SAR-405838

CAS No. 1303607-60-4

SAR-405838( MI-77301 | MI-773 )

Catalog No. M11218 CAS No. 1303607-60-4

SAR-405838(MI-77301, MI-773) is a potent and highly selective small-molecule inhibitor of MDM2-p53 interaction with Ki of 0.88 nM.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
2MG 75 Get Quote
5MG 122 Get Quote
10MG 203 Get Quote
25MG 397 Get Quote
50MG 584 Get Quote
100MG 833 Get Quote
500MG 1683 Get Quote
1G Get Quote Get Quote

Biological Information

  • Product Name
    SAR-405838
  • Note
    Research use only, not for human use.
  • Brief Description
    SAR-405838(MI-77301, MI-773) is a potent and highly selective small-molecule inhibitor of MDM2-p53 interaction with Ki of 0.88 nM.
  • Description
    SAR-405838(MI-77301, MI-773) is a potent and highly selective small-molecule inhibitor of MDM2-p53 interaction with Ki of 0.88 nM; activates wild-type p53 in vitro and causes p53-dependent cell-cycle arrest and/or apoptosis; 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.Blood Cancer Phase 1 Clinical.
  • In Vitro
    SAR405838 (MI-77301) 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. 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.
  • 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,).
  • Synonyms
    MI-77301 | MI-773
  • Pathway
    Apoptosis
  • Target
    MDM2-p53
  • Recptor
    Mdm2
  • Research Area
    Cancer
  • Indication
    Blood cancer

Chemical Information

  • CAS Number
    1303607-60-4
  • Formula Weight
    562.503
  • Molecular Formula
    C29H34Cl2FN3O3
  • Purity
    >98% (HPLC)
  • Solubility
    10 mM in DMSO
  • SMILES
    ClC1=CC=C2C(NC(C23[C@@H](C4=C(F)C(Cl)=CC=C4)[C@H](C(NC5CC[C@@H](O)CC5)=O)N[C@H]3CC(C)(C)C)=O)=C1
  • Chemical Name
    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)-

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

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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