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抑制剂/激活剂

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凋亡与自噬

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Rabusertib LY2603618; IC-83

Rabusertib (LY2603618) 是一种有效的选择性的 Chk1 抑制剂，IC50 为 7 nM。

货号：
TK0275
规格：

1mg

5mg

10mg

25mg
价格：
￥0.00

产品参数

CAS No.	911222-45-2
生物活性	Rabusertib (LY2603618) is a potent and selective inhibitor of Chk1 with an IC50 of 7 nM.
分子式	C18H22BrN5O3
分子量	436.3
运输条件	Room temperature in continental US; may vary elsewhere.
储存条件	Powder -20°C 3 years
溶解性数据	DMSO : 50 mg/mL (114.60 mM; Need ultrasonic)
体内研究	Mice bearing Calu-6 xenografts are treated with 150 mg/kg (IP) Gemcitabine and a single simultaneous 200 mg/kg oral dose of Rabusertib (LY2603618). 200 mg/kg of Rabusertib (LY2603618) is sufficient to inhibit 85 % of Chk1 autophosphorylation in vivo at 2 h. Rabusertib (LY2603618) effectively reduces Gemcitabine-induced phosphorylation on Tlk serine 695 as well, supporting the cited report with a selective chemical inhibitor of Chk1.
体外研究	Rabusertib (LY2603618) is a highly effective inhibitor of multiple aspects of Chk1 biology. Rabusertib (LY2603618) is tested against a panel of 51 diverse protein kinases in vitro. With an IC50 of 7 nM for Chk1, Rabusertib (LY2603618) is approximately 100-fold more potent against Chk1 than against any of the other protein kinases evaluated (PDK1, IC50=893 nM, others >1000 nM). Rabusertib (LY2603618) effectively reduced Chk1 autophosphorylation with an EC50 of 430 nM. Inhibition of Chk1 by Rabusertib (LY2603618) also effectively abrogated the G2/M DNA damage checkpoint in cells treated with DNA damaging agents. Treatment of cells with Rabusertib (LY2603618) produced a cellular phenotype similar to that reported for depletion of Chk1 by RNAi. Inhibition of intracellular Chk1 by Rabusertib (LY2603618) results in impaired DNA synthesis, elevated H2A.X phosphorylation indicative of DNA damage and premature entry into mitosis. Treatments of the SK-N-BE(2) cells with variable concentrations of Rabusertib (LY2603618) results in dose-dependent inhibition of cell growth determined by MTT assays with an IC50 of 10.81 µM.
文献	•Sci Transl Med. 2021 Jan 20;13(577):eaba7401. •Sci Transl Med. 2018 Jul 18;10(450). pii: eaaq1093. •Nucleic Acids Res. 2021 Apr 6;49(6):3322-3337. •Cell Syst. 2020 Jan 22;10(1):66-81.e11. •Cell Syst. 2020 Jan 22;10(1):66-81.e11. •Cell Prolif. 2020 Oct;53(10):e12895. •Cancer Biol Ther. 2022 Jan 9;1-14. •Harvard Medical School LINCS LIBRARY
纯度及产品资料	98%

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