MI-773 (SAR405838) (Synonyms: SAR405838) |
| カタログ番号GC11547 |
MI-773 (SAR405838) (MI-77301) は、MI-773 の類似体であり、非常に強力で選択的な MDM2-p53 相互作用阻害剤です。 MI-773 (SAR405838) は、0.88 nM の Ki で MDM2 に結合します。 MI-773 (SAR405838) はアポトーシスを誘導し、強力な抗腫瘍活性を持っています。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1303607-60-4
Sample solution is provided at 25 µL, 10mM.
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MI-773 (SAR405838) is a specific antagonist of MDM2 with Ki value of 0.88 nM [1].
Murine double minute 2 (MDM2) is a primary negative regulator of wild-type p53, which is a tumor suppressor. MDM2 is an E3 ubiquitin ligase that induces p53 degradation and blocks the p53 trans-activation domain (TAD) [1].
MI-773 (SAR405838) is a MDM2 antagonist. MI-773 (SAR405838) inhibited cells growth in SJSA-1, RS4;11, LNCaP and HCT-116 cancer cell lines with IC50 values of 0.092, 0.089, 0.27 and 0.20 μM, respectively. MI-773 (SAR405838) exhibited high selectivity over cancer cell lines with mutated or deleted p53 with IC50 values of >20, >10, >10 and >10 μM for HCT-116 (p53-/-), SAOS-2, PC-3 and SW620 cancer cell lines, respectively [1].
In mice bearing the SJSA-1, HCT-116, RS4;11, and LNCaP xenograft tumors, MI-773 (SAR405838) increased the levels of MDM2, p21 and p53 proteins in a dose- and time-dependent way and induced apoptosis. In the SJSA-1 xenograft model, MI-773 (SAR405838) (30-100 mg/kg) induced tumor regression and significantly inhibited tumor growth [1].
Reference:
[1]. Wang S, Sun W, Zhao Y, et al. SAR405838: an optimized inhibitor of MDM2-p53 interaction that induces complete and durable tumor regression. Cancer Res, 2014, 74(20): 5855-5865.
| Cas No. | 1303607-60-4 | SDF | |
| 同義語 | SAR405838 | ||
| Chemical Name | (2'S,3R,4'S,5'R)-6-chloro-4'-(3-chloro-2-fluorophenyl)-N-((1r,4R)-4-hydroxycyclohexyl)-2'-neopentyl-2-oxospiro[indoline-3,3'-pyrrolidine]-5'-carboxamide | ||
| Canonical SMILES | FC1=C(Cl)C=CC=C1[C@@H]2[C@@]3(C(C=CC(Cl)=C4)=C4NC3=O)[C@H](CC(C)(C)C)N[C@H]2C(N[C@@H]5CC[C@@H](O)CC5)=O | ||
| Formula | C29H34Cl2FN3O3 | M.Wt | 562.5 |
| 溶解度 | ≥ 17.2mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.7778 mL | 8.8889 mL | 17.7778 mL |
| 5 mM | 355.6 μL | 1.7778 mL | 3.5556 mL |
| 10 mM | 177.8 μL | 888.9 μL | 1.7778 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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- Purity: >98.00%
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Average Rating: 5 (Based on Reviews and 40 reference(s) in Google Scholar.)
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