1623432-51-8
1623432-51-8 structure
- Name: AM-7209
- Chemical Name: 4-({[(3r,5r,6s)-1-[(1s)-2-(Tert-Butylsulfonyl)-1-Cyclopropylethyl]-6-(4-Chloro-3-Fluorophenyl)-5-(3-Chlorophenyl)-3-Methyl-2-Oxopiperidin-3-Yl]acetyl}amino)-2-Methoxybenzoic Acid
- CAS Number: 1623432-51-8
- Molecular Formula: C37H41Cl2FN2O7S
- Molecular Weight: 747.700
- Catalog: Signaling Pathways Apoptosis MDM-2/p53
- Create Date: 2020-01-20 18:10:55
- Modify Date: 2023-02-01 17:55:04
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A potent and selective inhibitor of the MDM2-p53 interaction with Kd of 38 pM, and IC50 of 1.6 nM; potently inhibits cell growth on-target in the tumor cell line with wild-type p53 cell with IC50 of 2 nM, exhibits >12,500-fold selectivity over those with p53-deficient cells; demonstrates remarkable pharmacokinetic properties and in vivo antitumor activity in both the SJSA-1 osteosarcoma xenograft model (ED50=2.6 mg/kg QD) and the HCT-116 colorectal carcinoma xenograft model (ED50=10 mg/kg QD).
| Name | 4-({[(3r,5r,6s)-1-[(1s)-2-(Tert-Butylsulfonyl)-1-Cyclopropylethyl]-6-(4-Chloro-3-Fluorophenyl)-5-(3-Chlorophenyl)-3-Methyl-2-Oxopiperidin-3-Yl]acetyl}amino)-2-Methoxybenzoic Acid |
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| Synonyms |
Benzoic acid, 4-[[2-[(3R,5R,6S)-6-(4-chloro-3-fluorophenyl)-5-(3-chlorophenyl)-1-[(1S)-1-cyclopropyl-2-[(1,1-dimethylethyl)sulfonyl]ethyl]-3-methyl-2-oxo-3-piperidinyl]acetyl]amino]-2-methoxy-
4-({[(3r,5r,6s)-1-[(1s)-2-(Tert-Butylsulfonyl)-1-Cyclopropylethyl]-6-(4-Chloro-3-Fluorophenyl)-5-(3-Chlorophenyl)-3-Methyl-2-Oxopiperidin-3-Yl]acetyl}amino)-2-Methoxybenzoic Acid 4-({[(3R,5R,6S)-6-(4-Chloro-3-fluorophenyl)-5-(3-chlorophenyl)-1-{(1S)-1-cyclopropyl-2-[(2-methyl-2-propanyl)sulfonyl]ethyl}-3-methyl-2-oxo-3-piperidinyl]acetyl}amino)-2-methoxybenzoic acid |
| Description | A potent and selective inhibitor of the MDM2-p53 interaction with Kd of 38 pM, and IC50 of 1.6 nM; potently inhibits cell growth on-target in the tumor cell line with wild-type p53 cell with IC50 of 2 nM, exhibits >12,500-fold selectivity over those with p53-deficient cells; demonstrates remarkable pharmacokinetic properties and in vivo antitumor activity in both the SJSA-1 osteosarcoma xenograft model (ED50=2.6 mg/kg QD) and the HCT-116 colorectal carcinoma xenograft model (ED50=10 mg/kg QD). |
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| References | References 1. Rew Y, et al. J Med Chem. 2014 Dec 26;57(24):10499-511. View Related Products by Target MDM2-p53 |
| Density | 1.4±0.1 g/cm3 |
|---|---|
| Boiling Point | 896.2±65.0 °C at 760 mmHg |
| Molecular Formula | C37H41Cl2FN2O7S |
| Molecular Weight | 747.700 |
| Flash Point | 495.8±34.3 °C |
| Exact Mass | 746.199585 |
| LogP | 7.50 |
| Vapour Pressure | 0.0±0.3 mmHg at 25°C |
| Index of Refraction | 1.603 |