Ruxolitinib phosphate

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的、选择性的、口服活性的 JAK1/JAK2 抑制剂，IC50 分别为 3.3/2.8 nM。

A potent, selective, orally active JAK1/JAK2 inhibitor with IC50 of 3.3/2.8 nM, respectively; displays modest selectivity against Tyk2 (6-fold) and marked selectivity (>130-fold) against JAK3; inhibits IL-6 signaling (IC50=281 nM), and proliferation of JAK2V617F(+) Ba/F3 cells (IC50=127 nM); suppresses erythroid progenitor colony formation from JAK2V617F(+) polycythemia vera patients (IC50=67 nM) in primary cultures; markedly reduces level of inflammatory cytokines, and preferentially eliminates neoplastic cells in a mouse model of JAK2V617F(+) MPN.Bone Cancer Approved(In Vitro):Ruxolitinib (INCB018424) potently and selectively inhibits JAK2V617F-mediated signaling and proliferation. Ruxolitinib inhibits the growth of HEL cells with EC50 of 186 nM. Ruxolitinib markedly increases apoptosis in Ba/F3-EpoR-JAK2V617F cell system, and inhibits hematopoietic progenitor cell proliferation in primary MPN patient samples.(In Vivo):Ruxolitinib (180 mg/kg, p.o.) reduces the tumor burden of mice inoculated with JAK2V617F-expressing cells without causing anemia or lymphopenia.

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INCB-018424 phosphate | Ruxolitinib

Angiogenesis

JAK

JAK1|JAK2

Cancer

Bone Cancer

1092939-17-7

404.3602

C17H21N6O4P

>98% (HPLC)

DMSO: ≥ 31 mg/mL; H2O: 5.4 mg/mL (Need ultrasonic or warming)

C1CCC(C1)[C@@H](CC#N)N2C=C(C=N2)C3=C4C=CNC4=NC=N3.OP(=O)(O)O

1H-Pyrazole-1-propanenitrile, .beta.-cyclopentyl-4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-, (.beta.R)-, phosphate (1:1)

(-20℃)

With Ice Pack

≥ 2 years