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product name MI-773 (SAR405838)


Description: MI-773 (SAR405838) is a specific antagonist of MDM2 with Ki value of 0.88 nM. Murine double minute 2 (MDM2) is a primary negative regulator of wild-type p53, which is a tumor suppressor. MDM2 is an E3 ubiquitin ligase that induces p53 degradation and blocks the p53 trans-activation domain (TAD). MI-773 (SAR405838) is a MDM2 antagonist. MI-773 (SAR405838) inhibited cells growth in SJSA-1, RS4;11, LNCaP and HCT-116 cancer cell lines with IC50 values of 0.092, 0.089, 0.27 and 0.20 μM, respectively.

Reference: Cancer Res. 2014 Oct 15;74(20):5855-65.



Molecular Weight (MW)

562.50
Formula

C29H34Cl2FN3O3
CAS No.

1303607-60-4
Storage

-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)

DMSO: 100 mg/mL (177.77 mM)
Water: <1 mg/mL (slightly soluble or insoluble)
Ethanol: 31 mg/mL warming (55.11 mM)
Solubility (In vivo)

 
Chemical Name

(2S,3R,4S,5R)-6-chloro-4-(3-chloro-2-fluorophenyl)-N-((1r,4R)-4-hydroxycyclohexyl)-2-neopentyl-2-oxospiro[indoline-3,3-pyrrolidine]-5-carboxamide

other peoduct :

In Vitro MI-773 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
In Vivo 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).
Animal model SCID mice with SJSA-1 osteosarcoma (females), acute lymphoblastic leukemia RS4;11 (females), LNCaP prostate cancer (males), or HCT-116 colon cancer (females) xenograft model
Formulation & Dosages 10% PEG400: 3% Cremophor: 87% PBS, or 2% TPGS: 98% PEG200; 200 mg/kg; Oral
References [1] Wang S, et al. Cancer Res. 2014, 74(20), 5855-5865.

PND-1188