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VER-158411
CAS No. 1174664-88-0
VER-158411( VER-00158411 | V-158411 )
Catalog No. M10594 CAS No. 1174664-88-0
A potent, selective, ATP-competitive Chk1 and Chk2 inhibitor with IC50 of 4.4 nM and 4.5 nM, respectively.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 5MG | 1053 | Get Quote |
|
| 50MG | 2142 | Get Quote |
|
| 100MG | 2790 | Get Quote |
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| 200MG | Get Quote | Get Quote |
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| 500MG | Get Quote | Get Quote |
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| 1G | Get Quote | Get Quote |
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Biological Information
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Product NameVER-158411
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NoteResearch use only, not for human use.
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Brief DescriptionA potent, selective, ATP-competitive Chk1 and Chk2 inhibitor with IC50 of 4.4 nM and 4.5 nM, respectively.
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DescriptionA potent, selective, ATP-competitive Chk1 and Chk2 inhibitor with IC50 of 4.4 nM and 4.5 nM, respectively; dispalys >1,000-fold selectivity over CDK1; reduces pChk1 (S296) and pChk2 (S516) levels in a concentration dependent fashion in cells treated with etoposide with IC50s of 48 nM for Chk1 and 904 nM for Chk2; potentiates the cytotoxicity of chemotherapeutic agents in a variety of p53 deficient human tumor cell lines (GI50=0.5-9.5 uM) and human colon tumor xenograft models.
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In VitroCellular sensing of DNA damage, along with concomitant cell cycle arrest, is mediated by a great many proteins and enzymes. One focus of pharmaceutical development has been the inhibition of DNA damage signaling, and checkpoint kinases (CHKs). There have been a number of clinical trial of checkpoint kinase inhibits alone or as a combination therapy for example, as a means to sensitize proliferating tumor cells to chemotherapies that damage DNA. The development of checkpoint kinase inhibitors the treatment of cancer was a major objective in drug discovery.
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In Vivo——
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SynonymsVER-00158411 | V-158411
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PathwayAngiogenesis
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TargetChk
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RecptorChk
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Research Area——
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Indication——
Chemical Information
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CAS Number1174664-88-0
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Formula Weight538.652
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Molecular FormulaC31H34N6O3
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Purity>98% (HPLC)
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Solubility——
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SMILESO=C(C1=CN(CC2=CC=CC=C2)N=C1)NC(C=C3C(N4)=CC5=C4C=CC(OCC(C)(C)CN(C)C)=C5)=CNC3=O
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Chemical Name1-benzyl-N-(5-(5-(3-(dimethylamino)-2,2-dimethylpropoxy)-1H-indol-2-yl)-6-oxo-1,6-dihydropyridin-3-yl)-1H-pyrazole-4-carboxamide
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
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PV-1115
A potent and highly selective Chk2 inhibitor with IC50 of 0.14 nM; displays greater than 100 uM for Chk1 in vitro.
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XL-844
A potent, specific, orally available, ATP?competitive inhibitor of Chk1 and Chk2 with Ki of 2.2 nM and 0.07 nM, respectively.
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SAR-020106
SAR-020106 is a potent, ATP-competitive, and selective CHK1 inhibitor with an IC50 of 13.3 nmol/L on the isolated human enzyme.SAR-020106 is an ATP-competitive, potent, and selective CHK1 inhibitor with an IC(50) of 13.3 nmol/L on the isolated human enzyme. This compound abrogates an etoposide-induced G(2) arrest with an IC(50) of 55 nmol/L in HT29 cells, and significantly enhances the cell killing of gemcitabine and SN38 by 3.0- to 29-fold in several colon tumor lines in vitro and in a p53-dependent fashion.
