货号	规格	价格	上海	北京	珠海	重庆	武汉
V45371-1mg	≥98%	￥1090.00 V45371-1mg ￥1090.00 3-5天	0 货期：3-5天	-	-	-	-
V45371-5mg	≥98%	￥2790.00 V45371-5mg ￥2790.00 3-5天	0 货期：3-5天	-	-	-	-
V45371-10mg	≥98%	￥4190.00 V45371-10mg ￥4190.00 3-5天	0 货期：3-5天	-	-	-	-
V45371-25mg	≥98%	￥7530.00 V45371-25mg ￥7530.00 3-5天	0 货期：3-5天	-	-	-	-

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产品描述：

Uzansertib (INCB053914) is an orally active, ATP-competitive pan-PIM kinase inhibitor with IC50s of 0.24 nM, 30 nM, 0.12 nM for PIM1, PIM2, PIM3, respectively. Uzansertib has broad anti-proliferative activity against a variety of hematologic tumor cell lines.

靶点：

PIM1:0.24 nM (IC50); PIM2:30 nM (IC50); PIM3:0.12 nM (IC50)

体外研究：

Uzansertib 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 (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 (mean IC50, 4 nM and 27 nM, respectively).

体内研究：

Uzansertib (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 demonstrates a dose-dependent inhibition of BAD phosphorylation relative to vehicle a웿Ůñ샮㡽䇘睜⪰ޏࠃ

保存条件：

-20°C

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.947 ml	9.737 ml	19.474 ml
5 mM	0.389 ml	1.947 ml	3.895 ml
10 mM	0.195 ml	0.974 ml	1.947 ml
50 mM	0.039 ml	0.195 ml	0.389 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

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