IMR-1A

IMR-1A, a acid metabolite of IMR-1, is a Notch inhibitor with an IC50 of 0.5 μM. IMR-1A has a 50-fold increase in potency with respect to IMR-1. IMR-1 can metabolize in vivo to IMR-1A.

Product information

CAS Number: 331862-41-0

Molecular Weight: 325.36

Formula: C13H11NO5S2

Chemical Name: 2-(2-methoxy-4-{[(5E)-4-oxo-2-sulfanylidene-1, 3-thiazolidin-5-ylidene]methyl}phenoxy)acetic acid

Smiles: COC1=CC(=CC=C1OCC(O)=O)/C=C1/SC(=S)NC/1=O

InChiKey: DVBJNSKWHSGTDK-BJMVGYQFSA-N

InChi: InChI=1S/C13H11NO5S2/c1-18-9-4-7(2-3-8(9)19-6-11(15)16)5-10-12(17)14-13(20)21-10/h2-5H,6H2,1H3,(H,15,16)(H,14,17,20)/b10-5+

Technical Data

Appearance: Solid Power

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

Solubility: DMSO : 2 mg/mL (6.15 mM; Need ultrasonic)

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: ≥360 days 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:

IMR-1A (2 mg/kg (i.v.) and 100 mg/kg (i.p)) exhibits low systematic plasma clearance (CL = 7 mL/min/kg) with terminal elimination half-life (T1/2) of 2.22 h following a single i.v. administration. The normal liver blood flow in mice is 90 mL/min/kg and the Vss (volume of distribution) is ~4-fold. Plasma concentrations is quantifiable up to 24 h with Tmax of 0.50 h after i.p. administration.

References:

1. Astudillo L et al. The Small Molecule IMR-1 Inhibits the Notch Transcriptional Activation Complex to Suppress Tumorigenesis. Cancer Res. 2016 Jun 15;76(12):3593-603.

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