SML2772
SAR405838
≥98% (HPLC)
别名:
(2′S,3R,4′S,5′R)-6-Chloro-4′-(3-chloro-2-fluorophenyl)-2′-(2,2-dimethylpropyl)-1,2-dihydro-N-(trans-4-hydroxycyclohexyl)-2-oxospiro[3H-indole-3,3′-pyrrolidine]-5′-carboxamide, MI 77301, MI-77301, MI77301
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关于此项目
经验公式（希尔记法）:
C29H34Cl2FN3O3
化学文摘社编号:
分子量:
562.50
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
Assay:
≥98% (HPLC)
Storage condition:
desiccated
Quality Segment
assay
≥98% (HPLC)
storage condition
desiccated
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
−20°C
SMILES string
O=C([C@@H]1N[C@@H](CC(C)(C)C)[C@@]2(C(NC3=C2C=CC(Cl)=C3)=O)[C@H]1C4=CC=CC(Cl)=C4F)N[C@@H]5CC[C@H](CC5)O
InChI
1S/C29H34Cl2FN3O3/c1-28(2,3)14-22-29(19-12-7-15(30)13-21(19)34-27(29)38)23(18-5-4-6-20(31)24(18)32)25(35-22)26(37)33-16-8-10-17(36)11-9-16/h4-7,12-13,16-17,22-23,25,35-36H,8-11,14H2,1-3H3,(H,33,37)(H,34,38)/t16-,17-,22-,23-,25+,29+/m0/s1
InChI key
IDKAKZRYYDCJDU-HBMMIIHUSA-N
Biochem/physiol Actions
Orally available, highly potent and selective Mdm2 (Hdm2) inhibitor that blocks cancer growth in a wild-type p53-dependent manner both in vitro and in vivo.
SAR405838 (MI-77301) is an orally available (F = 67%/mouse, 48%/rat; 10 mg/kg p.o.), highly potent and selective Mdm2 (Hdm2) inhibitor (human Mdm2 Ki = 0.88 nM; no binding at 10 μM to Bcl-2, Bcl-xL, Mcl-1, Mdmx; no inhibition against >200 receptors/enzymes) that upregulates wild-type p53 activity (EC50 = 300-600 nM; SJSA-1) by blocking Mdm2-p53 interaction and Mdm2-mediated p53 degradation with 5-10-times higher potency than MI-219 and nutlin-3a. SAR405838 inhibits cancer growth in a wild-type p53-dependent manner both in cultures (IC50 = 89 nM/RS4;11, 92 nM/SJSA-1, 200 nM/HCT-116, 270 nM/LANCaP) and in xenograft models in vivo (50-200 mg/kg single or daily p.o. dosing).
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable