Voruciclib

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Voruciclib

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

1000023-04-0

包装与价格：

包装	价格(元)
1mg	电议
5mg	电议
10mg	电议
50mg	电议

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 selectiveCDKinhibitor withK_ivalues of 0.626 nM-9.1 nM. Voruciclib potently blocksCDK9, the transcriptional regulator ofMCL-1. Voruciclib represses expression ofMCL-1in multiple models of diffuse large B-cell lymphoma (DLBCL)^[1].

IC₅₀& Target^[1]

CDK9/cyc T2

0.626 nM (Ki)

CDK9/CycT1

1.68 nM (Ki)

CDK6/cycD1

2.92 nM (Ki)

CDK4/Cyc D1

3.96 nM (Ki)

CDK1/cycB

5.4 nM (Ki)

CDK1/cyc A

9.1 nM (Ki)

体外研究
(In Vitro)

Voruciclib (0.5-5 μM; 6 hours) shows targeted downregulation of MCL-1 in both ABC and GCB subtypes^[1].
K_ivalues 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^[1].

Cell Viability Assay^[1]

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^[1].

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.

Clinical Trial

分子量

469.84

性状

Solid

Formula

C₂₂H₁₉ClF₃NO₅

CAS 号

1000023-04-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。