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Chemical Structure| 675576-97-3 Chemical Structure| 675576-97-3

Structure of Nutlin-3b
CAS No.: 675576-97-3

Chemical Structure| 675576-97-3

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Nutlin 3b is a MDM2/p53 antagonist or inhibitor with IC50 of 13.6 μM.

Synonyms: (+)-Nutlin-3

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Product Details of Nutlin-3b

CAS No. :675576-97-3
Formula : C30H30Cl2N4O4
M.W : 581.49
SMILES Code : 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
Synonyms :
(+)-Nutlin-3
MDL No. :MFCD11977784
InChI Key :BDUHCSBCVGXTJM-IZLXSDGUSA-N
Pubchem ID :16755649

Safety of Nutlin-3b

GHS Pictogram:
Signal Word:Danger
Hazard Statements:H302-H319-H332-H372-H400
Precautionary Statements:P260-P264-P270-P273-P280-P301+P312+P330-P304+P312-P305+P351+P338-P314-P337+P313-P391-P501
Class:9
UN#:3077
Packing Group:

Isoform Comparison

Biological Activity

Description
Nutlin-3b acts as an inhibitor of the p53/MDM2 interaction, with an IC50 of 13.6 μM, showcasing a binding affinity to MDM2 that is 150-fold less potent than that of Nutlin-3a[1].

In Vitro:

Cell Line
Concentration Treated Time Description References
NHF-hTERT E6 and NHF-hTERT p53 shRNA cells 10 μM 7 days No senescent phenotype observed PMC3379802
IMR-90, MRC-5, GM08402 human lung fibroblasts 10 μM 7 days Induced cellular senescence, detected by SA-β-gal staining PMC3379802
NHF-hTERT cells 10 μM 7 days Induced cellular senescence, detected by SA-β-gal staining PMC3379802
GM08402 primary human skin fibroblasts 10 μM 7 days Induced cellular senescence, detected by SA-β-gal staining PMC3379802

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Nude mice Orthotopic hepatic tumor model Oral Nutlin-3, intraperitoneal arsenic trioxide 200 mg/kg Nutlin-3 + 5 mg/kg arsenic trioxide Twice daily Nutlin-3, daily arsenic trioxide, for 28 days Combination of Nutlin-3 and arsenic trioxide significantly inhibited tumor growth and lung metastasis PMC4046148
C57BL/6 mice Genetic retinoblastoma models Subconjunctival injection 25 mM Every 3 weeks for 18 weeks To test the pharmacokinetics and efficacy of nutlin-3aOC, results showed that subconjunctival administration significantly improved intraocular penetration without ocular or hematologic toxicity. PMC3477706
Nude mice Orthotopic hepatic tumor model Oral 200 mg/kg Twice daily for 28 days To evaluate the inhibitory effects of Nutlin-3 combined with arsenic trioxide on tumor growth and metastasis, results showed that the combination therapy significantly inhibited tumor growth and lung metastasis. PMC4046148
Mice EC-Bmpr2−/− mice Intraperitoneal injection 12 mg/kg Once daily for two weeks Nutlin-3a restores endothelial p53 and PPARγ-p53 complex formation, induces target gene expression, regenerates pulmonary microvessels and reverses pulmonary hypertension PMC7908816
NOD.Cg-PrkdcIl2rg/SzJ mice Cell line-derived xenograft model Oral gavage and tail vein injection 37.5 mg/kg idasanutlin + 3 mg/kg carfilzomib Idasanutlin on days 1-5 of each week, carfilzomib on days 1 and 4 of each week, for up to 3 weeks The combination of idasanutlin and carfilzomib significantly enhanced overall survival by reducing tumor growth. PMC10391328
Mice Genetic retinoblastoma models Subconjunctival injection 25 mM Every 3 weeks for 18 weeks To test the pharmacokinetics and efficacy of nutlin-3aOC, results showed that subconjunctival administration significantly improved intraocular penetration without ocular or hematologic toxicity. PMC3116943
Mice Fmr1 KO Mice model Intraperitoneal injection 10 mg/kg Every other day for five injections To evaluate the long-term effects of Nutlin-3 on hippocampal neurogenesis and cognitive functions in Fmr1 KO mice. Results showed that transient Nutlin-3 treatment had long-lasting beneficial effects on neurogenesis and cognitive functions. PMC9103116

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.72mL

0.34mL

0.17mL

8.60mL

1.72mL

0.86mL

17.20mL

3.44mL

1.72mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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