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
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关于此项目
经验公式（希尔记法）:
C18H22BrN5O3
化学文摘社编号:
分子量:
436.30
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
产品名称
LY2603618, ≥98% (HPLC)
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
SMILES string
CC1=C(Br)C=C(NC(NC2=CN=C(C)C=N2)=O)C(OC[C@H]3OCCNC3)=C1
InChI key
SYYBDNPGDKKJDU-ZDUSSCGKSA-N
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear (warmed)
storage temp.
2-8°C
Quality Level
Biochem/physiol Actions
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.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
新产品
此项目有
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)
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
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
Anne M van Harten et al.
Oncogenesis, 8(7), 38-38 (2019-06-19)
Head and neck squamous cell carcinomas (HNSCCs) coincide with poor survival rates. The lack of driver oncogenes complicates the development of targeted treatments for HNSCC. Here, we follow-up on two previous genome-wide RNA and microRNA interference screens in HNSCC to
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