Deltarasin hydrochloride

Deltarasin hydrochloride is an inhibitor of KRAS-PDEδinteraction with Kd of 38 nM for binding to purified PDEδ.

Product information

CAS Number: 1613404-76-4

Molecular Weight: 640.22

Formula: C40H38ClN5O

Chemical Name: N-(2-(3-(piperazin-1-ylmethyl)imidazo[2, 1-b]thiazol-6-yl)phenyl)quinoxaline-2-carboxamide hydrochloride

Smiles: Cl.C(C1C=CC=CC=1)N1C(=NC2=CC=CC=C12)C1C=CC(=CC=1)OC[C@H](C1CCNCC1)N1C(=NC2=CC=CC=C12)C1C=CC=CC=1

InChiKey: RNNBDBVWCNENOV-XVYLPRMCSA-N

InChi: InChI=1S/C40H37N5O.ClH/c1-3-11-29(12-4-1)27-44-36-17-9-7-15-34(36)42-39(44)32-19-21-33(22-20-32)46-28-38(30-23-25-41-26-24-30)45-37-18-10-8-16-35(37)43-40(45)31-13-5-2-6-14-31;/h1-22,30,38,41H,23-28H2;1H/t38-;/m1./s1

Technical Data

Appearance: Solid Power

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

Solubility: DMSO : ≥ 52 mg/mL (81.22 mM). H2O : 50 mg/mL (78.10 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: ≥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:

In liver cells, deltarasin inhibits the interaction of RAS with PDEδ with KD of 41 nM. Inhibition of PDEδ-KRAS interaction by deltarasin suppresses proliferation of human pancreatic ductal adenocarcinoma cells that are dependent on oncogenic KRAS.

In Vivo:

Deltarasin (10 mg/kg, i.p.) impairs dose-dependent tumor growth in nude mice bearing subcutaneous human Panc-Tu-I tumour cell xenografts.

References:

1. Zimmermann G, et al. Small molecule inhibition of the KRAS-PDEδ interaction impairs oncogenic KRAS signalling. Nature. 2013 May 30;497(7451):638-42.

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