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  2. Isotope-Labeled Compounds ATM/ATR
  3. Gartisertib-d8

Gartisertib-d8  (Synonyms: VX-803-d8; M4344-d8; ATR inhibitor 2-d8)

目录号: HY-136270S
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Gartisertib-d8 (VX-803-d8) 是氘代标记的 Gartisertib (HY-136270)。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。

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Gartisertib-d<sub>8</sub>

Gartisertib-d8 Chemical Structure

CAS No. : 1792214-00-6

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生物活性

Gartisertib-d8 (VX-803-d8) is the deuterium labeled Gartisertib (HY-136270). 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].

产品应用

1. 该化合物可作为示踪剂。
2. 该化合物可作为 NMR、GC-MS 或 LC-MS 分析中的内标品,用于定量分析。

体外研究
(In Vitro)

氢、碳和其他元素的稳定重同位素已被掺入药物分子中,主要用作药物开发过程中定量的示踪剂。氘化因其可能影响药物的药代动力学和代谢特征而受到关注。

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

分子量

549.60

Formula

C25H21D8F2N9O3

CAS 号
非标记 CAS
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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