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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.

  • eCF506
    T84991914078-41-3
    eCF506 is a potent and selective inhibitor of SRC (IC50 < 0.5 nM)
    • $40
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  • Staurosporine
    T668062996-74-1
    Staurosporine (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.
    • $56
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  • Ibrutinib
    T1835936563-96-1
    Ibrutinib (PCI-32765) is an irreversible inhibitor of BTK (IC50: 0.5 nM) that selectively blocks B cell activation.
    • $36
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  • Nintedanib
    T1777656247-17-5
    Nintedanib (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
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  • TAK-901
    T2709934541-31-8
    TAK-901 has been used in trials studying the treatment of Lymphoma, Myelofibrosis, Multiple Myeloma, Myeloid Metaplasia, and Advanced Solid Tumors, among others.
    • $66
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  • SI-2 hydrochloride
    T129061992052-49-9
    SI-2 hydrochloride (EPH 116 hydrochloride) is a highly promising inhibitor of SRC-3 SMI: SRC-3 (PPI)(IC50 values of 3-20 nM for breast cancer cell death), with acceptable oral availability.
    • $30
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  • Cyt-PTPε Inhibitor-1
    T10927428478-94-8In house
    Cyt-PTPε Inhibitor-1 (A Inhibitor-1) is an inhibitor of cytosolic protein tyrosine phosphatase ε. Cyt-PTPε Inhibitor-1 blocks the dephosphorylation of c-Src and exhibits anti-osteoclastic activity.
    • $58
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  • KX2-361
    T9411897016-26-1In house
    KX2-361 is a orally bioavailable small molecule dual Src/tubulin inhibitor that provides long term survival in a murine model of glioblastoma
    • $123
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  • LCB 03-0110 dihydrochloride
    T326131962928-28-4In house
    LCB 03-0110 Dihydrochloride is a potent inhibitor of the c-Src kinase (IC50 = 1.3 nM) and tyrosine kinases in the BTK and SYK family, as well as in the DDR2 family. It inhibits LPS-induced activation of macrophages and TGF-β1-induced activation of fibroblasts in vitro, inhibits activation of macrophages and fibroblasts, and inhibits scarring in wound healing models.
    • $71
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  • WAY-270250
    T77624852367-46-5
    WAY-270250 is an IGF-1R/SRC inhibitor.
    • $37
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  • CpCDPK1/TgCDPK1-IN-1
    T786051092788-23-2In house
    CpCDPK1/TgCDPK1-IN-1 is a potent dual inhibitor of CpCDPK1 and TgCDPK1, inhibits Abl and Src, and has antiparasitic activity for the study of Toxoplasma infections and cryptosporidiosis.
    • $350
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  • Osteogenic Growth Peptide (10-14) acetate
    T37603L
    Osteogenic 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
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  • BGB-102
    T10531807640-87-5
    BGB-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
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  • AP23846
    T68455878654-51-4In house
    AP23846 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 TargetMol
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  • GW297361
    T75163388627-21-2
    GW297361 is a potent inhibitor of the cell cycle protein-dependent kinase Cdk1 and also inhibits the Pho85 signaling pathway.The IC50s of GW297361 on yeast Cdk1 and Pho85 were 20 nM and 400 nM, respectively.
    • $247
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  • CGP77675
    T30855234772-64-6In house
    CGP77675 (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
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  • ARN25068
    T613602649882-80-2In house
    ARN25068 is a potent inhibitor of GSK-3β, FYN, and DYRK1A protein kinases, exerting its activity in the sub-micromolar range. This compound effectively addresses tau hyperphosphorylation [1].
    • $115
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  • A 419259 trihydrochloride
    TQ01321435934-25-0In house
    A 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
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  • TG 100801
    T13157867331-82-6In house
    TG 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
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  • AZ12672857
    T9650945396-55-4In house
    AZ12672857 is an inhibitor of EphB4 with IC50 of 1.3 nM. AZ12672857 inhibits cell proliferation of Src transfected 3T3 cells with IC50 of 2 nM and autophosphorylation of EphB4 in transfected CHO-K1 cells with IC50 of 9 nM.
    • $64
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  • TG 100572 Hydrochloride
    T13156L867331-64-4In house
    TG 100572 Hydrochloride is a inhibitor of multi-targeted kinase which inhibits receptor tyrosine kinases and Src kinases(IC50s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.1, 0.4, 1, 0.2 nM for VEGFR1, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src, Yes, respectively).
    • $399
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  • WAY-600
    T67301062159-35-6In house
    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); selective for mTOR than PI3Kα (>100-fold) and PI3Kγ (>500-fold).
    • $32
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  • Repotrectinib
    T40711802220-02-5
    Repotrectinib (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.
    • $45
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  • PP121
    T24151092788-83-4
    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) , also inhibits DNA-PK (IC50: 60 nM).
    • $51
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  • Tirbanibulin
    T6345897016-82-9
    Tirbanibulin (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
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  • PP1
    T6196172889-26-8
    PP1 (AGL 1872), a specific and effective Src inhibitor, is with IC50 for Lck Fyn is 5 nM 6 nM, respectively.
    • $34
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  • AD80
    T43011384071-99-1
    AD80, a multikinase inhibitor, inhibits RET, RAF, SRCand S6K, with greatly reduced mTOR activity.
    • $39
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  • Bosutinib
    T0152380843-75-4
    Bosutinib (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
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  • OSI-930
    T2624728033-96-3
    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 growth (angiogenesis) in tumors.
    • $47
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  • Dasatinib monohydrate
    T1448L863127-77-9
    Dasatinib 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
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  • Bafetinib
    T6311859212-16-1
    Bafetinib (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
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  • Scutellarein
    T3319529-53-3
    Scutellarein (6-Hydroxyapigenin) reduces inflammatory responses by inhibiting Src kinase activity.
    • $110
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  • Tofacitinib
    T6321477600-75-2
    Tofacitinib (Tasocitinib) is an oral, small molecule inhibitor of Janus kinases that is used to treat moderate-to-severe rheumatoid arthritis.
    • $30
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  • Vemurafenib
    T2382918504-65-1
    Vemurafenib (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
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  • MLN8054
    T6315869363-13-3
    MLN8054 is a potent and selective Aurora A kinase inhibitor with an IC50 of 4 nM.
    • $48
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  • Saracatinib
    T6078379231-04-6
    Saracatinib (AZD0530) (AZD0530) is an effective Src inhibitor (IC50: 2.7 nM), and effective to Lck, Fyn, Lyn, Blk, Fgr and c-Yes.
    • $59
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  • Rebastinib
    T26401020172-07-9
    DCC-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
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  • 5α-Hydroxycostic acid
    TN3139132185-83-2
    5alpha-Hydroxycostic acid possesses anti-angiogenic ability by interfering the VEGF- and Ang2-related pathways, and it may be a good drug candidate.
    • $162
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  • Dasatinib
    T1448302962-49-8
    Dasatinib (BMS-354825) is a tyrosine kinase inhibitor that inhibits Src and Bcr-Abl (Ki=16/30 pM) and is orally active and ATP-competitive. Dasatinib has antitumor activity and is used in the treatment of leukemia and lymphoma.
    • $37
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  • PP2
    T6266172889-27-9
    PP2 (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
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  • Pelitinib
    T2327257933-82-7
    Pelitinib (EKB-569) (EKB-569) is an effective irreversible EGFR inhibitor (IC50: 38.5 nM).
    • $43
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  • Ponatinib
    T2372943319-70-8
    Ponatinib (AP24534) 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).
    • $50
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  • PD173074
    T2642219580-11-7
    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 FGFR1 than PDGFR and c-Src.
    • $36
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  • 1-Naphthyl PP1 hydrochloride
    T7371956025-47-1
    1-Naphthyl PP1 hydrochloride (1-NA-PP 1 hydrochloride) is a selective inhibitor of src family kinases v-Src
    • $31
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  • GluR6 antagonist-1
    T9723323176-64-3
    GluR6 antagonist-1 inhibits the pY binding site of tyrosine kinase p56lck SH2 domain.
    • $38
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  • NCGC00262650
    T8995344359-25-7
    NCGC00262650 is an inhibitor of AMA1-RON2 interaction and c-Src tyrosine kinase activity.
    • $34
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  • 7-Hydroxy-4H-chromen-4-one
    T734559887-89-7
    7-Hydroxy-4H-chromen-4-one (7-hydroxy-4-benzopyrone) is a Src kinase inhibitor (IC50 of <300 μM).
    • $30
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  • AD57
    T22552L1093380-42-7
    AD57 is a potent inhibitor of both c-Src and Abl with IC50 of 0.025 μM and 0.041 μM, respectively.
    • $47
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  • Hck-IN-1
    T115381473404-51-1
    Hck-IN-1 is a selective Nef-dependent Hck inhibitor (IC50s: 2.8 μM and >20 μM for Nef:Hck complex and Hck) with antiretroviral activity. Hck-IN-1 is a direct and wide HIV-1 Nef antagonist with an IC50 of 100-300 nM for wild-type HIV-1 replication.
    • $133
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  • Masitinib mesylate
    T85441048007-93-7
    Masitinib mesylate (AB-1010 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,respectively).
    • $30
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