| ln Vivo |
MI-773 (10-100 mg/kg; orally; once daily) TFA induced dose-dependent tumor growth inhibition and regression in the UM-PDX-HACC-5 adenoid cystic carcinoma model, with a dose of 100 mg/kg mediating 127% TGI index and 86% tumor shrinkage via p53-dependent apoptosis [1]. MI-773 (100 mg/kg; orally; once daily) TFA mediated significant tumor regression in the ACCx6 adenoid cystic carcinoma PDX model [1]. MI-773 (100 mg/kg; orally; once daily) TFA mediated significant tumor regression in the ACCx9 adenoid cystic carcinoma PDX model [1].
|
|---|---|
| Animal Protocol |
Animal/Disease Models:CB.17.SCID (male and female, severe combined immunodeficiency) [1]
Doses: 10 mg/kg; 50 mg/kg; 100 mg/kg Route of Administration: Oral; Daily Experimental Results: After 20 days of treatment (10 mg/kg), tumor growth rate decreased slightly, tumor growth inhibition rate (TGI) was 34%, and the final average tumor volume was 600 mm3, with a tumor growth inhibition rate of 34%. After 20 days of treatment (100 mg/kg), tumor growth inhibition rate (TGI) reached 127%, tumor volume decreased by 86%, and the final average tumor volume was 30 mm3, with a tumor growth inhibition rate of 100 mg/kg. After 20 days of treatment (100 mg/kg), tumor regression time was prolonged (defined as tumor volume increasing to twice the pre-treatment volume; p=0.044). The proportion of TUNEL-positive apoptotic cells (p=0.015) and p53-positive cells (p<0.001) in tumor tissue was increased, and p53 localization shifted from the nucleus to the cytoplasm (100 mg/kg). The levels of p53 and phosphorylated p53 (Ser392) proteins in tumor lysates were elevated (50 or 100 mg/kg). No significant weight loss was observed in any of the treatment groups. |
| References |
| Molecular Formula |
C31H35CL2F4N3O5
|
|---|---|
| Molecular Weight |
676.53
|
| CAS # |
1303609-37-1
|
| Related CAS # |
MI-773
|
| Appearance |
White to off-white solid
|
| SMILES |
O=C([C@H](N[C@@H]1CC(C)(C)C)[C@H](C2=CC=CC(Cl)=C2F)[C@]31C(NC4=C3C=CC(Cl)=C4)=O)N[C@H]5CC[C@H](O)CC5.OC(C(F)(F)F)=O
|
| 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 Note: 请将本产品存放在密封保护的环境中，避免受潮。 |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~147.81 mM; with sonication)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.70 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 canAdd 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. Preparation of 20% SBE-β-CD saline (4°C, store for one week): Dissolve 2 g of SBE-β-CD powder in 10 mL of saline until completely dissolved and clear. 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. Solubility in Formulation 2: ≥ 2.5 mg/mL (3.70 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 canAdd 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.4781 mL | 7.3907 mL | 14.7813 mL | |
| 5 mM | 0.2956 mL | 1.4781 mL | 2.9563 mL | |
| 10 mM | 0.1478 mL | 0.7391 mL | 1.4781 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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