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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
产品货号 : M37619
cas no: 2505078-08-8
Elenestinib (BLU-263) 是一种有效的口服活性酪氨酸激酶 (tyrosine kinase) 抑制剂。Elenestinib 具有研究系统性肥大细胞增多症（SM）的潜力。Elenestinib 抑制 KIT D816V 的 IC50 为 0.2 nM。
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Bezuclastinib
产品货号 : M35498
cas no: 1616385-51-3
Bezuclastinib (CGT9486) 是一种口服活性、高选择性的酪氨酸激酶 (tyrosine kinase) 抑制剂，具有有效的抗 KIT D816V 活性。Bezuclastinib 可用于非晚期系统性肥大细胞增多症 (NonAdvSM) 的研究。
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M4205
产品货号 : M28834
cas no: 2590556-80-0
M4205 是一种 c-Kit 抑制剂，对外显子 11、13、17 中的 c-Kit 突变表现出高活性。
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c-Kit-IN-3
产品货号 : M26080
cas no: 2363169-01-9
c-Kit-IN-3 是一种选择性 c-KIT 激酶抑制剂，对于 c-Kit (wt) 和 c-Kit (T670I) 的 IC50 分别为 4 nM 和 8 nM。
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CS-2660
产品货号 : M25002
cas no: 951151-97-6
CS-2660是一种高选择性、口服、耐受性良好的VEGFR2抑制剂，IC50为40 nM，抑制密切相关的酪氨酸激酶，例如Ret和Kit，IC50为180 nM和500 nM。
