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c-Kit
T0093 Sorafenib tosylate Sorafenib Tosylate is the tosylate salt of sorafenib, a synthetic compound targeting growth signaling and angiogenesis. Sorafenib blocks the enzyme RAF kinase, a critical component of the RAF/MEK/ERK signaling pathway that controls cell division and proliferation; in addition, sorafenib inhibits the
T0097L Pazopanib Pazopanib, a small molecule inhibitor, inhibits multiple protein tyrosine kinases with potential antineoplastic activity. Pazopanib selectively inhibits VEGFR-1, -2 and -3, c-kit and PDGF-R, which may result in inhibition of angiogenesis in tumors in which these receptors are upregulated.
T0374L Sunitinib Sunitinib, a multi-targeted RTK inhibitor, is targeting PDGFRβ and VEGFR2 (Flk-1) with IC50 of 2 nM and 80 nM and also inhibits c-Kit.
T1448 Dasatinib Dasatinib Anhydrous is an orally bioavailable synthetic small molecule-inhibitor of SRC-family protein-tyrosine kinases.
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-promoting activities of these kinases. Apparently, because of its less stringent binding affinity for the BCR-ABL kinase, dasatinib has been shown
T1621 Imatinib Mesylate Imatinib mesylate is a specific tyrosine kinase receptor inhibitor with antineoplastic activity, used in the therapy of Philadelphia chromosome-positive chronic myelogenous leukemia and gastrointestinal stromal tumors.
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 and >100-fold selectivity for the same target versus FGFR, EGFR, and KDR.
T1792 Regorafenib Regorafenib is a Kinase Inhibitor. The mechanism of action of regorafenib is as a Protein Kinase Inhibitor, and Cytochrome P450 2C9 Inhibitor.
T1797 XL184(Cabozantinib malate) Cabozantinib S-malate is the s-malate salt form of cabozantinib, an orally bioavailable, small molecule receptor tyrosine kinase (RTK) inhibitor with potential antineoplastic activity.
T1830 BX795 BX795 is an effective and selective PDK1 inhibitor (IC50: 6 nM), and its selectivity is 140- and 1600-fold for PDK1 over PKA and PKC in cell-free assays, respectively. Meanwhile, the selectivity for PDK1 is 100-fold than GSK3β.
T1836 AZD2932 AZD2932 is a potent and multi-targeted kinase inhibitor VEGFR2, PDGFβ, Flt-3, and c-Kit.
T1925 PLX647 PLX647 is a highly selective dual FMS/KIT kinase inhibitor (IC50: 28/16 nM).
T2070 CEP-32496 CEP-32496 is a highly potent inhibitor of BRAF.
T2115 Pexidartinib Pexidartinib is a capsule formulation containing a small-molecule receptor tyrosine kinase (RTK) inhibitor of KIT, CSF1R and FLT3 with potential antineoplastic activity.
T2288L Motesanib Diphosphate (AMG-706) Motesanib Diphosphate is the orally bioavailable diphosphate salt of a multiple-receptor tyrosine kinase inhibitor with potential antineoplastic activity.
T2341 KW-2449 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-1R, EGFR.
T2372 Ponatinib Ponatinib is a tyrosine kinase receptor inhibitor that is used in the therapy of refractory chronic myelogenous leukemia (CML) positive for the Philadelphia chromosome.
T2446 KI8751 KI8751 is a potent and selective inhibitor of VEGFR2 with IC50 of 0.9 nM.
T2500 Cediranib Cediranib (AZD2171) is a highly potent (IC50 < 1 nmol/L) ATP-competitive inhibitor of recombinant KDR tyrosine kinase in vitro, also inhibits Flt1/4 (IC50: 5 nM/≤3 nM), similar activity against PDGFRβ and c-Kit, selective more for VEGFR than PDGFR-α (36-fold), CSF-1R (110-fold), and Flt3 (1000-
T2514 Linifanib Linifanib (ABT-869) is a novel, potent ATP-competitive VEGFR/PDGFR inhibitor for KDR (IC50: 4 nM), CSF-1R (IC50: 3 nM), Flt-1/3 (IC50: 3/4 nM) and PDGFRβ (IC50: 66 nM). Linifanib may exhibit potent antiproliferative and apoptotic effects on tumor cells whose proliferation is dependent on mutant kin
T2516 Amuvatinib(MP470) Amuvatinib is an orally bioavailable synthetic carbothioamide with potential antineoplastic activity.
T2582 Apatinib Apatinib is an orally bioavailable and specific VEGFR2 inhibitor (IC50: 1 nM). In addition, this agent mildly inhibits c-Kit and c-SRC tyrosine kinases.
T2586 Cabozantinib Cabozantinib is an orally bioavailable, small molecule receptor tyrosine kinase (RTK) inhibitor with potential antineoplastic activity.
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 been distributed under the commercial name Masivet. It has been available in Europe since the second part of 2009. In the USA it is distrib
T2668 JNK-IN-8 JNK-IN-8 is an irreversible JNK1/2/4 inhibitor (IC50: 4.7/18.7/1 nM). The selectivity is higher 10-fold than MNK2, Fms and no inhibition of Met, c-Kit, PDGFRβ in A375 cell line.
T3452 ISCK03 ISCK03 is a selective SCF/c-Kit inhibitor.
T4053 AST 487 AST 487 is a RET kinase inhibitor, inhibiting RET autophosphorylation and activation of downstream effectors. It also can inhibit Flt-3.
T4332 DCC-2618 DCC-2618 is an effective inhibitor of c-Met and c-Kit (IC50s<200 nM).
T6078 Saracatinib Saracatinib (AZD0530) is an effective Src inhibitor (IC50: 2.7 nM), and effective to c-Yes, Lyn, Fyn, Fgr, Blk and Lck; less active for Abl and EGFR (L858R and L861Q).
T6091 CP-673451 CP-673451 is a specific inhibitor of PDGFRα/β (IC50: 10/1 nM) with antiangiogenic and antitumor activity and the selectivity is higher 450-fold than other angiogenic receptors.
T6097 GNF-5837 GNF-5837 is a specific, and orally bioavailable pan-TRK inhibitor for TrkA/TrkB (IC50: 8/12 nM).
T6137 KRN-633 KRN-633 is an effective VEGFR inhibitor. The IC50s of KRN-633 for VEGFR1, VEGFR2, and VEGFR3 is 170, 160 and 125 nM, respectively.
T6166 Telatinib Telatinib is an effective inhibitor of VEGFR2/3, c-Kit, and PDGFRα. The IC50s of Telatinib forVEGFR2/3, c-Kit and PDGFRα are 6 nM/4 nM, 1 nM, and 15 nM, respectively.
T6193 Dovitinib (TKI-258) Dilactic Acid Dovitinib Dilactic acid (TKI258 Dilactic acid) is the Dilactic acid of Dovitinib, which is a multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit) with IC50 of 1 nM/2 nM, also potent to class IV (FGFR1/3) and class V (VEGFR1-4) RTKs with IC50 of 8-13 nM, less potent to InsR, EGFR, c-Met, Ep
T6196 PP1 PP1, a specific and effective Src inhibitor, is with IC50 for Lck/Fyn is 5 nM/ 6 nM, respectively.
T6230 Imatinib (STI571) Imatinib is a tyrosine kinase inhibitor and ANTINEOPLASTIC AGENT that inhibits the BCR-ABL kinase created by chromosome rearrangements in CHRONIC MYELOID LEUKEMIA and ACUTE LYMPHOBLASTIC LEUKEMIA, as well as PDG-derived tyrosine kinases that are overexpressed in gastrointestinal stromal tumors.
T6289 Dovitinib Dovitinib (TKI258, CHIR258) is a multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit, IC50: 1/2 nM), also effective to class IV (FGFR1/3) and class V (VEGFR1-4) RTKs (IC50: 8-13 nM), less potent to EGFR, InsR, EphA2, c-Met, IGF-1R, Tie2, and HER2.
T6479 Dovitinib (TKI258) Lactate Dovitinib (TKI258) Lactate is the Lactate of Dovitinib, which is a multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit) with IC50 of 1 nM/2 nM, also potent to class IV (FGFR1/3) and class V (VEGFR1-4) RTKs with IC50 of 8-13 nM, less potent to InsR, EGFR, c-Met, EphA2, Tie2, IGFR1 and HER2.
T6711 Tyrphostin AG 1296 Tyrphostin AG 1296 is an inhibitor of PDGFR with IC50 of 0.3-0.5 μM, no activity to EGFR.
T4320 Flumatinib Flumatinib is an orally bioavailable tyrosine kinase inhibitor flumatinib, with potential antineoplastic activity.
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