| Size | Price | Stock | Qty |
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| 5mg |
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| Other Sizes |
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| ln Vitro |
In MCF7 and ZR75-30 cell lines, RO-5963 (10–20 μM; 48 hours) exhibits more apoptotic activity than Nutlin [1]. Effectively activating p53 and raising p21 and MDM2 levels, RO-5963 (10 μM, 24 hours) [1].
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| Cell Assay |
Apoptosis analysis [1]
Cell Types: ZR75-30, MCF7 Cell Tested Concentrations: 10, 20 μM Incubation Duration: 48 hrs (hours) Experimental Results: Strong display of apoptotic activity. Western Blot Analysis[1] Cell Types: LNCap, U2OS, RKO, A489, 22Rv1, HCT116, H460, LOX, MCF7, A549, G401 Cell Tested Concentrations: 10 μM Incubation Duration: 24 hrs (hours) Experimental Results: Effectively activates p53 and increases p21 and MDM2 level. |
| References |
| Molecular Formula |
C24H21CLF2N4O5
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|---|---|
| Molecular Weight |
518.897151708603
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| Exact Mass |
518.116
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| CAS # |
1416663-77-8
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| PubChem CID |
136209736
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
1.4
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
36
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| Complexity |
959
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=C(C=CC\2=C1N=C/C2=C\C3=C(N(C(=O)N3)C(C4=CC(=C(C=C4)F)F)C(=O)NC(CO)CO)O)Cl
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| InChi Key |
IFYMUYSGUSHEPI-NTUHNPAUSA-N
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| InChi Code |
InChI=1S/C24H21ClF2N4O5/c1-11-16(25)4-3-15-13(8-28-20(11)15)7-19-23(35)31(24(36)30-19)21(22(34)29-14(9-32)10-33)12-2-5-17(26)18(27)6-12/h2-8,14,21,32-33,35H,9-10H2,1H3,(H,29,34)(H,30,36)/b13-7+
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| Chemical Name |
2-[5-[(Z)-(6-chloro-7-methylindol-3-ylidene)methyl]-4-hydroxy-2-oxo-1H-imidazol-3-yl]-2-(3,4-difluorophenyl)-N-(1,3-dihydroxypropan-2-yl)acetamide
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| Synonyms |
RO-5963 RO5963 RO 5963
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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 : ~150 mg/mL (~289.07 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 3.75 mg/mL (7.23 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 37.5 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: ≥ 3.75 mg/mL (7.23 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 37.5 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9272 mL | 9.6358 mL | 19.2715 mL | |
| 5 mM | 0.3854 mL | 1.9272 mL | 3.8543 mL | |
| 10 mM | 0.1927 mL | 0.9636 mL | 1.9272 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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