Idasanutlin


Catalog No. Size PriceQuantity
M8041-2 2mg solid $85
M8041-10 10mg solid $255

Description

Idasanutlin, also known as RG7388 and RO5503781, is a highly potent and selective MDM2 antagonist with potential anticancer activity. RG7388 binds to MDM2 blocking the interaction between the MDM2 protein and the transcriptional activation domain of the tumor suppressor protein p53. By preventing the MDM2-p53 interaction, p53 is not enzymatically degraded and the transcriptional activity of p53 is restored. This may lead to p53-mediated induction of tumor cell apoptosis. MDM2, a zinc finger nuclear phosphoprotein and negative regulator of the p53 pathway, is often overexpressed in cancer cells and has been implicated in cancer cell proliferation and survival.

Product information

CAS Number: 1229705-06-9

Molecular Weight: 616.48

Formula: C31H29Cl2F2N3O4

Synonym:

Idasanutlin

RG 7388

RG-7388

Chemical Name: 4-((2R, 3S, 4R, 5S)-3-(3-chloro-2-fluorophenyl)-4-(4-chloro-2-fluorophenyl)-4-cyano-5-neopentylpyrrolidine-2-carboxamido)-3-methoxybenzoic acid.

Smiles: CC(C)(C)C[C@@H]1N[C@H]([C@H](C2=CC=CC(Cl)=C2F)[C@@]1(C#N)C1=CC=C(Cl)C=C1F)C(=O)NC1=CC=C(C=C1OC)C(O)=O

InChiKey: TVTXCJFHQKSQQM-LJQIRTBHSA-N

InChi: InChI=1S/C31H29Cl2F2N3O4/c1-30(2,3)14-24-31(15-36,19-10-9-17(32)13-21(19)34)25(18-6-5-7-20(33)26(18)35)27(38-24)28(39)37-22-11-8-16(29(40)41)12-23(22)42-4/h5-13,24-25,27,38H,14H2,1-4H3,(H,37,39)(H,40,41)/t24-,25-,27+,31-/m0/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO: 100 mg/mL(162.21 mM). Water: Insoluble.

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

Idasanutlin inhibits cell proliferation with IC50 of 30 nM, and induces dose-dependent p53 stabilization, cell cycle arrest, as well as cell apoptosis in cancer cells expressing wild-type p53.

In Vivo:

In a mouse SJSA human osteosarcoma xenograft model, Idasanutlin (25 mg/kg p.o.) causes tumor growth inhibition and regression. In a SJSA xenograft model, Idasanutlin results in induction of apoptosis and antiproliferation.

References:

  1. Ding Q, et al. J Med Chem. 2013, 56(14), 5979-5983.
  2. Higgins B, et al. Clin Cancer Res. 2014, 20(14), 3742-3752.

Products are for research use only. Not for human use.

Payment & Security

American Express Diners Club Discover JCB Mastercard PayPal Venmo Visa

Your payment information is processed securely. We do not store credit card details nor have access to your credit card information.

Estimate shipping

You may also like

Recently viewed