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| 25mg |
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Purity: ≥98%
Nutlin-3b, a less active/inactive isomer of nutlin-3, is a novel antagonist or inhibitor of p53/MDM2 (murine double minute 2) protein protein interaction with IC50 value of 13.6 μM. Compared to Nutlin-3a, it is 150 times less potent.
| Targets |
MDM2/p53 (IC50 = 13.6 μg/mL)
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| ln Vitro |
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| ln Vivo |
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| Cell Assay |
On a Biacore S51, competition assay is conducted. An immobilized PentaHis antibody is used to capture the His-tagged p53 on a Series S Sensor chip CM5. A response unit equals one pg of protein per millimeter 2, so the level of capture is around 200. MDM2 protein is kept at a constant 300 nM concentration. Each MDM2 test sample contains a concentration series of Nutlin-3 after it has been dissolved in DMSO at a 10 mM concentration and further diluted. Running buffer (10 mM Hepes, 0.15 M NaCl, 2% DMSO) is used for the assay, which is carried out at 25 °C. Calculating IC50 involves calculating the percentage of MDM2-p53 binding in the presence of Nutlin-3 compared to binding in the absence of Nutlin-3.
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| Animal Protocol |
HCT116, RKO, SJSA-1, SW480, and MDA-MB-435
~30 μM; 48 h MTT assay |
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| References | ||
| Additional Infomation |
Nutlin-3 is a Nutlin and a piperazinone. It has a role as an anticoronaviral agent.
Nutlin-3 is a small molecule inhibitor that targets p53-Mdm2 interaction. |
| Molecular Formula |
C30H30CL2N4O4
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| Molecular Weight |
581.49
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| Exact Mass |
580.164
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| Elemental Analysis |
C, 61.97; H, 5.20; Cl, 12.19; N, 9.64; O, 11.01
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| CAS # |
675576-97-3
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| Related CAS # |
Nutlin-3a;675576-98-4;Nutlin-3;548472-68-0
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| PubChem CID |
16755649
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| Appearance |
Off-white to yellow solid powder
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| Density |
1.4±0.1 g/cm3
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| Index of Refraction |
1.648
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| LogP |
2.77
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
40
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| Complexity |
919
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| Defined Atom Stereocenter Count |
2
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| SMILES |
O=C1NCCN(C(N2[C@@H](C3=CC=C(Cl)C=C3)[C@@H](C4=CC=C(Cl)C=C4)N=C2C5=CC=C(OC)C=C5OC(C)C)=O)C1
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| InChi Key |
BDUHCSBCVGXTJM-IZLXSDGUSA-N
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| InChi Code |
InChI=1S/C30H30Cl2N4O4/c1-18(2)40-25-16-23(39-3)12-13-24(25)29-34-27(19-4-8-21(31)9-5-19)28(20-6-10-22(32)11-7-20)36(29)30(38)35-15-14-33-26(37)17-35/h4-13,16,18,27-28H,14-15,17H2,1-3H3,(H,33,37)/t27-,28+/m1/s1
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| Chemical Name |
4-[(4R,5S)-4,5-bis(4-chlorophenyl)-2-(4-methoxy-2-propan-2-yloxyphenyl)-4,5-dihydroimidazole-1-carbonyl]piperazin-2-one
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| Synonyms |
(+)-Nutlin-3; Nutlin 3b; Nutlin-3b; Nutlin3b
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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 (~172.0 mM)
Water: <1 mg/mL (slightly soluble or insoluble) Ethanol: ~100 mg/mL (~172.0 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.30 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 (4.30 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 can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7197 mL | 8.5986 mL | 17.1972 mL | |
| 5 mM | 0.3439 mL | 1.7197 mL | 3.4394 mL | |
| 10 mM | 0.1720 mL | 0.8599 mL | 1.7197 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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