Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Uzansertib phosphate (INCB053914 phosphate) 是一种可口服的 ATP 竞争性泛-PIM 激酶抑制剂,对多种血液肿瘤细胞系具有广泛的抗增殖活性,对 PIM1、PIM2 和 PIM3 的 IC50分别为 0.24 、30 和 0.12 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 927 | 现货 | ||
5 mg | ¥ 2,990 | 现货 | ||
10 mg | ¥ 4,390 | 现货 | ||
25 mg | ¥ 6,910 | 现货 | ||
50 mg | ¥ 9,480 | 现货 | ||
100 mg | ¥ 12,800 | 现货 |
产品描述 | Uzansertib phosphate (INCB053914 phosphate) is an orally active, ATP-competitive inhibitor of pan-PIM kinase(PIM1, PIM2, PIM3 with IC50s of 0.24 nM, 30 nM, 0.12 nM , respectively). |
靶点活性 | Pim1:0.24 nM, Pim3:0.12 nM, Pim2:30 nM |
体外活性 | INCB053914, a novel, potent, and selective adenosine triphosphate-competitive pan-PIM kinase inhibitor.?In vitro, INCB053914 inhibited proliferation and the phosphorylation of downstream substrates in cell lines from multiple hematologic malignancies. |
体内活性 | Effects were confirmed in primary bone marrow blasts from patients with acute myeloid leukemia treated ex vivo and in blood samples from patients receiving INCB053914 in an ongoing phase 1 dose-escalation study.?In vivo, single-agent INCB053914 inhibited Bcl-2-associated death promoter protein phosphorylation and dose-dependently inhibited tumor growth in acute myeloid leukemia and multiple myeloma xenografts.?Additive or synergistic inhibition of tumor growth was observed when INCB053914 was combined with selective PI3Kδ inhibition, selective JAK1 or JAK1/2 inhibition, or cytarabine. |
别名 | INCB053914 phosphate |
分子量 | 611.51 |
分子式 | C26H29F3N5O7P |
CAS No. | 2088852-47-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 5 mg/mL (8.18 mM), sonification/heating is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.6353 mL | 8.1765 mL | 16.353 mL | 40.8824 mL |
5 mM | 0.3271 mL | 1.6353 mL | 3.2706 mL | 8.1765 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Uzansertib phosphate 2088852-47-3 Chromatin/Epigenetic JAK/STAT signaling Pim cell inhibit malignancies INCB 053914 INCB-053914 INCB053914 phosphate Inhibitor orally Uzansertib Phosphate INCB053914 ATP-competitive tumor Pim kinases Uzansertib hematologic lines broad INCB-053914 Phosphate activity anti-proliferative INCB 053914 Phosphate INCB053914 Phosphate inhibitor