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.

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

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

GNF-5837 is a specific, and orally bioavailable pan-TRK inhibitor for TrkA TrkB (IC50: 8 12 nM).

JNJ-38158471 (CS-2660), a highly selective, orally available, well tolerated VEGFR2 inhibitor with IC50 of 40 nM, inhibits closely related tyrosine kinases such as Ret and Kit with IC50 of 180 nM and 500 nM.

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.

Linifanib (AL-39324) (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 kinases, such as FMS-related tyrosine kinase receptor-3 (FLT3).

Masitinib (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.

SU14813 is a multi-receptor tyrosine kinase inhibitor with potent antiangiogenesis and antitumor activity (IC50s of 50, 2, 4, 15 nM for VEGFR2, VEGFR1, PDGFRβ and KIT).

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).

c-Kit-IN-2 is a c-KIT inhibitor (IC50: 82 nM) exhibiting superior antiproliferative activities against all three GIST cell lines, GIST430, GIST882, and GIST48 (GI50s: 1, 3, and 2 nM).

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.

c-Kit-IN-3 D-tartrate is a potent and selective c-KIT kinase inhibitor (IC50s: 4 nM, 8 nM for c-KIT wt, and c-KIT T670I).

c-Kit-IN-3 hydrochloride is a potent and selective c-KIT kinase inhibitor (IC50s: 4 nM, 8 nM for c-KIT wt, and c-KIT T670I).

c-Kit-IN-3 L-tartrate is a potent and selective c-KIT kinase inhibitor (IC50s: 4 nM, 8 nM for c-KIT wt, and c-KIT T670I).

c-Kit-IN-3 maleate is a potent and selective c-KIT kinase inhibitor (IC50s: 4 nM, 8 nM for c-KIT wt, and c-KIT T670I).

c-Kit-IN-3 tartrate is a potent and selective c-KIT kinase inhibitor (IC50s: 4 nM, 8 nM for c-KIT wt, and c-KIT T670I).

C-Kit-IN-6 (Compound 101) is an inhibitor of c-Kit, demonstrating IC50 values ranging from 100 nM to 1 μM.

C-Kit-IN-8 (Compound 53) acts as an inhibitor of c-Kit kinase, hampering uKIT kinase activity with an IC50 greater than 1 μM. Additionally, it inhibits the proliferation of both wild-type and mutant GIST430 and BaF3 cancer cells, exhibiting an IC50 greater than 0.1 μM.

c-Kit-IN-7 (compound 104) serves as an effective inhibitor of c-Kit, exhibiting an IC50 of 10 nM or less. It plays a crucial role in cancer research.

KIT PDGFRA-IN-1 (compound 19) is an inhibitor targeting the stem cell growth factor receptor (KIT) and platelet-derived growth factor receptor alpha (PDGFRA). Its IC50 values are 2.3 µM for KIT-wt, 12 µM for KIT-D816H, 492 µM for KIT-T670I, 0.8 µM for PDGFRA-wt, 99.9 µM for PDGFRA-D842V, 42.3 µM for PDGFRA-T674I, and 4.3 µM for PDGFRA-G680R. The GR50 values for GIST-T1, T1-a-D842V, and GIST-48B cell lines (gastrointestinal stromal tumor cell lines with PDGFR and KIT mutations) are 12 nM, 8900 nM, and ≥10,000 nM, respectively.

c-Kit-IN-1 (DCC-2618) is an effective inhibitor of c-Met and c-Kit (IC50s<200 nM).

Anti-c-Kit CD117 Antibody (SR-1) is a mouse IgG2a, κ chimeric antibody that specifically targets human c-Kit CD117. The recommended isotype control for this antibody is Mouse IgG2a kappa, Isotype Control.