GDC0575 monohydrochloride

TargetMol
Product Code: TAR-T27407
Supplier: TargetMol
CodeSizePrice
TAR-T27407-1mg1mg£121.00
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TAR-T27407-2mg2mg£142.00
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TAR-T27407-5mg5mg£173.00
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TAR-T27407-1mL1 mL * 10 mM (in DMSO)£193.00
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TAR-T27407-10mg10mg£217.00
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TAR-T27407-25mg25mg£335.00
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TAR-T27407-50mg50mg£450.00
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TAR-T27407-100mg100mg£613.00
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Prices exclude any Taxes / VAT

Overview

Regulatory Status: RUO
Shipping:
cool pack
Storage:
-20℃

Images

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Further Information

Bioactivity:
GDC-0575 is a potent and selective inhibitor of cell cycle checkpoint kinase 1 (Chk1) with an IC50 of 1.2?nM. GDC-0575 specifically binds to and inhibits Chk1; this may result in tumor cells bypassing Chk1-dependent cell cycle arrest in the S and G2/M phases, which permits the cells to undergo DNA repair prior to entry into mitosis.
CAS:
1196504-54-7
Formula:
C16H21BrClN5O
Molecular Weight:
414.73
Pathway:
Cell Cycle/Checkpoint
Purity:
0.9785
SMILES:
Cl.N[C@@H]1CCCN(C1)c1c(Br)cnc2[nH]cc(NC(=O)C3CC3)c12
Target:
Chk

References

1. Grellety T, et al. Enhancing Abiraterone Acetate Efficacy in Androgen Receptor-positive Triple-negative Breast Cancer: Chk1 as a Potential Target. Clin Cancer Res. 2019 Jan 15;25(2):856-867. 2. Italiano A, et al. Phase I study of the checkpoint kinase 1 inhibitor GDC-0575 in combination with gemcitabine in patients with refractory solid tumors. Ann Oncol. 2018 May 1;29(5):1304-1311. 3. Oo ZY, Stevenson AJ, Proctor M, Daignault SM, Walpole S, Lanagan C, Chen J, ?kalamera D, Spoerri L, Ainger SA, Sturm RA, Haass NK, Gabrielli B. Endogenous Replication Stress Marks Melanomas Sensitive to CHEK1 Inhibitors In Vivo. Clin Cancer Res. 2018 Jun 15;24(12):2901-2912. doi: 10.1158/1078-0432.CCR-17-2701. Epub 2018 Mar 13. PubMed PMID: 29535131. 4. Laroche-Clary A, Lucchesi C, Rey C, Verbeke S, Bourdon A, Chaire V, Alg?o MP, Cousin S, Toulmonde M, V?lasco V, Shutzman J, Savina A, Le Loarer F, Italiano A. CHK1 inhibition in soft-tissue sarcomas: biological and clinical implications. Ann Oncol. 2018 Apr 1;29(4):1023-1029. doi: 10.1093/annonc/mdy039. PubMed PMID: 29409053.