c-Kit

SCFR; CD117

c-Kit

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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.

c-Kit Related Products (160)
Recombinant Proteins (12)
Antibodies (3)

By Effects:	Substrate (1) Inhibitors (152)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-168580

c-Kit-IN-7	Inhibitor
c-Kit-IN-7 (Compound 104) is a potent inhibitor of c-Kit, with IC₅₀ values of ≤10 nM. c-Kit-IN-7 inhibits the cell proliferation in GIST430 and BaF3 mutants, with IC₅₀ values of ≤100 nM. c-Kit-IN-7 plays an important role in cancer driven by c-KIT kinase mutations research.

HY-150582

c-Met-IN-14	Inhibitor
c-Met-IN-14 (compound 26af) is a selective inhibitor of c-Met kinase from N-sulfonylamidine-based derivatives, with an IC₅₀ value of 2.89 nM. c-Met-IN-14 shows anticancer activity by blocking phosphorylation of c-Met, and arrests cell cycle at G2/M phase. c-Met-IN-14 induces apoptosis of A549 cells in a dose-dependent manner.

HY-50905S

Dovitinib-d₈	Inhibitor
Dovitinib-d₈ is the deuterium labeled Dovitinib. Dovitinib (CHIR-258) is a multi-targeted tyrosine kinase inhibitor with IC₅₀s of 1, 2, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, FGFR1/FGFR3, VEGFR1/VEGFR2/VEGFR3 and PDGFRα/PDGFRβ, respectively.

HY-153920A

Pimicotinib hydrochloride	Inhibitor
Pimicotinib (ABSK021) hydrochloride is a selective and orally active CSF1R inhibitor with an IC₅₀ value of 19.48 nM (determined by inhibiting ADP production). Pimicotinib hydrochloride exhibits anti-tumor activity.

HY-10331AR

Regorafenib monohydrate (Standard)	Inhibitor
Regorafenib (monohydrate) (Standard) is the analytical standard of Regorafenib (monohydrate). This product is intended for research and analytical applications. Regorafenib (BAY 73-4506) monohydrate is an orally active and potent multi-targeted receptor tyrosine kinase inhibitor, with IC₅₀ values of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively. Regorafenib monohydrate shows very robust antitumor and antiangiogenic activity.

HY-13838A

PLX647 dihydrochloride	Inhibitor
PLX647 dihydrochloride is an orally active, highly specific dual FMS and KIT kinase inhibitor, with IC₅₀s of 28 and 16 nM, reapectively. PLX647 dihydrochloride shows selectivity for FMS and KIT over a panel of 400 kinases at a concentration of 1 μM except FLT3 and KDR (IC₅₀s=91 and 130 nM, respectively).

HY-117873A

KBP-7018 hydrochloride	Inhibitor
KBP-7018 hydrochloride is a tyrosine kinase-selective inhibitor. KBP-7018 hydrochloride has potent inhibitory effects on c-KIT, PDGFR, and RET with IC₅₀ values of 10 nM, 7.6 nM and 25 nM, respectively. KBP-7018 hydrochloride can be used for the research of idiopathic pulmonary fibrosis.

HY-10330S

Toceranib-d₈	Inhibitor	99.08%
Toceranib-d₈ is the deuterium labeled Toceranib. Toceranib (SU11654) is an orally active receptor tyrosine kinase (RTK) inhibitor, and it potently inhibits PDGFR, VEGFR, and Kit with Kis of 5 and 6 nM for PDGFRβ and Flk-1/KDR, respectively. Toceranib (SU11654) has antitumor and antiangiogenic activity, and used in the treatment of canine mast cell tumors.

HY-110071

APcK110	Inhibitor
APcK110 is a potent Kit inhibitor that can be used for the research of acute myeloid leukemia (AML). APcK110 induces AML cell apoptosis.

HY-18949

JI6	Inhibitor
JI6 is a potent, selective and orally active FLT3 inhibitor, with IC₅₀s of ～40, 8, and 4 nM for FLT3-WT, FLT3-D835Y, and FLT3-D835H, respectively. JI6 also inhibits JAK3 and c-Kit, with IC₅₀s of ～250 and ～500 nM, respectively. JI6 can be used for the research of acute myeloid leukemia.

HY-150026

Multi-kinase-IN-2	Inhibitor
Multi-kinase-IN-2 (compound 7h) is an orally active and potent angiokinase inhibitor. Multi-kinase-IN-2 exhibits excellent inhibitory activity against angiokinases including VEGFR-1/2/3, PDGFRα/β, and FGFR-1, as well as LYN and c-KIT kinases. Multi-kinase-IN-2 significantly attenuates phosphorylation of AKT and ERK proteins. Multi-kinase-IN-2 induces cell apoptosis. Multi-kinase-IN-2 shows anticancer activity.

HY-121708

KI-328	Inhibitor
KI-328 is a novel inhibitor targeting KIT kinase that has selective activity against some KIT mutant kinases commonly found in acute myeloid leukemia (AML). KI-328 showed specificity for KIT kinase in in vitro kinase assays and inhibited the growth of wild-type (Wt) and mutant KIT-expressing cells, but had lower activity against D816V-KIT. Comparative analysis of the inhibitory effects of several potent KIT inhibitors on the growth of multiple mutant KIT-expressing cells showed that the multi-kinase inhibitors had comparable activity against D816V-KIT as against other mutant KITs; however, heat shock protein 90 (HSP90) inhibitors showed significant activity against D816V-KIT, inhibiting the growth of D816V-KIT-expressing cells at concentrations that did not affect the growth of other mutant KIT-expressing cells. These results suggest that potent KIT inhibitors have different activities against different types of KIT mutant kinases. Therefore, in clinical development, KIT inhibitors need to validate their activity against multiple types of KIT mutant kinases.

HY-139996

Pomalidomide-C5-Dovitinib	Inhibitor
Pomalidomide-C5-Dovitinib (compound 2) is a PROTAC containing Pomalidomide, Dovitinib and connected with CRBN. Pomalidomide-C5-Dovitinib shows enhanced antiproliferative effects against FLT3-ITD+ AML cells. Pomalidomide-C5-Dovitinib induces the degradation of the FLT3-ITD and KIT proteins in a ubiquitin-proteasome-dependent manner and completely blocks their downstream signaling pathway. Pomalidomide-C5-Dovitinib has the potential for the research of FLT3-ITD⁺ acute myeloid leukemia.

HY-149019

Antitumor agent-70	Inhibitor
Antitumor agent-70 (compound 8b) has anti-tumor activity and can induce cell apoptosis. Antitumor agent-70 inhibits multiple myeloma with an IC₅₀ value of 0.12 μM. Antitumor agent-70 is a potential multi-targeted kinase inhibitor especially for c-Kit.

HY-160689

GW694590A	Inhibitor
GW694590A (UNC10112731) is a MYC protein stabilizer that increases endogenous MYC protein levels. GW694590A also targets receptor tyrosine kinases, inhibiting DDR2, KIT and PDGFRα by 81% at 1 μM. , 68% and 67%. GW694590A is a protein kinase inhibitor across ATP-dependent and -independent luciferases with potential effects on the Fluc reporter gene.

HY-156470

Multi-kinase-IN-6	Inhibitor
Multi-kinase-IN-6 (compound 10e) is a multikinase inhibitor that shows good enzyme inhibitory activity against TrkA, ALK2, c-KIT, EGFR, PIM1, CK2α, CHK1, and CDK2. Multi-kinase-IN-6 reveals antiproliferative activity against MCF7, HCT116 and EKVX with IC₅₀ values of 3.36 μM, 1.40 μM and 3.49 μM, respectively. Multi-kinase-IN-6 shows cell cycle arrest at the G1/S phase and G1 phase in MCF7 and HCT116 cells with good apoptotic effect.

HY-149415

Multi-kinase-IN-5	Inhibitor
Multi-kinase-IN-5 (compound 15c) is a promising multi-kinase inhibitory agent. Multi-kinase-IN-5 inhibits a panel of protein kinases (RET, KIT, cMet, VEGFR1,2, FGFR1, PDGFR and BRAF), showing % inhibition of 74%, 31%, 62%, 40%, 73%, 74%, 59%, and 69%, respectively, and IC₅₀ of 1.287, 0.117 and 1.185 μM against FGFR1, VEGFR, and RET kinases, respectively.

HY-168581

c-Kit-IN-8	Inhibitor
c-Kit-IN-8 (Compound 53) is an inhibitor for c-Kit kinase, that inhibits uKIT kinase with an IC₅₀ > 1 μM. c-Kit-IN-8 inhibits the proliferation of cancer cell GIST430 and BaF3 wildtype and mutants with IC₅₀ > 0.1 μM.

HY-114588

Tafetinib analogue 1	Inhibitor
Tafetinib (SIM010603) analogue 1 is an analog of the tyrosine kinase receptor inhibitor Tafetinib (SIM010603)..

HY-50946R

Imatinib Mesylate (Standard)	Inhibitor
Imatinib (Mesylate) (Standard) is the analytical standard of Imatinib (Mesylate). This product is intended for research and analytical applications. Imatinib Mesylate (STI571 Mesylate) is a tyrosine kinases inhibitor that inhibits c-Kit, Bcr-Abl, and PDGFR (IC₅₀=100 nM) tyrosine kinases.

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c-Kit

c-Kit

c-Kit Related Products (160)

Recombinant Proteins (12)

Antibodies (3)

c-Kit Related Products (160):