Voruciclib|cas:1000023-04-0|西域试剂

Voruciclib,99.73%

产品编号：Bellancom-12422| CAS NO：1000023-04-0| 分子式：C₂₂H₁₉ClF₃NO₅| 分子量：469.84

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-12422		￥2800.00	杭州北京（现货）
Bellancom-12422		￥5500.00	杭州北京（现货）

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Voruciclib

产品介绍

Voruciclib 是一种具有口服活性和选择性 CDK 抑制剂，K_i 为 0.626 nM-9.1 nM。Voruciclib 可以有效阻断 MCL-1 的转录调节子 CDK9。Voruciclib 抑制多种弥漫性大 B 细胞淋巴瘤 (DLBCL) 模型中 MCL-1 的表达。

生物活性

Voruciclib is an orally active and selective CDK inhibitor with K_i values of 0.626 nM-9.1 nM. Voruciclib potently blocks CDK9, the transcriptional regulator of MCL-1. Voruciclib represses expression of MCL-1 in multiple models of diffuse large B-cell lymphoma (DLBCL).

体外研究

Voruciclib (0.5-5 µM; 6 hours) shows targeted downregulation of MCL-1 in both ABC and GCB subtypes.
K_i values for each target such as CDK9/cyc T2, CDK9/cyc T1, CDK6/cyc D1, CDK4/cyc D1, CDK1/cyc B, and CDK1/cyc A for Voruciclib hydrochloride are 0.626 nM, 1.68 nM, 2.92 nM, 3.96 nM, 5.4 nM, 9.1 nM, respectively.

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

Cell Viability Assay

Cell Line:	U2932, RIVA, OCI-LY10 cells (ABC subtype), NU-DHL-1, SU-DHL-4, SU-DHL-6 cells (GCB subtype)
Concentration:	0.5 µM, 1 µM, 2 µM, 3 µM, 4 µM, 5 µM
Incubation Time:	6 hours
Result:	Showed targeted downregulation of MCL-1 in both ABC and GCB subtypes.

体内研究
(In Vivo)

Combination of Voruciclib hydrochloride (200 mpk; Oral gavage) and Venetoclax (10 mpk, 1 mpk, 50 mpk, 25 mpk in U2932, RIVA, SU-DHL-4 and NU-DHL-1, respectively) leads to enhance tumor growth inhibition compared to either drug alone in U2932, RIVA, SU-DHL-4 (six days per week for 4 weeks), and NU-DHL-1 models (five days per week for 3 weeks) of DLBCL.

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

Animal Model:	ABC subtypes (U2932, RIVA, OCI-LY10), GCB subtypes (SU-DHL-4, NU-DHL-1) xenografted in Female NOD.CB17-Prkdcscid/NCrHsd mice
Dosage:	200 mpk
Administration:	Oral gavage; U2932, RIVA, SU-DHL-4 (six days per week for 4 weeks), OCI-LY10 (six days per week for 2 weeks), NU-DHL-1 (five days per week for 3 weeks)
Result:	Enhanced tumor growth inhibition in U2932, RIVA, SU-DHL-4 and NU-DHL-1 models except in OCI-LY10 model.

体内研究

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

Animal Model:	ABC subtypes (U2932, RIVA, OCI-LY10), GCB subtypes (SU-DHL-4, NU-DHL-1) xenografted in Female NOD.CB17-Prkdcscid/NCrHsd mice
Dosage:	200 mpk
Administration:	Oral gavage; U2932, RIVA, SU-DHL-4 (six days per week for 4 weeks), OCI-LY10 (six days per week for 2 weeks), NU-DHL-1 (five days per week for 3 weeks)
Result:	Enhanced tumor growth inhibition in U2932, RIVA, SU-DHL-4 and NU-DHL-1 models except in OCI-LY10 model.

体内研究

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

Animal Model:	ABC subtypes (U2932, RIVA, OCI-LY10), GCB subtypes (SU-DHL-4, NU-DHL-1) xenografted in Female NOD.CB17-Prkdcscid/NCrHsd mice
Dosage:	200 mpk
Administration:	Oral gavage; U2932, RIVA, SU-DHL-4 (six days per week for 4 weeks), OCI-LY10 (six days per week for 2 weeks), NU-DHL-1 (five days per week for 3 weeks)
Result:	Enhanced tumor growth inhibition in U2932, RIVA, SU-DHL-4 and NU-DHL-1 models except in OCI-LY10 model.

性状

Solid

溶解性数据

In Vitro:

DMSO : 50 mg/mL (106.42 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1284 mL	10.6419 mL	21.2838 mL
5 mM	0.4257 mL	2.1284 mL	4.2568 mL
10 mM	0.2128 mL	1.0642 mL	2.1284 mL

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。-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。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式