
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)






Size | Price / USD | Stock | Quantity |
2MG | 75 | Get Quote |
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5MG | 122 | Get Quote |
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10MG | 203 | Get Quote |
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25MG | 397 | Get Quote |
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50MG | 584 | Get Quote |
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100MG | 833 | Get Quote |
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500MG | 1683 | Get Quote |
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1G | Get Quote | Get Quote |
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Biological Information
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Product NameSAR-405838
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NoteResearch use only, not for human use.
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Brief DescriptionSAR-405838(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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DescriptionSAR-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.
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In VitroSAR405838 (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.
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In VivoAt 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,).
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SynonymsMI-77301 | MI-773
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PathwayApoptosis
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TargetMDM2-p53
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RecptorMdm2
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Research AreaCancer
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IndicationBlood cancer
Chemical Information
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CAS Number1303607-60-4
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Formula Weight562.503
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Molecular FormulaC29H34Cl2FN3O3
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Purity>98% (HPLC)
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Solubility10 mM in DMSO
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SMILESClC1=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
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Chemical NameSpiro[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
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Storage(-20℃)
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ShippingWith Ice Pack
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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.
molnova catalog



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