c-kit kinase

Sorafenib (Bay 43-9006) is a multikinase inhibitor that targets Raf-1, B-Raf, VEGFR2, VEGFR3, VEGFR4, PDGFRβ, FLT3, c-Kit, and others (IC50=6 22 90 15 20 20 57 58 nM) with oral activity. It exhibits antitumor properties and can induce autophagy, apoptosis, and agonistic iron death.

Imatinib Mesylate (STI-571) is a tyrosine kinase receptor inhibitor with antineoplastic activity (IC50s: 0.6 μM, 0.1 μM and 0.1 μM for v-Abl, c-Kit and PDGFR, respectively).

Gilteritinib (ASP2215) is a potent inhibitor of FMS-related tyrosine kinase 3 (FLT3) and AXL tyrosine kinase receptors (IC50 = 0.29 nM and <1 nM, respectively). In preclinical studies, gilteritinib demonstrated strong antileukemic and antitumor effects. Gilteritinib is currently in several Phase 3 clinical trials for acute myeloid leukemia.

Ripretinib (DCC-2618) is an orally bioavailable inhibitor of (KIT) and (PDGFRA).

c-Kit-IN-3 is a selective inhibitor of c-KIT kinase with IC50s of 4 nM and 8 nM for c-Kit (wt) and c-Kit (T670I).

Famitinib (SHR1020) is a potent orally active multi-targeted kinase inhibitor that effectively inhibits the activity of c-kit, VEGFR-2, and PDGFRβ with IC50 values of 2.3 nM, 4.7 nM, and 6.6 nM, respectively [1]. It demonstrates remarkable antitumor properties in human gastric cancer cells and xenografts, inducing apoptosis [2].

Sorafenib tosylate (Bay 43-9006) is a potent multikinase inhibitor (IC50s: 6 20 22 nM for Raf-1 VEGFR-3 B-Raf).

Sunitinib Malate (Sunitinib) is an indolinone-based tyrosine kinase inhibitor. It blocks the tyrosine kinase activities of VEGFR2, PDGFRβ (IC50: 80 2 nM), and c-kit.

Regorafenib (BAY 73-4506) is an orally active, multi-targeted receptor tyrosine kinase inhibitor that inhibits RET, C-RAF, VEGFR2, c-Kit, VEGFR1, and PDGFRβ, exhibiting both antitumor and anti-angiogenic activity.

Regorafenib Monohydrate is a novel oral multikinase inhibitor with IC50 values of 13, 4.2, 46, 22, 7, 1.5, 2.5, 28, 19 nM for VEGFR1, murine VEGFR2, murine VEGFR3, PDGFR-β, KIT, RET, RAF-1, B-RAF and B-RAF(V600E) respectively.

Cabozantinib S-malate (XL184) is the s-malate salt form of cabozantinib, an orally bioavailable, small molecule receptor tyrosine kinase (RTK) inhibitor with potential antineoplastic activity.

Pexidartinib (PLX-3397) is a capsule containing a small-molecule receptor tyrosine kinase (RTK) inhibitor targeting KIT, CSF1R, and FLT3, with potential antineoplastic activity.

Ponatinib (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).

Cediranib (AZD2171) (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-fold) in HUVEC cells.

Cabozantinib (XL184) is a multi-targeted tyrosine kinase receptor inhibitor that inhibits VEGFR2, c-Met, Kit, Axl, and Flt3 (IC50=0.035 1.3 4.6 7 11.3 nM). Cabozantinib exhibits both antitumor and antiangiogenic activity.

Imatinib (STI571) is a multi-targeted receptor tyrosine kinase inhibitor that selectively inhibits the kinase activities of BCR ABL, v-Abl, PDGFR, and c-kit with oral activity. Imatinib has antitumor activity for the treatment of chronic granulocytic leukemia.

Amuvatinib (MP470) is an orally bioavailable synthetic carbothioamide with potential antineoplastic activity.

AST 487 (NVP-AST 487) is a RET kinase inhibitor, inhibiting RET autophosphorylation and activation of downstream effectors. It also can inhibit Flt-3.

Sitravatinib (MGCD516) is an inhibitor targeting multiple RTKs involved in driving sarcoma cell growth, including c-Met, c-Kit, PDGFRα β, PDGFR, and Axl.

AZD2932 is a potent, multi-targeted kinase inhibitor of VEGFR2, PDGFβ, Flt-3, and c-Kit.

KG5 is a dual allosteric inhibitor of PDGFRβ and B-Raf with a Kd of 520 nM and 300 nM for PDGFRβ and PDGFRα. KG5 inhibits FLT3, KIT, and c-Raf with anticancer and antiangiogenic activities.

AC710 is a potent PDGFR inhibitor with Kds of 0.6 nM for FLT3, 1 nM for KIT, 1.57 nM for CSF1R, 1.3 nM for PDGFRα, and 1 nM for PDGFRβ.

CHMFL-ABL KIT-155 is a highly potent and orally active type II ABL c-KIT dual kinase inhibitor (IC50s: 46 nM 75 nM). It arrests cell cycle progression and induces apoptosis.

Ilorasertib hydrochloride (ABT-348 hydrochloride) is an ATP-competitive multitargeted kinase inhibitor, which inhibits Aurora C, Aurora B, and Aurora A (IC50s: 1 nM, 7 nM, 120 nM). It also suppresses RET tyrosine kinase, PDGFRβ, and Flt1 (IC50s: 7 nM, 3 nM, and 32 nM).