Uzansertib phosphate INCB053914 phosphate|cas:2088852-47-3|西域试剂

Uzansertib phosphate INCB053914 phosphate,99.39%

产品编号：Bellancom-101870B| CAS NO：2088852-47-3| 分子式：C₂₆H₂₉F₃N₅O₇P| 分子量：611.51

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货号	价格	库存与货期
Bellancom-101870B	￥1200.00	杭州北京（现货）
Bellancom-101870B	￥3600.00	杭州北京（现货）
Bellancom-101870B	￥5400.00	杭州北京（现货）
Bellancom-101870B	￥9800.00	杭州北京（现货）
Bellancom-101870B	￥15000.00	杭州北京（现货）

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Uzansertib phosphate INCB053914 phosphate

产品介绍

Uzansertib (INCB053914) phosphate 是一种具有口服活性的，ATP 竞争性泛-PIM 激酶抑制剂，对于 PIM1，PIM2 和 PIM3 的 IC₅₀ 分别为 0.24 nM，30 nM 和 0.12 nM。Uzansertib phosphate 对多种血液肿瘤细胞系具有广泛的抗增殖活性。

生物活性

Uzansertib (INCB053914) phosphate 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 phosphate has broad anti-proliferative activity against a variety of hematologic tumor cell lines.

体外研究

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).

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

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) .

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female immune compromised (severe combined immunodeficiency [SCID]) mice (5-9 weeks of age) bearing MOLM-16 (AML) or KMS-12-BM (MM)
Dosage:	25, 50, 75, 100 mg/kg
Administration:	PO; twice a day; for 15 days
Result:	Inhibited tumor growth in a dose-dependent manner in mice.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female immune compromised (severe combined immunodeficiency [SCID]) mice (5-9 weeks of age) bearing MOLM-16 (AML) or KMS-12-BM (MM)
Dosage:	25, 50, 75, 100 mg/kg
Administration:	PO; twice a day; for 15 days
Result:	Inhibited tumor growth in a dose-dependent manner in mice.

性状

Solid

溶解性数据

In Vitro:

DMSO : 5 mg/mL (8.18 mM; Need ultrasonic and warming)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.6353 mL	8.1765 mL	16.3530 mL
5 mM	0.3271 mL	1.6353 mL	3.2706 mL
10 mM	---	---	---

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 1.8 mg/mL (2.94 mM); Clear solution

此方案可获得 ≥ 1.8 mg/mL (2.94 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 18.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 1.8 mg/mL (2.94 mM); Clear solution

此方案可获得 ≥ 1.8 mg/mL (2.94 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 18.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 1.8 mg/mL (2.94 mM); Clear solution

此方案可获得 ≥ 1.8 mg/mL (2.94 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 18.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。