Veliparib dihydrochloride

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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:

912445-05-7

包装与价格：

包装	价格(元)
10 mM * 1 mL in DMSO	电议
5mg	电议
10mg	电议
50mg	电议
100mg	电议
200mg	电议
500mg	电议
1 g	电议

产品名称

维利帕尼二盐酸盐
ABT-888 dihydrochloride

产品介绍

Veliparib dihydrochloride是有效的PARP1和PARP2抑制剂，K_i分别为5.2 nM，2.9 nM。

生物活性

Veliparib (dihydrochloride) is a potent inhibitor of PARP1 and PARP2 with K_is of 5.2 nM and 2.9 nM in cell-free assays, respectively.

IC₅₀& Target^[1]

PARP-2

2.9 nM (Ki)

PARP-1

5.2 nM (Ki)

体外研究
(In Vitro)

Veliparib is inactive to SIRT2 (>5 μM)^[1]. Veliparib inhibits the PARP activity with EC₅₀of 2 nM in C41 cells^[2]. Veliparib can decrease the PAR levels in both irradiated and nonirradiated H460 cells. Veliparib reduces clonogenic survival and inhibits DNA repair by PARP-1 inhibition in H460 cells. Veliparib increases apoptosis and autophagy in H460 cells when combination with radiation^[3]. Veliparib inhibits PARP activity in H1299, DU145 and 22RV1 cells and the inhibition is independent of p53 function. Veliparib (10 μM) suppresses the surviving fraction (SF) by 43% in the clonogenic H1299 cells. Veliparib shows effective radiosensitivity in oxic H1299 cells. Veliparib can attenuate the SF of hypoxic-irradiated cells including H1299, DU145 and 22RV1^[4].

体内研究
(In Vivo)

The oral bioavailability of Veliparib is 56%-92% in mice, SD rats, beagle dogs, and cynomolgus monkeys after oral administration^[1]. Veliparib (25 mg/kg, i.p.) can improve tumor growth delay in a NCI-H460 xenograft model. Combination with radiation, veliparib decreases the tumor vessel formation^[3]. Veliparib reduces intratumor PAR levels by more than 95% at a dose of 3 and 12.5 mg/kg in A375 and Colo829 xenograft models and the suppression can be maintained over time^[4].

Clinical Trial

分子量

317.21

性状

Solid

Formula

C₁₃H₁₈Cl₂N₄O

CAS 号

912445-05-7

中文名称

维利帕尼二盐酸盐

运输条件

Room temperature in continental US; may vary elsewhere.

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)

溶解性数据

In Vitro:

H₂O : 250 mg/mL(788.12 mM;Need ultrasonic)

DMSO : ≥ 3.2 mg/mL(10.09 mM)

*"≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	3.1525 mL	15.7624 mL	31.5249 mL
5 mM	0.6305 mL	3.1525 mL	6.3050 mL
10 mM	0.3152 mL	1.5762 mL	3.1525 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 (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 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： PBS
Solubility: 100 mg/mL (315.25 mM); Clear solution; Need ultrasonic

*以上所有助溶剂都可在本网站选购。