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c-Kit
c-Kit, a type III receptor tyrosine kinase (RTK), plays a crucial role in cancer occurrence. Currently, c-Kit is mainly considered a stem cell factor (SCF), which participates in vital functions of the human body, such as fertility, homeostasis, and melanogenesis; nevertheless, early studies on c-Kit introduced it as an oncogene. Deregulation of c-Kit, including overexpression and gain of function mutations, has been detected in several human cancers. Leukemia is the first cancer linked to c-Kit activating mutation. c-Kit, a protooncogene in a region on the long arm of chromosome 4 (4q11–4q13), encodes the SCF receptor (CD117). c-Kit also plays an important role in stem cell maintenance and differentiation. Numerous Kit mutation sites are found and vary in different cancer types,16 reflecting the effect of each mutation on downstream signaling pathways including PI3K, Src kinase and Ras-Erk. Kinase superfamily proteins are considered a main target for molecular cancer therapy, so the use of kinase inhibitors could significantly improve cancer treatment.
References
1.Maryam Abbaspour Babaei,et al. Drug Des Devel Ther. 2016; 10: 2443–2459.
References
1.Maryam Abbaspour Babaei,et al. Drug Des Devel Ther. 2016; 10: 2443–2459.
Angiogenesis
c-Kit
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BLU-263
catalog no : M37619
cas no: 2505078-08-8
BLU-263 is an investigational, potent, and selective oral small molecule inhibitor of KIT with sub-nanomolar potency against D816V-mutant KIT.
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Bezuclastinib
catalog no : M35498
cas no: 1616385-51-3
Bezuclastinib (CGT9486) is a novel, potent and highly selective tyrosine kinase and c-kit D816V inhibitor for the study of advanced mastocytosis.
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M4205
catalog no : M28834
cas no: 2590556-80-0
M4205 is an inhibitor of c-Kit exhibiting high activity on c-Kit mutations in exons 11, 13, 17.
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c-Kit-IN-3
catalog no : M26080
cas no: 2363169-01-9
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).
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CS-2660
catalog no : M25002
cas no: 951151-97-6
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.