PLX647 dihydrochloride

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

PLX647 dihydrochloride 

PLX647 dihydrochloride 是一种具有口服活性的，具有高度特异性的 FMS 和 KIT 双激酶抑制剂，IC50 分别为 28 和 16 nM。PLX647 dihydrochloride (1 μM) 在 400 个激酶组中显示出对 FMS 和 KIT 有选择性，但 FLT3 和 KDR 除外 (IC50= 91 和 130 nM)。

PLX647 dihydrochloride

PLX647 dihydrochloride Chemical Structure

CAS No. : 1779796-38-1

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PLX647 dihydrochloride 的其他形式现货产品:

PLX647

生物活性

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)[1].

体外研究
(In Vitro)

In vitro, PLX647 dihydrochloride potently inhibits proliferation of BCR-FMS cells, with an IC50 of 92 nM. A corresponding Ba/F3 cell line expressing BCR-KIT is also quite sensitive to PLX647 dihydrochloride, with an IC50 of 180 nM. PLX647 dihydrochloride also inhibits endogenous FMS and KIT, as demonstrated by inhibition of the ligand-dependent cell lines M-NFS-60 (IC50=380 nM) and M-07e (IC50=230 nM), which express FMS and KIT, respectively[1].
PLX647 dihydrochloride potently inhibits the growth of FLT3-ITD-expressing MV4-11 cells (IC50=110 nM). PLX647 dihydrochloride displays minimal inhibition of the proliferation of Ba/F3 cells expressing BCR-KDR (IC50=5 μM). PLX647 dihydrochloride inhibits osteoclast differentiation with an IC50 of 0.17 μM[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

PLX647 dihydrochloride (40 mg/kg; p.o.; twice daily for 7 days) reduces macrophage accumulation in UUO kidney and blood monocytes[1].
PLX647 dihydrochloride (40 mg/kg; p.o.; male Swiss Webster mice) reduces LPS-induced TNF-α and IL-6 release[1].
PLX647 dihydrochloride (20-80 mg/kg; p.o.; daily or twice daily from 27-41 days) shows effects on collagen-induced arthritis[1].
PLX647 dihydrochloride (30 mg/kg) results in significant inhibition of TRAP5b immunostaining and bone osteolysis. PLX647 dihydrochloride (30 mg/kg BID) is able to prevent bone damage by the tumor cells[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male C57BL/6 mice (mouse unilateral ureter obstruction model)[1]
Dosage: 40 mg/kg
Administration: P.o.; twice daily for 7 days
Result: Resulted in reduction in the levels of F4/80+ macrophages by 77%.
Animal Model: 7-9 wk old Male DBA/1J mice (Mouse collagen-induced arthritis model)[1]
Dosage: 20 mg/kg, 80 mg/kg
Administration: P.o.; daily (20 mg/kg) from 27-41 days, twice daily (80 mg/kg) from 27-41 days
Result: 20 mg/kg PLX647 had no initial effect on the development of severe arthritis. However, starting on day 33, no further development of disease severity was recorded, and a 30% inhibition of the macroscopic signs of arthritis was evident in clinical score on day 41. Mice treated with 80 mg/kg BID PLX647 initially shows delayed development of severe arthritic signs. Starting on day 33, the signs of arthritis began to decrease in this treatment group, reaching a maximum reversal of 76% on day 41.

分子量

455.30

Formula

C21H19Cl2F3N4
CAS 号

1779796-38-1
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Zhang C, et al. Design and pharmacology of a highly specific dual FMS and KIT kinase inhibitor. Proc Natl Acad Sci U S A. 2013 Apr 2;110(14):5689-94.

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