Nutlin-3b

Alias: (+)-Nutlin-3; Nutlin 3b; Nutlin-3b; Nutlin3b
Cat No.:V0043 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 interactionwith IC50 value of 13.6 μM.
Nutlin-3b Chemical Structure CAS No.: 675576-97-3
Product category: Mdm2
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
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Other Forms of Nutlin-3b:

  • Nutlin-3a
  • Nutlin (3)
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

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.

Biological Activity I Assay Protocols (From Reference)
Targets
MDM2/p53 (IC50 = 13.6 μg/mL)
ln Vitro
Nutlin-3b is useful as a negative control s for non-MDM2-related cellular activities.Only in cells that have p53 that is in the wild-type form does nutlin-3a induce the expression of MDM2 and p21 (but not p53). Regardless of whether the cells have p53 or not, nutlin-3b has no impact. Only the active enantiomer Nutlin-3a distinguishes between cells harboring mutant and wild-type p53 and exhibits strong antiproliferative activity. Nutlin-3b's potency against mutant p53 cells is almost identical to that of Nutlin-3a, while it is significantly less potent against wild-type p53 cells. After 48 hours of exposure to Nutlin-3a, 45% of the cell population became TUNEL positive, but cells treated with Nutlin-3b are identical to the untreated controls. [1]
ln Vivo
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.
Animal Protocol
HCT116, RKO, SJSA-1, SW480, and MDA-MB-435
~30 μM; 48 h
MTT assay
References

[1]. Science . 2004 Feb 6;303(5659):844-8.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C30H30CL2N4O4
Molecular Weight
581.49
Exact Mass
580.1644
Elemental Analysis
C, 61.97; H, 5.20; Cl, 12.19; N, 9.64; O, 11.01
CAS #
675576-97-3
Appearance
Solid powder
SMILES
CC(C)OC1=C(C=CC(=C1)OC)C2=N[C@@H]([C@@H](N2C(=O)N3CCNC(=O)C3)C4=CC=C(C=C4)Cl)C5=CC=C(C=C5)Cl
InChi Key
BDUHCSBCVGXTJM-IZLXSDGUSA-N
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
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
Synonyms
(+)-Nutlin-3; Nutlin 3b; Nutlin-3b; Nutlin3b
HS Tariff Code
2934.99.9001
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)
Solubility Data
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)
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.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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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.

Biological Data
  • Nutlin-3b

  • Nutlin-3b

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