| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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Purity: ≥98%
MI-773 (2'R,3S-isomer) (also known as MI773; SAR-405838; SAR405838), a spirooxindole analog, is a specific and orally bioavailable small molecule antagonist of MDM2-p53 protein‐protein interaction with antitumor activity. With a Ki value of 0.88 nM, it prevents the interaction of MDM2-p53. Clinical trials had already begun when it was abandoned for business purposes.
| Targets |
MDM2 (Ki = 0.88 nM); MDM2 (Kd = 8.2 nM)
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|---|---|
| ln Vitro |
MI-773 binds to MDM2 with a Ki of 0.88 nM. MI-773 potently inhibits cell growth in cancer cell lines, including SJSA-1 (IC50, 0.092 μM), RS4;11 (IC50, 0.089 μM), LNCaP (IC50, 0.27 μM), and HCT-116 (IC50, 0.20 μM) cells, and displays high selectivity over cancer cell lines with mutated or deleted p53, including SAOS-2 (IC50, >10 μM), PC-3 (IC50, >10 μM), SW620 (IC50, >10 μM), and HCT-116 (p53-/-) (IC50, >20 μM) cells. [1]
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| ln Vivo |
MI-773 (p.o.) effectively inhibits tumor growth in a dose-dependent manner in the SJSA-1 osteosarcoma, acute lymphoblastic leukemia RS4;11, LNCaP prostate cancer, and HCT-116 colon cancer xenograft model (10 mg/kg, 30 mg/kg, 50 mg/kg, 100 mg/kg, and 200 mg/kg). [1]
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| Enzyme Assay |
Using a Fluorescence-polarization (FP) binding assay, the binding affinities of p53 peptide and MDM2 inhibitors to the MDM2 protein are assessed. Using a competitive FP-based assay, MI-773's binding affinities to Bcl-2, Bcl-xL, Mcl-1, and β--catenin are identified, and its affinity to MDMx is identified using Biolayer Interferometry technology.
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| Cell Assay |
In a water-soluble tetrazolium-based assay, cell growth inhibition activity is assessed. Trypan blue staining is used to measure cell death, and a kit for staining with Annexin V-FLUOS determines apoptosis.
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| References |
| Molecular Formula |
C29H34CL2FN3O3
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|---|---|
| Molecular Weight |
562.503
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| Exact Mass |
561.20
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| Elemental Analysis |
C, 61.92; H, 6.09; Cl, 12.60; F, 3.38; N, 7.47; O, 8.53
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| CAS # |
1303607-07-9
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| Related CAS # |
1303607-07-9; 1303607-60-4;
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| Appearance |
Solid powder
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| SMILES |
CC(C)(C)C[C@@H]1[C@]2([C@H]([C@@H](N1)C(=O)NC3CCC(CC3)O)C4=C(C(=CC=C4)Cl)F)C5=C(C=C(C=C5)Cl)NC2=O
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| InChi Key |
IDKAKZRYYDCJDU-YJRDPZTCSA-N
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| InChi Code |
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+/m1/s1
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| Chemical Name |
(2'R,3S,3'S,5'R)-6-chloro-3'-(3-chloro-2-fluorophenyl)-5'-(2,2-dimethylpropyl)-N-(4-hydroxycyclohexyl)-2-oxospiro[1H-indole-3,4'-pyrrolidine]-2'-carboxamide
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| Synonyms |
MI 773; MI773; MI-773
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~100 mg/mL (~177.8 mM)
Ethanol: ~31 mg/mL (~55.1 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.44 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.44 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.44 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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