LY2603618

SKU: orb1223677

描述

A potent and selective small molecule inhibitor of Chk1 (IC50= 7 nM); promotes impaired DNA synthesis and elevates H2A.X phosphorylation indicative of DNA damage and premature entry into mitosis.Pancreatic Cancer Phase 2 Discontinued(In Vitro):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.

图片与验证

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关键属性

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CAS 号	911222-45-2
MW	436.303
纯度	>98% (HPLC)
分子式	C₁₈H₂₂BrN₅O₃
SMILES	CC1=CC(=C(C=C1Br)NC(=O)NC2=NC=C(N=C2)C)OC[C@@H]3CNCCO3
靶点	Chk
溶解性	DMSO: 29.5 mg/mL

生物活性

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体内

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

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.

储存与操作

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储存	Storage temperature: -20°C. Stability: ≥ 2 years
有效期	12 months from date of receipt.
免责声明	For research use only

别名

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IC-83 | LY 2603618 | LY-2603618 | Rabusertib

相似产品

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LY2603618 [orb1301087]
纯度：
>98%
CAS 号：
911222-45-2
MW:
436.30
分子式：
C₁₈H₂₂BrN₅O₃
可选规格： 25 mg, 5 mg
GDC-0575 [orb1226825]
纯度：
>98% (HPLC)
CAS 号：
1196541-47-5
MW:
377.286
分子式：
C₁₇H₂₁BrN₄O
可选规格： 10 mg, 25 mg, 5 mg, 50 mg, 100 mg, 200 mg, 500 mg, 1 g

质量保证

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常用数据库链接

基因符号

Chk

实验方案信息

查看更多实验方案

纯度：	>98%
CAS 号：	911222-45-2
MW:	436.30
分子式：	C₁₈H₂₂BrN₅O₃