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SAR405838

Chemical Structure : SAR405838

CAS No.: 1303607-60-4

SAR405838 (MI-77301, MI-773, SAR-405838)

Catalog No.: PC-45588Not For Human Use, Lab Use Only.

SAR405838 (MI-77301, MI-773) is a potent and highly selective small-molecule inhibitor of MDM2-p53 interaction with Ki of 0.88 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

SAR405838 (MI-77301, MI-773) is a potent and highly selective small-molecule inhibitor of MDM2-p53 interaction with Ki of 0.88 nM.
SAR405838 activates wild-type p53 in vitro and causes p53-dependent cell-cycle arrest and/or apoptosis.
SAR405838 shows durable tumor regression or complete tumor growth inhibition in mouse xenograft models of SJSA-1 osteosarcoma, RS4;11 acute leukemia, LNCaP prostate cancer, and HCT-116 colon cancer; orally bioactive.

Physicochemical Properties

M.Wt 562.503
Formula C29H34Cl2FN3O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

Spiro[3H-indole-3,3'-pyrrolidine]-5'-carboxamide, 6-chloro-4'-(3-chloro-2-fluorophenyl)-2'-(2,2-dimethylpropyl)-1,2-dihydro-N-(trans-4-hydroxycyclohexyl)-2-oxo-, (2'S,3R,4'S,5'R)-

References

1. Wang S, et al. Cancer Res. 2014 Oct 15;74(20):5855-65.

2. Bill KL, et al. Clin Cancer Res. 2016 Mar 1;22(5):1150-60.

3. Lu J, et al. Oncotarget. 2016 Dec 13;7(50):82757-82769.

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