MI-773 (SAR405838)
SAR405838
CAS: 1303607-60-4
Molecular Formula: C29H34Cl2FN3O3
MI-773 (SAR405838) - Names and Identifiers
| Name | SAR405838 |
| Synonyms | MI 77301 SAR405838 SAR 405838 SAR-405838 MI-773 (SAR405838) SAR405838 (MI-773) SAR405838, MI-77301 MI-77301 (SAR405838) (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-oxo-spiro[3H-indole-3,3'-pyrrolidine]-5'-carboxamide |
| CAS | 1303607-60-4 |
MI-773 (SAR405838) - Physico-chemical Properties
| Molecular Formula | C29H34Cl2FN3O3 |
| Molar Mass | 562.5 |
| Density | 1.36±0.1 g/cm3(Predicted) |
| Boling Point | 732.1±60.0 °C(Predicted) |
| Solubility | 10 mM in DMSO |
| pKa | 12.03±0.70(Predicted) |
| Storage Condition | -20℃ |
| In vitro study | MI-773 can bind to MDM2 with a Ki of 0.88 nm. MI-773 effectively inhibited the proliferation of SJSA-1, RS4;11, LNCaP, and HCT-116 tumor cells, with IC50 values of 0.092 μm, 0.089 μm, 0.27 μm, and 0.20 μm, respectively. MI-773 showed high selectivity for p53 mutant or knockout tumor cell lines, including SAOS-2, PC-3, SW620 and HCT-116(p53-/-) cell lines, with IC50 values greater than 10 μm, 10 M, 10 M and 20 M. MI-773 can bind to MDM2 with a Ki of 0.88 nm. MI-773 effectively inhibited the proliferation of SJSA-1, RS4;11, LNCaP, and HCT-116 tumor cells, with IC50 values of 0.092 μm, 0.089 μm, 0.27 μm, and 0.20 μm, respectively. MI-773 showed high selectivity for tumor cell lines with p53 mutation or knockout, including SAOS-2, PC-3, SW620 and HCT-116(p53 |
| In vivo study | In SJSA 1 osteosarcoma, RS4;11 acute lymphoblastic leukemia, LNCaP prostate cancer, and HCT-116 colon cancer xenograft models, MI-773(10, 30, 50, 100, and 200mg/kg,p.o.) can effectively inhibit tumor growth, the inhibitory effect is dose dependent. In SJSA 1 osteosarcoma, RS4;11 acute lymphoblastic leukemia, LNCaP prostate cancer and HCT-116 colon cancer xenograft models, MI-773(10, 30, 50, 100 and 200mg/kg,p.o.) can effectively inhibit tumor growth, the inhibitory effect is dose dependent. |
MI-773 (SAR405838) - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.778 ml | 8.889 ml | 17.778 ml |
| 5 mM | 0.356 ml | 1.778 ml | 3.556 ml |
| 10 mM | 0.178 ml | 0.889 ml | 1.778 ml |
| 5 mM | 0.036 ml | 0.178 ml | 0.356 ml |
Last Update：2024-01-02 23:10:35
MI-773 (SAR405838) - Reference Information
| biological activity | MI-773 (SAR405838) is an oral bioeffective MDM2 antagonist with Ki of 0.88 nM. Phase 1. MI-773 (SAR405838) is an oral bioeffective MDM2 antagonist with Ki of 0.88 nM. Phase 1. |
| In vitro study | MI-773 can be combined with MDM2 with a Ki value of 0.88 nm. MI-773 can effectively inhibit SJSA-1 and RS4;11. The IC50 values of LNCaP and HCT-116 tumor cells are 0.092 μM, 0.089 μM, 0.27 μM and 0.20 μM respectively. MI-773 showed high selectivity to tumor cell lines with p53 mutation or knockout, including SAOS-2, PC-3, SW620 and HCT-116(p53-/-) cell lines, with IC50 values greater than 10 μM, 10 μM, 10 μM and 20 μM respectively. MI-773 can be combined with MDM2, and its Ki value is 0.88 nm. MI-773 can effectively inhibit SJSA-1 and RS4;11. The IC50 values of LNCaP and HCT-116 tumor cells are 0.092 μM, 0.089 μM, 0.27 μM and 0.20 μM respectively. MI-773 showed high selectivity to p53 mutation or knockout tumor cell lines, including SAOS-2, PC-3, SW620 and HCT-116(p53 |
| in vivo study | in SJSA 1 osteosarcoma, RS4; In 11 acute lymphoblastic leukemia, LNCaP prostate cancer and HCT-116 colon cancer transplanted tumor models, MI-773(10, 30, 50, 100 and 200 mg/kg,p.o.) can effectively inhibit tumor growth, and the inhibitory effect is dose-dependent. in SJSA 1 osteosarcoma, RS4;11 acute lymphoblastic leukemia, LNCaP prostate cancer and HCT-116 colon cancer transplanted tumor models, MI-773(10, 30, 50, 100 and 200 mg/kg,p.o.) can effectively inhibit tumor growth, and its inhibitory effect is dose-dependent. |
| target | TargetValue p53 MDM2 (Cell-free say) 0.88 nM(Ki) |
| Target | Value |
| p53 | |
| MDM2 (Cell-free assay) | 0.88 nM(Ki) |
Last Update：2024-04-10 22:30:50
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Product Name: SAR405838 Visit Supplier Webpage Request for quotation
CAS: 1303607-60-4
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 1303607-60-4
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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