Gartisertib(Synonyms: VX-803; M4344; ATR inhibitor 2)

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Gartisertib (Synonyms: VX-803; M4344; ATR inhibitor 2) 纯度: 99.88%

Gartisertib (VX-803) 是一种 ATP 竞争性的,具有口服活性的,选择性的 ATR 抑制剂,Ki<150 pm。gartisertib 抑制 atr 驱动的磷酸化检查点激酶-1 (chk1) 磷酸化, ic50值为 8 nM。具有抗肿瘤活性。

Gartisertib(Synonyms: VX-803;  M4344;  ATR inhibitor 2)

Gartisertib Chemical Structure

CAS No. : 1613191-99-3

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥5000 In-stock
5 mg ¥4200 In-stock
10 mg ¥7000 In-stock
50 mg ¥20000 In-stock
100 mg ¥30000 In-stock
200 mg   询价  
500 mg   询价  

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生物活性

Gartisertib (VX-803) is an ATP-competitive, orally active, and selective ATR inhibitor, with a Ki of <150 pm. gartisertib potently inhibits atr-driven phosphorylated checkpoint kinase-1 (chk1) phosphorylation with an ic50 of 8 nM. Antitumor activity[1][2].

IC50 & Target[1]

ATR

<150 pM (Ki)

体内研究
(In Vivo)

In monotherapy efficacy studies Gartisertib shows tumor stasis to regression in tumor models with alternative lengthening of telomeres (ALT). In combination with PARP inhibitors, tumor regression could be observed in triple-negative breast cancer xenograft models[1].

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.

分子量

541.55

Formula

C25H29F2N9O3

CAS 号

1613191-99-3

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 : 25 mg/mL (46.16 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.8466 mL 9.2328 mL 18.4655 mL
5 mM 0.3693 mL 1.8466 mL 3.6931 mL
10 mM 0.1847 mL 0.9233 mL 1.8466 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。

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    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (3.84 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.84 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 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
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: 2.08 mg/mL (3.84 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.08 mg/mL (3.84 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Frank T. Zenke, et al. Abstract 369: Antitumor activity of M4344, a potent and selective ATR inhibitor, in monotherapy and combination therapy. Experimental and Molecular Therapeutics.

    [2]. Gorecki L, et al. Discovery of ATR kinase inhibitor berzosertib (VX-970, M6620): Clinical candidate for cancer therapy. Pharmacol Ther. 2020 Feb 26:107518.

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