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PLX647
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
PLX647图片
CAS NO:873786-09-5
包装与价格：
包装价格(元)
10mM (in 1mL DMSO)电议
10mg电议
50mg电议

产品介绍
PLX647 是一种具有口服活性、高度特异性的双重 FMS 和 KIT 激酶抑制剂，IC50 分别为 28 和 16 nM。 PLX647 对 FMS 和 KIT 的选择性超过 400 种激酶，浓度为 1 μM，FLT3 和 KDR 除外（IC50s 分别为 91 和 130 nM）。
Cas No.873786-09-5
化学名(E)-N-(5-((1H-pyrrolo[2,3-b]pyridin-3-yl)methyl)pyridin-2(1H)-ylidene)-1-(4-(trifluoromethyl)phenyl)methanamine
Canonical SMILESFC(F)(F)C1=CC=C(C/N=C2C=CC(CC3=CNC4=C3C=CC=N4)=CN\2)C=C1
分子式C21H17F3N4
分子量382.38
溶解度≥ 19.1mg/mL in DMSO
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

PLX647 is a potent and specific dual inhibitor of FMS and KIT kinases with IC50 values of 28 and 16 nM, respectively [1].

McDonough feline sarcoma viral (v-fms) oncogene homolog (FMS, also known as CSF1R) is a member of the platelet-derived growth factor receptor (PDGFR) family. Macrophage colony-stimulating factor (M-CSF or CSF-1) and interleukin 34 are two known FMS ligands. FMS plays important roles in regulating the survival, proliferation, and differentiation of monocyte/macrophage lineages. The stem cell factor (SCF) receptor v-kit Hardy-Zuckerman 4 feline sarcoma viral oncogene homolog (KIT) is also a member of the PDGFR family. Mutational activation of KIT occurs in many cancers [1].

PLX647 is a potent and specific dual inhibitor of FMS and KIT kinases. PLX647 showed aqueous solubility of 14 μM. PLX647 bound to the autoinhibited state of the KIT kinase with the juxtamembrane domain and prevented the activation loop from adopting the DFG-in conformation. In Ba/F3 cells expressing breakpoint cluster region activated kinase (BCR)-FMS and BCR-KIT, PLX647 inhibited cell proliferation with IC50 values of 0.092 and 0.18 μM. Also, PLX647 inhibited osteoclast differentiation with IC50 value of 0.17 μM [1].

In mice, PLX647 (40 mg/kg) significantly reduced LPS-induced TNF-α and IL-6 release by 85% and 75%, respectively. In an acute renal inflammation mouse model, PLX647 (40 mg/kg twice daily) reduced the levels of F4/80+ macrophages by 77% [1].

Reference:
[1].  Zhang C, Ibrahim PN, Zhang J, et al. Design and pharmacology of a highly specific dual FMS and KIT kinase inhibitor. Proc Natl Acad Sci U S A, 2013, 110(14): 5689-5694.