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Umbralisib hydrochloride (Synonyms: TGR-1202 hydrochloride; RP5264 hydrochloride) 纯度: 98.98%
Umbralisib hydrochloride (TGR-1202 hydrochloride) 是一种新颖的 PI3Kδ 抑制剂,IC50 和 EC50 值分别为 22.2 nM 和 24.3 nM;Umbralisib hydrochloride (TGR-1202 hydrochloride) 同时可抑制 CK1ε,EC50 值为 6.0 μM。
Umbralisib hydrochloride Chemical Structure
CAS No. : 1532533-78-0
规格 | 价格 | 是否有货 | 数量 |
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10 mM * 1 mL in DMSO | ¥1471 | In-stock | |
5 mg | ¥1100 | In-stock | |
10 mg | ¥1900 | In-stock | |
25 mg | ¥4400 | In-stock | |
50 mg | ¥5800 | In-stock | |
100 mg | ¥9900 | In-stock | |
200 mg | 询价 | ||
500 mg | 询价 |
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Umbralisib hydrochloride 相关产品
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生物活性 |
Umbralisib hydrochloride (TGR-1202 hydrochloride) is a novel PI3Kδ inhibitor, with IC50 and EC50 of 22.2 nM and 24.3 nM, respectively; Umbralisib hydrochloride (TGR-1202 hydrochloride) is also active against CK1ε, with an EC50 value of 6.0 μM. |
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IC50 & Target |
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体外研究 (In Vitro) |
Umbralisib (RP5264) causes a half-maximal inhibition of human whole blood CD19 cell proliferation between 100-300 nM[1]. In human lymphoma and leukemia cell lines, Umbralisib (TGR-1202; 10 nM-100 μM) inhibits phosphorylated AKT at Ser473 in a concentration-dependent manner. Umbralisib and carfilzomib synergistically kill blood cancer cells through disrupting the 4E-BP1-eIF4F-c-Myc axis. Umbralisib and carfilzomib in combination synergistically and selectively silence the c-Myc and E2F transcription programs. Umbralisib (15-50 μM) potently represses the expression of c-Myc in the DLBCL cell line LY7, and is uniquely characterized with structural features suitable for targeting CK1ε in lymphoma cells[2]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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体内研究 (In Vivo) |
In a subcutaneous xenograft model of T-cell acute lymphoblastic leukemia (T-ALL) in NOD/SCID mice using the MOLT-4 cell line, Umbralisib (TGR-1202; 150 mg/kg, daily p.o.) significantly shrinks the tumors by day 25[2]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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Clinical Trial |
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分子量 |
608.01 |
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Formula |
C31H25ClF3N5O3 |
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CAS 号 |
1532533-78-0 |
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运输条件 |
Room temperature in continental US; may vary elsewhere. |
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储存方式 |
4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
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溶解性数据 |
In Vitro:
DMSO : ≥ 150 mg/mL (246.71 mM) H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble) * “≥” means soluble, but saturation unknown. 配制储备液
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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。 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
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参考文献 |
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