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CAS No. : 2088852-47-3

MCE 國(guó)際站：Uzansertib phosphate

產(chǎn)品活性：Uzansertib (INCB053914) phosphate 是一種具有口服活性的，ATP 競(jìng)爭(zhēng)性泛-PIM 激酶抑制劑，對(duì)于 PIM1，PIM2 和 PIM3 的 IC₅₀ 分別為 0.24 nM，30 nM 和 0.12 nM。Uzansertib phosphate 對(duì)多種血液腫瘤細(xì)胞系具有廣泛的抗增殖活性。

研究領(lǐng)域：JAK/STAT Signaling

作用靶點(diǎn)：Pim

In Vitro: Uzansertib phosphate inhibits proliferation in all multiple myeloma (MM) cell lines tested, with mean GI₅₀ values ranging from 13.2 nM to 230.0 nM in AML, MM, DLBCL, MCL, and T-ALL cell lines.
Uzansertib phosphate (0.1, 0.3, 1, 3, 10, 30, 100, 300, 1000 nM) inhibits the phosphorylation of downstream PIM kinase substrates (p70S6K/S6 and 4E-BP1) in a dose-dependent manner in MOLM-16 (AML), Pfeiffer (DLBCL), and KMS-12-PE/BM (MM) cell lines.
PIM kinase-mediated phosphorylation of BAD in MOLM-16 and KMS-12-BM cells is particularly sensitive to inhibition by Uzansertib phosphate (mean IC₅₀, 4 nM and 27 nM, respectively).

In Vivo: Uzansertib phosphate (25-100 mg/kg; PO; twice a day; for 15 days) inhibits tumor growth in a dose-dependent manner in mice bearing MOLM-16 (AML) or KMS-12-BM (MM) .
Uzansertib phosphate demonstrates a dose-dependent inhibition of BAD phosphorylation relative to vehicle at 4 hours post dose (MOLM-16 tumors, IC₅₀=70 nM; KMS-12-BM tumors, IC₅₀=145 nM) .

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