SML2855
LY2603618
≥98% (HPLC)
别名:
(S)-1-[5-Bromo-4-methyl-2-(morpholin-2-ylmethoxy)phenyl]-3-(5-methylpyrazin-2-yl)urea, 1-[5-Bromo-4-methyl-2-(S)-(morpholin-2-ylmethoxy)phenyl]-3-(5-methylpyrazin-2-yl)urea, IC-83, LCI-1, LY 2603618, LY-2603618, Rabusertib
质量水平
方案
≥98% (HPLC)
表单
powder
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear (warmed)
储存温度
2-8°C
SMILES字符串
CC1=C(Br)C=C(NC(NC2=CN=C(C)C=N2)=O)C(OC[C@H]3OCCNC3)=C1
InChI
1S/C18H22BrN5O3/c1-11-5-16(27-10-13-8-20-3-4-26-13)15(6-14(11)19)23-18(25)24-17-9-21-12(2)7-22-17/h5-7,9,13,20H,3-4,8,10H2,1-2H3,(H2,22,23,24,25)/t13-/m0/s1
InChI key
SYYBDNPGDKKJDU-ZDUSSCGKSA-N
相关类别
生化/生理作用
LY2603618 (LCI-1) is a potent and selective checkpoint kinase 1 (Chk1) inhibitor (IC50 = 7 nM) that produces a cellular phenotype identical to that reported upon Chk1 depletion by RNAi. LY2603618 prevents doxorubicin-induced Chk1 autophosphorylation (IC50 = 52 nM; HeLa), allowing cells to traverse the G2/M checkpoint and proceed into mitosis with unresolved replicated chromosomes. LY2603618 renders mutant p53, but not wild-type, HT-29 colon cancer cells more sensitive to gemcitabine both in vitro and in mice in vivo.
Potent and selective checkpoint kinase 1 (Chk1) inhibitor that renders mutant p53 cancer cells more sensitive to DNA-damaging agents in vitro and in vivo.
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
新产品
此项目有
Darlene Barnard et al.
Investigational new drugs, 34(1), 49-60 (2015-11-28)
Pharmacological inhibition of CHK1 in the absence of p53 functionality leads to abrogation of the S and G2/M DNA damage checkpoints. We report the preclinical therapeutic activity of LY2603618 (CHK1 inhibitor) at inhibiting CHK1 activation by gemcitabine and enhancing in
Jianyun Zhao et al.
Oncotarget, 7(23), 34785-34799 (2016-05-12)
Resistance to standard chemotherapy agents remains a major obstacle for improving treatment outcomes for acute myeloid leukemia (AML). The Bcl-2-selective inhibitor ABT-199 has demonstrated encouraging preclinical results, drug resistance remains a concern. Mcl-1 has been demonstrated to contribute to ABT-199
Constance King et al.
Investigational new drugs, 32(2), 213-226 (2013-10-12)
Interference with DNA damage checkpoints has been demonstrated preclinically to be a highly effective means of increasing the cytotoxicity of a number of DNA-damaging cancer therapies. Cell cycle arrest at these checkpoints protects injured cells from apoptotic cell death until
Yvonne de Jong et al.
Journal of bone oncology, 19, 100268-100268 (2019-12-14)
Chondrosarcomas are malignant cartilage tumors that are relatively resistant towards conventional therapeutic approaches. Kinase inhibitors have been investigated and shown successful for several different cancer types. In this study we aimed at identifying kinase inhibitors that inhibit the survival of
Characterization and preclinical development of LCI-1, a selective and potent Chk1 inhibitor in phase I clinical trials
Marshall M, Barda D, Barnard D, et al.
Molecular Cancer Therapeutics, 8, B248-B248 (2009)
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