LY2603618

SKU: orb1301087

特色

描述

Rabusertib (IC-83) is a selective checkpoint kinase 1 (Chk1) inhibitor investigated for its chemosensitizing potential in oncology research. It has been evaluated in preclinical and clinical studies for solid tumors, including pancreatic and non-small cell lung cancers, to enhance the efficacy of DNA-damaging chemotherapeutic agents.

研究领域

Cell Biology

图片与验证

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关键属性

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CAS 号	911222-45-2
MW	436.30
纯度	>98%
分子式	C₁₈H₂₂BrN₅O₃
SMILES	Cc1cnc(NC(=O)Nc2cc(Br)c(C)cc2OC[C@@H]2CNCCO2)cn1
靶点	Kinase
溶解性	Soluble in DMSO (up to 10 mg/ml)

生物活性

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靶点 IC50	CaMK II:1550 nM\|PDK1:893 nM\|Chk1:7 nM\|NTRK1:12000 nM\|VEGFR3:2128 nM\|RSK2:5700 nM\|JNK1:4930 nM\|MET:2200 nM\|Chk2:12000 nM
体内	In xenograft models, LY2603618 delays tumor growth when given in combination with pemetrexed.
体外	Chk1 is an ATP-dependent serine-threonine kinase and a key component in the DNA replication-monitoring checkpoint system activated by double-stranded breaks (DSBs). Chk1 contributes to all currently defined cell cycle checkpoints, including G1/S, intra-S-phase, G2/M, and the mitotic spindle checkpoint. By inhibiting the activity of chk1, Rabusertib prevents the repair of DNA caused by DNA-damaging agents, thus potentiating the antitumor efficacies of various chemotherapeutic agents. However, preClinicalal data involving Rabusertib has not been published until now. Inhibition of Chk1 is predicted to enhance the effects of antimetabolites, such as gemcitabine. Rabusertib treatment impairs DNA synthesis, increases DNA damage (via mitotic defects), induces apoptosis, and has synergistic activity with pemetrexed, especially in p53 mutant tumor cells.
细胞研究	LY2603618 is prepared in DMSO (10 mM) and stock, and then diluted 1000-fold into medium. Cells are plated at 2.5×103 per well, on 96-well tissue culture plates and incubated for one cell doubling (18-24 h). Gemcitabine dilutions are set up by half-log steps across a final concentration range of 1-1000 nM. LY2603618 is prepared by dilutions in DMSO to 5000× final concentration, and then diluted 1000-fold into medium to generate 5× stocks for addition to wells. Approximately 24 h after Gemcitabine addition, LY2603618 is added. Each combination is done in triplicate. After a period of two cell doublings following LY2603618 addition, MTS/PMS reagent is added to each well according to the manufacturer's instructions. Absorbance is read on a Spectra Max 250 spectrophotometer at 490 nm and the data analyzed with GraphPad Prism 4.0. Dose-response curves are fit by non-linear regression, with bottom fits constrained to 0 % inhibition.

储存与操作

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储存	-20°C
有效期	12 months from date of receipt.
免责声明	For research use only

别名

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Rabusertib

相似产品

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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
LY2603618 [orb1223677]
纯度：
>98% (HPLC)
CAS 号：
911222-45-2
MW:
436.303
分子式：
C₁₈H₂₂BrN₅O₃
可选规格： 2 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg, 200 mg, 500 mg, 1 g

质量保证

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化合物标识

PubChem CID

11955855 ↗

关键属性

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暂无计算属性。

实验方案信息

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纯度：	>98% (HPLC)
CAS 号：	1196541-47-5
MW:	377.286
分子式：	C₁₇H₂₁BrN₄O

LY2603618

描述

研究领域

图片与验证

关键属性

生物活性

储存与操作

别名

相似产品

GDC-0575 [orb1226825]

LY2603618 [orb1223677]

质量保证

化合物标识

关键属性

实验方案信息

可选规格