MI-773 (SAR405838) (Synonyms: SAR405838) |
| Catalog No.GC11547 |
MI-773 (SAR405838) (MI-77301), an analog of MI-773, is a highly potent and selective MDM2-p53 interaction inhibitor. MI-773 (SAR405838) binds to MDM2 with a Ki of 0.88 nM. MI-773 (SAR405838) induces apoptosis and has potent antitumor activity.
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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 | |
| Synonyms | 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 |
| Solubility | ≥ 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. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.7778 mL | 8.8889 mL | 17.7778 mL |
| 5 mM | 0.3556 mL | 1.7778 mL | 3.5556 mL |
| 10 mM | 0.1778 mL | 0.8889 mL | 1.7778 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
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- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 40 reference(s) in Google Scholar.)
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