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Angiogenesis Filter
Angiogenesis Tyrosine Kinase/AdaptorsACK
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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.
- eCF506T84991914078-41-3eCF506 is a potent and selective inhibitor of SRC (IC50 < 0.5 nM)
- $40
SizeQTY
- StaurosporineT668062996-74-1Staurosporine (AM-2282) is a protein kinase inhibitor with ATP-competitive and non-selective inhibitory activity (IC50=6 15 2 3 3000 nM) against PKC, PKA, c-Fgr, phosphorylase kinase and TAOK2. Staurosporine also induces apoptosis.
- $44.8
- $56
SizeQTY
Cited - NintedanibT1777656247-17-5Nintedanib (Intedanib) is a triple vascular kinase inhibitor that inhibits VEGFR1, VEGFR2, and VEGFR3 (IC50=34 13 13 nM), FGFR1, FGFR2, and FGFR3 (IC50=69 37 108 nM), PDGFRα, and PDGFRβ (IC50=59 65 nM). Nintedanib has antitumor activity and inhibits tumor growth by inhibiting angiogenesis.
- $38
SizeQTY Cited - IbrutinibT1835936563-96-1Ibrutinib (PCI-32765) is an irreversible inhibitor of BTK (IC50: 0.5 nM) that selectively blocks B cell activation.
- $36
SizeQTY Cited - DasatinibT1448302962-49-8Dasatinib (BMS-354825) is an orally active, ATP-competitive tyrosine kinase inhibitor that targets Src and Bcr-Abl (Ki=16 30 pM), with antitumor activity, used in the treatment of leukemia and lymphoma.
- $37
SizeQTY Cited - VemurafenibT2382918504-65-1Vemurafenib (RG7204) is a B-RAF inhibitor that inhibits RAFV600E and c-RAF-1 (IC50=31/48 nM) selectively and potently. Vemurafenib exhibits antitumor activity and is used for the treatment of BRAF V600E mutation-positive melanoma.
- $50
SizeQTY Cited - UM-164T4597903564-48-7UM-164 (DAS-DFGO-II), a highly potent c-Src inhibitor with a dissociation constant (Kd) of 2.7 nM, also effectively inhibits p38α and p38β.
- $30
SizeQTY
- BafetinibT6311859212-16-1Bafetinib (INNO-406) (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 less effective to c-Kit and PDGFR.
- $31
SizeQTY Cited - FenleanT31773863193-70-8In houseFenlean (FLZ) is a tyrosine kinase Src inhibitor, a synthetic cyclic derivative of squamous amide from Annona glabra, with cytoprotective activity, which protects tyrosine hydroxylase function in a chronic MPTP/prostaglandin-type mouse model of Parkinson's disease.Fenlean inhibits the production of Aβ in the mitochondria, which may be useful in the study of age-related macular degeneration and Parkinson's disease. and Parkinson's.
- $119
SizeQTY - PonatinibT2372943319-70-8Ponatinib (AP24534) is an orally available, multitargeted kinase inhibitor with IC50 values of 0.37 nM (Abl), 1.1 nM (PDGFRα), 1.5 nM (VEGFR2), 2.2 nM (FGFR1), and 5.4 nM (Src).
- $50
SizeQTY Cited - RepotrectinibT40711802220-02-5Repotrectinib (TPX-0005) is a potent ALK ROS1 TRK inhibitor, with IC50 values of 1.01 nM for WT ALK, 5.3 nM for SRC, 1.08 nM for ALK L1196M, and 1.26 nM for ALK G1202R.
- $45
SizeQTY Cited - BosutinibT0152380843-75-4Bosutinib (SKI-606) is a synthetic quinolone derivative and dual kinase inhibitor that targets both Abl (IC50: 1 nM) and Src (IC50: 1.2 nM) kinases.
- $37
SizeQTY Cited - Lyn-IN-1T11916887650-05-7Lyn-IN-1 (Bafetinib analog) is a selective, potent dual inhibitor of Bcr-Abl and Lyn.
- $39
SizeQTY - TG 100801T13157867331-82-6In houseTG 100801 is a dual inhibitor of VEGFr2 and Src family (Src and YES) kinases and is a candidate compound for the treatment of age-related macular degeneration (AMD).
- $84
SizeQTY - URMC-099T60571229582-33-5URMC-099 is an orally bioavailable, brain penetrant MLK inhibitor (IC50: 19/42/14/150 nM, for MLK1/MLK2/MLK3/DLK), and also inhibits LRRK2 activity (IC50: 11 nM).
- $52
SizeQTY - A 419259 trihydrochlorideTQ01321435934-25-0In houseA 419259 trihydrochloride (RK 20449 trihydrochloride) is an Src family kinases inhibitor (IC50s: 9 nM, 3 nM and 3 nM for Src, Lck and Lyn).
- $48
SizeQTY - BGB-102T10531807640-87-5BGB-102 (JNJ-26483327) is a kinase inhibitor targeting FLT3 and YES1 and an antagonist targeting EGFR and VEGFR3, which may be useful in the study of macular degeneration and diseases associated with genetic disorders and malformations.
- $328
SizeQTY - PF 477736T6028952021-60-2PF 477736 (PF-736,PF-00477736) 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.
- $45
SizeQTY - PD173074T2642219580-11-7PD173074 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 FGFR1 than PDGFR and c-Src.
- $36
SizeQTY Cited - TolimidoneT689641964-07-2Tolimidone (NSC 314335) is a chemical compound which inhibits acid secretion in animal models and also acts as a bronchodilator in histamine-challenged animals.
- $43
SizeQTY - AP23846T68455878654-51-4In houseAP23846 is a novel and potent Src family kinase inhibitor that reduces vascular endothelial growth factor and interleukin-8 expression and abrogates downstream angiogenic processes in human solid tumor cell lines.
- $293
SizeQTY - $293
- Beta-HydroxyisovalerylshikoninTN14407415-78-3Beta-Hydroxyisovalerylshikonin is an inhibitor of protein-tyrosine kinases such as v-Src and EGFR, and has been shown to induce apoptosis in several human tumor cell lines. Beta-Hydroxyisovalerylshikonin significantly decreased viability of HCT116 cells (IC50 values = 30.9 μg mL).
- $139
SizeQTY - ScutellareinT3319529-53-3Scutellarein (6-Hydroxyapigenin) reduces inflammatory responses by inhibiting Src kinase activity.
- $110
SizeQTY Cited - PRT062607 hydrochlorideT26961370261-97-4PRT062607 hydrochloride (P505-15 Hydrochloride) is a selective inhibitor of Syk (IC50: 1 nM). It displays at least 80-fold selectivity for Syk over other kinases.
- $33
SizeQTY - PelitinibT2327257933-82-7Pelitinib (EKB-569) (EKB-569) is an effective irreversible EGFR inhibitor (IC50: 38.5 nM).
- $43
SizeQTY Cited - PD-089828T8976179343-17-0PD 089828 is a competitive inhibitor of the receptor tyrosine kinases FGFR1, PDGFRβ, and EGFR (IC50s = 0.15, 1.76, and 5.47 µM, respectively) and a noncompetitive inhibitor of the nonreceptor tyrosine kinase c-Src (IC50 = 0.18 µM)
- $31
SizeQTY - SGI-7079T69821239875-86-5SGI-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 EGFR inhibitor resistance.
- $35
SizeQTY - ZM 306416T1754690206-97-4ZM 306416 (CB 676475), a VEGFR1 inhibitor (IC50: 0.33 μM), can also inhibit EGFR (IC50<10 nM).
- $40
SizeQTY - PP2T6266172889-27-9PP2 (AG 1879,AGL 1879) is a effective inhibitor of Lck/Fyn (IC50:4/5 nM) , ~100-fold less potent to EGFR, inactive for ZAP-70, PKA and JAK2.
- $39
SizeQTY Cited - CH6953755T107842055918-71-1CH6953755 is an orally active, potent and selective YES1 kinase inhibitor (IC50:1.8 nM).CH6953755 has anticancer activity and inhibits cancer cell proliferation by inhibiting YES1 kinase.
- $53
SizeQTY - PD173955T3063260415-63-2PD173955 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 PKC.
- $40
SizeQTY - 1-Naphthyl PP1T3935221243-82-91-Naphthyl PP1 (1-NA-PP 1) is a selective Src inhibitor, targeting v-Src and c-Fyn, c-Abl, CDK2, and CAMK II with IC50 values of 1.0, 0.6, 0.6, 18, and 22 μM, respectively.
- $31
SizeQTY - RigosertibT16750592542-59-1Rigosertib (ON-01910) is a selective, non-ATP-competitive PLK1 inhibitor (IC50: 9 nM) and multi-kinase inhibitor. As a selective anti-cancer agent, Rigosertib induces apoptosis by inhibiting the PI3 kinase Akt pathway, promotes histone H2AX phosphorylation, and induces G2 M arrest in the cell cycle.
- $34
SizeQTY - TirbanibulinT6345897016-82-9Tirbanibulin (KX2-391) is a highly selective Src kinase inhibitor that has demonstrated efficacy in pre-Clinicalal animal models of colon, pancreatic, prostate and breast cancer. It is a substrate-targeted kinase inhibitor. KX2-391, belongs to an emerging new family of targeted cancer treatments called protein kinase inhibitors.
- $35
SizeQTY Cited - KX2-361T9411897016-26-1In houseKX2-361 is a orally bioavailable small molecule dual Src/tubulin inhibitor that provides long term survival in a murine model of glioblastoma
- $74
SizeQTY - Ponatinib HydrochlorideT2372L1114544-31-8Ponatinib Hydrochloride (AP-24534 Hydrochloride) is a hydrochloride of ponatinib. Ponatinib is an orally active multi-targeted kinase inhibitor with IC50s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively.
- $43
SizeQTY - CHIR-124T6350405168-58-3CHIR-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.
- $35
SizeQTY - lavendustin CT4185125697-93-0lavendustin C (NSC 666251) is a potent inhibitor of epidermal growth factor (EGF) receptor-associated tyrosine kinase.
- $37
SizeQTY - MasitinibT2609790299-79-5Masitinib (AB1010) 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 been distributed under the commercial name Masivet. It has been available in Europe since the second part of 2009. In the USA it is distributed under the name Kinavet and has been available for veterinaries since 2011.
- $31
SizeQTY - NVP-BHG712T6348940310-85-0NVP-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 c-Abl with IC50 of 0.395 μM, 1.266 μM and 1.667 μM, respectively.
- $31
SizeQTY - RebastinibT26401020172-07-9DCC-2036 (Rebastinib (DCC-2036)) is a conformational control Bcr-Abl inhibitor for Abl1(WT, IC50: 0.8 nM) and Abl1(T315I, IC50: 4 nM), also inhibits LYN, SRC, HCK, FGR, FLT3, KDR, and Tie-2, and low activity to c-Kit. Rebastinib aimed at the Angiopoietin2-Tie2 pathway.
- $40
SizeQTY Cited - SaracatinibT6078379231-04-6Saracatinib (AZD0530) (AZD0530) is an effective Src inhibitor (IC50: 2.7 nM), and effective to Lck, Fyn, Lyn, Blk, Fgr and c-Yes.
- $59
SizeQTY Cited - CGP77675T30855234772-64-6In houseCGP77675 (ZINC1488120) is a potent and selective inhibitor of Src family kinase with IC50s of 5-20 and 40 nM for the phosphorylation of peptide substrates and autophosphorylation of purified Src. CGP77675 exhibits anticancer activity.
- $43
SizeQTY - Dasatinib monohydrateT1448L863127-77-9Dasatinib monohydrate (BMS-354825 Monohydrate) is an orally bioavailable synthetic small molecule-inhibitor of SRC-family protein-tyrosine kinases. Dasatinib monohydrate binds to and inhibits the growth-promoting activities of these kinases. Apparently, because of its less stringent binding affinity for the BCR-ABL kinase, Dasatinib monohydrate has been shown to overcome the resistance to imatinib of chronic myeloid leukemia (CML) cells harboring BCR-ABL kinase domain point mutations.
- $33
SizeQTY Cited - Osteogenic Growth Peptide (10-14) acetateT37603LOsteogenic Growth Peptide (10-14) acetate (Osteogenic Growth Peptide) is a Src inhibitor and an effective mitogen and stimulator of osteogenesis and hematopoiesis. Osteogenic Growth Peptide (10-14) acetate is responsible for the binding to the OGP receptor and activates an intracell
- $227
SizeQTY - CSF1R-IN-2T131942271119-26-5CSF1R-IN-2 is an oral-active SRC, MET and c-FMS inhibitor (IC50s: 0.12 nM, 0.14 nM and 0.76 nM for SRC, MET and c-FMS respectively).
- $38
SizeQTY - SU6656T6997330161-87-0SU 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.
- $34
SizeQTY - AgerafenibT20701188910-76-0Agerafenib (CEP32496) is a highly potent inhibitor of BRAF.
- $38
SizeQTY
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