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Request The Product List ofc-Kit c-Kit

c-Kit (Mast/stem cell growth factor receptor, SCFR or CD117) is a proteinthat in humans is encoded by the KIT gene. c-Kit (CD117) is an important cell surface marker used to identify certain types of hematopoietic(blood) progenitors in the bone marrow. c-Kit is a cytokine receptor expressed on the surface of hematopoietic stem cells as well as other cell types. Altered forms of this receptor may be associated with some types of cancer. c-Kit is a receptor tyrosine kinase type III, which binds to stem cell factor. When c-Kit binds to stem cell factor (SCF) it forms adimer that activates its intrinsic tyrosine kinase activity, that in turn phosphorylates and activates signal transduction molecules that propagate the signal in the cell. Signalling through c-Kit plays a role in cell survival, proliferation, and differentiation.

Cat. No. Product Name CAS No. Information
GY03922

ISCK03

945526-43-2

A specific c-Kit inhibitor that inhibits c-kit phosphorylation in vitro and SCF-induced c-kit phosphorylation in human melanoma cells; also inhibits p44/42 ERK mitogen-activated protein kinase (MAPK) phosphorylation, does not inhibit HGF-induced phosphorylation of p44/42 ERK proteins; induces the dose-dependent depigmentation of newly regrown hair, promotes the depigmentation of UV-induced hyperpigmented spots in vivo; orally acitve.

GY02792

Avapritinib

1703793-34-3

Avapritinib (BLU-285) is a potent and highly selective inhibitor of mutant KIT and PDGFRα with IC50 of 0.6, 0.27 and 0.24 nM for KIT del557-558, KIT D816V and PDGFRA D842V, respectively; displays weak inhibition against WT KIT with IC50 of 73 nM, >150-fold more potent on KIT D816V than several important kinase antitargets such as VEGFR2, SRC and FLT3; inhibits other well-characterized disease-driving KIT mutants both in vitro and in vivo in preclinical models, demonstrates marked activity in patients with diseases associated with KIT and PDGFRA (GIST) activation loop mutations.

GY10077

AZD3229

AZD3229 (AZD-3229) is a potent, pan-KIT mutant inhibitor with potent single digit nM growth inhibition against a diverse panel of mutant KIT driven Ba/F3 cell lines (GI50=1-50 nM); shows good margin to KDR-driven effects, also inhibits PDGFR mutants (Tel-PDGFRα, Tel-PDGFRβ, V561D/D842V).

GY02161

Sitravatinib

1123837-84-2

A novel, broad spectrum small molecule inhibitor that blocks a wide array of RTKs known to be amplified/overexpressed in sarcomas, including c-Kit, PDGFRβ, PDGFRα, c-Met, and Axl (IC50=1.5-30 nM); significantly blocks the phosphorylation of potential driver RTKs and induces potent anti-proliferative effects in vitro; suppresses tumor growth in tumor xenografts in vivo.

GY02106

Masitinib mesylate

1048007-93-7

A potent tyrosine kinase inhibitor targeting c-Kit and PDGFR with IC50 of 0.15 and 0.05 uM in cell based assays; also inhibits Lyn, and to a lesser extent, FGFR3, and inhibits KIT gain-of-function mutants V559D (IC50=3.0 nM) and Δ27 mouse mutant (IC50=5 nM); dose-dependently inhibits SCF-induced cell proliferation in Ba/F3 cells expressing human wild-type KIT (IC50=150 nM); inhibits tumour growth in vivo.

GY01659

OSI-930

728033-96-3

OSI-930 is a potent, orally active, dual inhibitor of c-Kit and VEGFR-2 (KDR) with IC50 of 15 nM and 9 nM, respectively; also inhibits Lck, c-Raf, Flt1, and CSF-1R (IC50<100 nM); exhibits antitumor activity in mutant Kit-expressing HMC-1 xenograft model.

GY01551

Amuvatinib

850879-09-3

Amuvatinib is a novel RTK inhibitor that effectively inhibits c-Kit, PDGFRα and Flt3 with IC50 of 10 nM, 40 nM and 81 nM, respectively; also inhibits several mutants of c-Kit and Axl; inhibits prostate cancer cell proliferation (IC50=4-8 uM), promotes cell cycle arrest and apoptosis; completely inhibites phosphorylation of the HER members (HER1, 2, 3), binding of PI3K regulatory unit p85 to HER3 and downstream Akt activity in combination with Erlotinib; exhibits synergistic effect in LNCaP mouse xenograft model.

GY01204

Masitinib

790299-79-5

Masitinib is a potent tyrosine kinase inhibitor targeting c-Kit and PDGFR with IC50 of 0.15 and 0.05 uM in cell based assays; also inhibits Lyn, and to a lesser extent, FGFR3, and inhibits KIT gain-of-function mutants V559D (IC50=3.0 nM) and Δ27 mouse mutant (IC50=5 nM); dose-dependently inhibits SCF-induced cell proliferation in Ba/F3 cells expressing human wild-type KIT (IC50=150 nM); inhibits tumour growth in vivo.

GY05989

KBP-7018

1613437-66-3

KBP-7018(KBP 7018;KBP7018) is a novel potent, multikinase inhibitor with IC50 of 10, 7.6 and 25 nM for c-Kit, RET and PDGFRβ, respectively; also potently inhibits FLT3, VEGFR2, Fyn, PDGFRα and VEGFR2; shows promising outcomes for the treatments of idiopathic pulmonary fibrosis (IPF).

GY05988

KBP-7018 hydrochloride

1613437-67-4

KBP-7018 hydrochloride (KBP 7018;KBP7018) is a novel potent, multikinase inhibitor with IC50 of 10, 7.6 and 25 nM for c-Kit, RET and PDGFRβ, respectively; also potently inhibits FLT3, VEGFR2, Fyn, PDGFRα and VEGFR2; shows promising outcomes for the treatments of idiopathic pulmonary fibrosis (IPF).

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