1. Apoptosis
  2. MDM-2/p53

SAR405838 (Synonyms: MI-77301)

Cat. No.: HY-18986 Purity: 98.95%
Data Sheet SDS Handling Instructions

SAR405838 is a highly potent and selective MDM2 inhibitor, binds to MDM2 with Ki= 0.88 nM and has high specificity over other proteins.

For research use only. We do not sell to patients.
SAR405838 Chemical Structure

SAR405838 Chemical Structure

CAS No. : 1303607-60-4

Size Price Stock Quantity
10 mM * 1 mL in DMSO $155 In-stock
5 mg $125 In-stock
10 mg $210 In-stock
50 mg $810 In-stock
100 mg $1300 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Description

SAR405838 is a highly potent and selective MDM2 inhibitor, binds to MDM2 with Ki= 0.88 nM and has high specificity over other proteins. IC50 value: 0.88 nM (Ki) [1] Target: MDM2 in vitro: SAR405838 potently inhibits cell growth in cancer cell lines, including SJSA-1 (IC50, 0.092 μM), RS4;11 (IC50, 0.089 μM), LNCaP (IC50, 0.27 μM), and HCT-116 (IC50, 0.20 μM) cells, and displays high selectivity over cancer cell lines with mutated or deleted p53, including SAOS-2 (IC50, >10 μM), PC-3 (IC50, >10 μM), SW620 (IC50, >10 μM), and HCT-116 (p53-/-) (IC50, >20 μM) cells.[1] SAR405838 effectively induces apoptosis in the RS4;11 cell line. SAR405838 potently inhibits cell growth and induces dose-dependent apoptosis in the ABTR1 and ABTR2 sublines, albeit with modestly reduced potency compared with that in the control RS4;11 cell line.[2] in vivo: At well-tolerated dose schedules, SAR405838 achieves either 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. Remarkably, a single oral dose of SAR405838 is sufficient to achieve complete tumor regression in the SJSA-1 model. In the SJSA-1 osteosarcoma, acute lymphoblastic leukemia RS4;11, LNCaP prostate cancer, and HCT-116 colon cancer xenograft model, MI-773 (p.o.) effectively inhibits tumor growth in a dose-dependent manner (10 mg/kg, 30 mg/kg, 50 mg/kg, 100 mg/kg, and 200 mg/kg,). [1]

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT01636479 Sanofi Neoplasm Malignant July 13, 2012 Phase 1
NCT01985191 Sanofi|Merck KGaA Neoplasm Malignant November 2013 Phase 1
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References
Molecular Weight

562.5

Formula

C₂₉H₃₄Cl₂FN₃O₃

CAS No.

1303607-60-4

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Product Name:
SAR405838
Cat. No.:
HY-18986
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