-1 (HPK1;IC50<0.05 µΜ). It also inhibits Lck (0.05 µΜ<I...
TN3139 5alpha-Hydroxycostic acid 5alpha-Hydroxycostic acid possesses anti-angiogenic ability by interfering the VEGF- and Ang2-related pathways, and it may be a good drug candidate.
TQ0132 A 419259 trihydrochloride A 419259 trihydrochloride is an Src family kinases inhibitor (IC50s: 9 nM, 3 nM and 3 nM for Src, Lck and Lyn).
TQ0169 Inulicin Inulicin, an active compound isolated from Inula Britannica L., inhibits VEGF-mediated activation of Src and FAK.
Bosutinib HOT
T0152CAS 380843-75-4
Bosutinib is a synthetic quinolone derivative and dual kinase inhibitor that targets both Abl (IC50: 1 nM) and Src (IC50: 1.2 nM) kinases.
A 419259
T10206CAS 364042-47-7
A 419259 is a pyrrolo-pyrimidine inhibitor, designed to enhance selectivity towards the Src family (IC50s: 9 nM, <3 nM and <3 nM for Src, Lck and Lyn).
Bosutinib D8
T10583CAS T10583
Bosutinib D8 is a deuterium-labeled Bosutinib. Bosutinib (SKI-606) is a dual Src/Abl inhibitor (IC50s: 1.2 nM/1 nM).
CH6953755
T10784CAS 2055918-71-1
CH6953755 is a potent, orally active and selective inhibitor of YES1 kinase (IC50: 1.8 nM). It inhibits YES1 kinase, leading to antitumor activity against YES1 ...
Keap1–Nrf2-IN-1
T11752CAS 2232112-72-8
Keap1–Nrf2 IN-1 activates Nrf2-regulated cytoprotective response and antagonizes acetaminophen-induced liver injury both in cellular and in vivo models. Keap1...
Lyn-IN-1
T11916CAS 887650-05-7
Lyn-IN-1 is a selective and potent dual inhibitor of Bcr-Abl and Lyn
TL02-59
T13186CAS 1315330-17-6
TL02-59 is an orally active inhibitor of Src-family kinase Fgr (IC50: 0.03 nM), and potently suppresses acute myelogenous leukemia (AML) cell growth.
TL02-59 dihydrochloride
T13186LCAS 2415263-06-6
TL02-59 dihydrochloride is an orally active inhibitor of Src-family kinase Fgr (IC50: 0.03 nM).
Dasatinib HOT
T1448CAS 302962-49-8
Dasatinib is a potent inhibitor of the Bcr-Abl and Src family (IC50s: 0.6, 0.8, 79 and 37 nM for Abl, Src, c-Kit, and c-KitD816V, respectively).
Dasatinib monohydrate
T1448LCAS 863127-77-9
Dasatinib is an orally bioavailable synthetic small molecule-inhibitor of SRC-family protein-tyrosine kinases. Dasatinib binds to and inhibits the growth-promot...
Tirbanibulin dihydrochloride
T15674CAS 1038395-65-1
Tirbanibulin is an inhibitor of Src that targets the peptide substrate site of Src (GI50: 9-60 nM in cancer cell lines).
Tirbanibulin Mesylate
T15675CAS 1080645-95-9
Tirbanibulin Mesylate is an inhibitor of Src that targets the peptide substrate site of Src (GI50: 9-60 nM in cancer cell lines).
Tandutinib
T1667CAS 387867-13-2
Tandutinib (MLN518, CT53518), an effective FLT3 antagonist (IC50: 0.22 μM), can also inhibit c-Kit and PDGFR, 15-20 fold higher potency for FLT3 versus CSF-1R ...
Rigosertib
T16750CAS 592542-59-1
Rigosertib is a selective and non-ATP-competitive inhibitor of PLK1 (IC50: 9 nM). Rigosertib is a multi-kinase inhibitor and a selective anti-cancer agent, whic...
RK-24466
T16760CAS 213743-31-8
RK-24466 is a selective and potent inhibitor of Lck, inhibits Lck (64-509) and LckCD isoforms with IC50s of less than 1 and 2 nM, respectively.
ZM 306416
T1754CAS 690206-97-4
ZM 306416, a VEGFR1 inhibitor (IC50: 0.33 μM), can also inhibit EGFR (IC50<10 nM).
Nintedanib HOT
T1777CAS 656247-17-5
Nintedanib is an inhibitor of the receptor tyrosine kinases VEGFR/FGFR/PDGFR (IC50s: 13-34/37-610/59/65 nM for VEGFR1-3, FGFR1-4, and PDGFRα/β, respectively).
WH-4-023
T1811CAS 837422-57-8
WH-4-023 is a potent and orally active Lck/Src inhibitor. It also potently inhibits SIK.
KX1004
T1812CAS 518058-84-9
KX1-004, a potential protective drug for NIHL, is an effective small molecule inhibitor of Src-PTK.
Ibrutinib HOT
T1835CAS 936563-96-1
Ibrutinib is an irreversible inhibitor of BTK (IC50: 0.5 nM) that selectively blocks B cell activation.
WHI-P154
T1985CAS 211555-04-3
WHI-P154 is a potent JAK3 inhibitor.
CEP32496
T2070CAS 1188910-76-0
CEP-32496 is a highly potent inhibitor of BRAF.
Dasatinib hydrochloride
T22303CAS 854001-07-3
Dasatinib hydrochloride is a highly ATP competitive, potent, orally active inhibitor of dual Src/Bcr-Abl(with Ki values of 16 pM and 30 pM for Src and Bcr-Abl, ...
DGY-06-116
T22306CAS T22306
DGY-06-116 is an selective and irreversible covalent inhibitor of Src and FGFR1 with IC50 value of 3nM and 8340 nM, respectively.
DGY-06-116
T22306CAS T22306
DGY-06-116 is an selective and irreversible covalent inhibitor of Src and FGFR1 with IC50 value of 3nM and 8340 nM, respectively.
PP 3
T23176CAS 5334-30-5
PP 3 is a Negative control for the Src kinase inhibitor PP 2
Pelitinib
T2327CAS 257933-82-7
Pelitinib (EKB-569) is an effective irreversible EGFR inhibitor (IC50: 38.5 nM).
KW2449
T2341CAS 1000669-72-6
KW-2449 is a multiple-targeted inhibitor, mostly for Flt3 (IC50: 6.6 nM), modestly effective to Bcr-Abl, FGFR1, and Aurora A; little inhibitory on PDGFRβ, IGF-...
ENMD2076
T2358CAS 934353-76-1
ENMD-2076, a multi-targeted kinase inhibitor, has specific activity against Aurora A, Flt3, KDR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα.
Ponatinib HOT
T2372CAS 943319-70-8
Ponatinib is an orally available, multitargeted kinase inhibitor (IC50s: 0.37/1.1/1.5/2.2/5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively).
PP121
T2415CAS 1092788-83-4
PP-121 is a multi-targeted inhibitor of PDGFR (IC50: 2 nM), Hck (IC50: 8 nM), mTOR (IC50: 10 nM), VEGFR2(IC50: 12 nM), Src (IC50: 14 nM) and Abl (IC50: 18 nM) ,...
Spebrutinib
T2603CAS 1202757-89-8
Spebrutinib is an orally bioavailable, selective inhibitor of Bruton's agammaglobulinemia tyrosine kinase (BTK), with potential antineoplastic activity.
CHIR98014
T2608CAS 252935-94-7
CHIR-98014 is a selective GSK3 inhibitor; potentiate insulin activation of glucose transport and utilization in vitro and in vivo.
Masitinib
T2609CAS 790299-79-5
Masitinib is a tyrosine-kinase inhibitor used in the treatment of mast cell tumors in animals, specifically dogs. Since its introduction in November 2008 it has...
BMS 599626
T2610CAS 714971-09-2
BMS-599626 has been used in trials studying the treatment of Cancer, Metastases, and HER2 or EGFR Expressing Advanced Solid Malignancies.
OSI 930
T2624CAS 728033-96-3
OSI-930, an orally active inhibitor of c-Kit and the vascular endothelial growth factor receptor-2 (VEGFR-2), targets cancer cell proliferation and blood vessel...
PD173074
T2642CAS 219580-11-7
PD173074 is an effective FGFR1 inhibitor (IC50: 25 nM) and also inhibits VEGFR2 (IC50: 100-200 nM) in cell-free assays. The selectivity is higher ~1000-fold for...
PRT062607 hydrochloride HOT
T2696CAS 1370261-97-4
PRT062607 (BIIB-057) is a selective inhibitor of Syk (IC50: 1 nM). It displays at least 80-fold selectivity for Syk over other kinases.
TAK901
T2709CAS 934541-31-8
TAK-901 has been used in trials studying the treatment of Lymphoma, Myelofibrosis, Multiple Myeloma, Myeloid Metaplasia, and Advanced Solid Tumors, among others...
PD173955
T3063CAS 260415-63-2
PD173955 is src family-selective tyrosine kinase inhibitor with IC50 of ~22 nM for Src, Yes and Abl kinase; less potent for FGFRα and no activity on InsR and P...
Scutellarein
T3319CAS 529-53-3
Scutellarein reduces inflammatory responses by inhibiting Src kinase activity.
Src Inhibitor 1
T3593CAS 179248-59-0
Src Inhibitor 1 is a potent and selective dual site Src tyrosine kinase inhibitor.
1-Naphthyl PP1
T3935CAS 221243-82-9
1-Naphthyl PP1 is a selective src inhibitor(v-Src and c-Fyn, c-Abl, CDK2 and CAMK II with IC50s of 1.0, 0.6, 0.6, 18 and 22 μM, respectively)
TPX0005
T4071CAS 1802220-02-5
TPX-0005 is a potent ALK/ROS1/TRK inhibitor, with IC50 of 1.01 nM, 5.3 nM, 1.08 nM and 1.26 nM for WT ALK, SRC, ALK L1196M and ALK G1202R, respectively.
CCT196969
T4133CAS 1163719-56-9
CCT196969 is a novel orally available, pan-RAF inhibitor with anti-SRC activity. It also inhibits SRC, LCK, and the p38 MAPKs.
AD80
T4301CAS 1384071-99-1
AD80, a multikinase inhibitor, inhibits RET, RAF, SRCand S6K, with greatly reduced mTOR activity.
UM164
T4597CAS 903564-48-7
UM-164 is a highly potent inhibitor of c-Src with a Kd of 2.7 nM. UM-164 also potently inhibits p38α and p38β.
K 0859
T4618CAS 890129-26-7
BGG463 can inhibit c-ABL-T334I, BCR-ABL and BCR-ABL-T315I variants with a 50% inhibitory concentration (IC50) of 0.25 μM, 0.09 μM and 0.590 μM, respectively.
PF477736
T6028CAS 952021-60-2
PF-477736 is a specifc, effective and ATP-competitive Chk1 inhibitor (Ki: 0.49 nM ) and also inhibits FGFR3, Aurora-A, VEGFR2, Flt3, Fms (CSF1R), Ret and Yes.
ZM 447439
T6077CAS 331771-20-1
ZM 447439 is a selective and ATP-competitive inhibitor for Aurora A and Aurora B with IC50 of 110 nM and 130 nM, respectively. It is more than 8-fold selective ...
Saracatinib HOT
T6078CAS 379231-04-6
Saracatinib (AZD0530) is an effective Src inhibitor (IC50: 2.7 nM), and effective to Lck, Fyn, Lyn, Blk, Fgr and c-Yes.
PP1
T6196CAS 172889-26-8
PP1, a specific and effective Src inhibitor, is with IC50 for Lck/Fyn is 5 nM/ 6 nM, respectively.
Benidipine hydrochloride
T6227CAS 91599-74-5
Benidipine HCl, a hydrochloride salt form of benidipine, is used as a blocker of dihydropyridine calcium channel.
PP2
T6266CAS 172889-27-9
PP2 is a effective inhibitor of Lck/Fyn (IC50:4/5 nM) , ~100-fold less potent to EGFR, inactive for ZAP-70, PKA and JAK2.
Bafetinib
T6311CAS 859212-16-1
Bafetinib (INNO-406) is an effective and specific dual Bcr-Abl/Lyn inhibitor (IC50: 5.8/19 nM), and no inhibition of the phosphorylation of the T315I mutant and...
MLN8054
T6315CAS 869363-13-3
MLN8054 is a potent and selective Aurora A kinase inhibitor with an IC50 of 4 nM.
Tofacitinib
T6321CAS 477600-75-2
Tofacitinib is an oral, small molecule inhibitor of Janus kinases that is used to treat moderate-to-severe rheumatoid arthritis.
KX2-391
T6345CAS 897016-82-9
KX2-391 is a highly selective Src kinase inhibitor that has demonstrated efficacy in pre-Clinicalal animal models of colon, pancreatic, prostate and breast canc...
NVP-BHG712
T6348CAS 940310-85-0
NVP-BHG712 is a specific EphB4 inhibitor with ED50 of 25 nM that discriminates between VEGFR and EphB4 inhibition; also shows activity against c-Raf, c-Src and ...
CHIR124
T6350CAS 405168-58-3
CHIR-124 is an effective Chk1 inhibitor (IC50: 0.3 nM). It has 2, 000-fold selectivity against Chk2, 500- to 5, 000-fold less activity against Cdc2 and CDK2/4.
BMS536924
T6419CAS 468740-43-4
BMS-536924 is an ATP-competitive IGF-1R/IR inhibitor with IC50 of 100 nM/73 nM, modest activity for Mek, Fak, and Lck with very little activity for Akt1, MAPK1/...
Butein
T6427CAS 487-52-5
Butein, a plant polyphenol, is isolated from Rhus verniciflua. It can inhibit the activation of protein tyrosine kinase, NF-κB and STAT3, and also can inhibit ...
Staurosporine
T6680CAS 62996-74-1
Staurosporine is a potent PKC inhibitor for PKCα/γ/η (IC50: 2/5/4 nM), less potent to PKCε (73 nM), PKCδ (20 nM) and little action to PKCζ (1086 nM).
WAY600
T6730CAS 1062159-35-6
WAY-600 is a potent, ATP-competitive and selective inhibitor of mTOR with IC50 of 9 nM; blocks mTORC1/P-S6K(T389) and mTORC2/P-AKT(S473) but not P-AKT(T308); se...
WYE687
T6732CAS 1062161-90-3
WYE-687 is an ATP-competitive and selective inhibitor of mTOR with IC50 of 7 nM; blocks mTORC1/pS6K(T389) and mTORC2/P-AKT(S473) but no effect observed on P-AKT...
MCB613
T6886CAS 1162656-22-5
MCB-613 is an effective steroid receptor coactivator (SRC) stimulator.
Tolimidone
T6896CAS 41964-07-2
MLR-1023 is a chemical compound which inhibits acid secretion in animal models and also acts as a bronchodilator in histamine-challenged animals.
ON123300
T6920CAS 1357470-29-1
ON123300 is a potent and multi-targeted kinase inhibitor for CDK4/Ark5/PDGFRβ/FGFR1/RET/Fyn (IC50: 3.9/5/26/26/9.2/11 nM).
SGI7079
T6982CAS 1239875-86-5
SGI-7079 is a new selective Axl inhibitor. SGI-7079 can be a dose-dependent manner inhibited growth of tumors. It is also a potential therapeutic target for EGF...
SU6656
T6997CAS 330161-87-0
SU 6656 is a selective inhibitor of Src family kinases, with IC50 of 280 nM, 20 nM, 130 nM, and 170 nM for Src, Yes, Lyn, and Fyn, respectively.
AMG-47a
T7123CAS 882663-88-9
AMG-47a is a potent inhibitor of Lck and T cell proliferation. AMG-47a could promote the degradation of the KRAS oncoprotein. AMG-47a selectively reduced the ...
7-Hydroxy-4-chromone
T7345CAS 59887-89-7
7-Hydroxychromone is a Src kinase inhibitor (IC50 of <300 μM).
1-Naphthyl PP1 hydrochloride
T7371CAS 956025-47-1
1-Naphthyl PP1 hydrochloride is a selective inhibitor of src family kinases v-Src
eCF506
T8499CAS 1914078-41-3
eCF506 is a potent and selective inhibitor of SRC (IC50 < 0.5 nM)
Masitinib mesylate
T8544CAS 1048007-93-7
Masitinib mesylate is a selective and orally bioavailable c-Kit inhibitor (IC50 of 200 nM,540/800 nM,510 nM for human recombinant c-Kit;PDGFRα/β;LynB,respecti...
NCGC00262650
T8995CAS 344359-25-7
NCGC00262650 is an inhibitor of AMA1-RON2 interaction and c-Src tyrosine kinase activity.
squarunkinA
T9002CAS 2101958-02-3
squarunkinA is a novel modulator of the UNC119-Cargo Interaction, potently and selectively inhibiting the binding of a myristoylated peptide representing the N-...
HPK1-IN-2 dihydrochloride
T9017CAS 2056122-11-1
HPK1-IN-2 dihydrochloride is a potent and orally active inhibitor of hematopoietic progenitor kinase-1 (HPK1;IC50<0.05 µΜ). It also inhibits Lck (0.05 µΜ<I...
5alpha-Hydroxycostic acid
TN3139CAS 132185-83-2
5alpha-Hydroxycostic acid possesses anti-angiogenic ability by interfering the VEGF- and Ang2-related pathways, and it may be a good drug candidate.
A 419259 trihydrochloride
TQ0132CAS 1435934-25-0
A 419259 trihydrochloride is an Src family kinases inhibitor (IC50s: 9 nM, 3 nM and 3 nM for Src, Lck and Lyn).
Inulicin
TQ0169CAS 33627-41-7
Inulicin, an active compound isolated from Inula Britannica L., inhibits VEGF-mediated activation of Src and FAK.