Elimusertib (BAY-1895344)

Elimusertib (BAY-1895344) is a very potent and highly selective ATR (ataxia telangiectasia and Rad3-related) inhibitor with IC50 of 7 nM. Elimusertib potently inhibits proliferation of a broad spectrum of human tumor cell lines with median IC50 of 78 nM.

Product information

CAS Number: 1876467-74-1

Molecular Weight: 375.43

Formula: C20H21N7O

Synonym:

BAY-1895344

Chemical Name: (R)-3-methyl-4-(4-(1-methyl-1H-pyrazol-5-yl)-8-(1H-pyrazol-5-yl)-1, 7-naphthyridin-2-yl)morpholine hydrochloride

Smiles: CN1N=CC=C1C1=CC(=NC2=C(N=CC=C12)C1=CC=NN1)N1CCOC[C@H]1C

InChiKey: YBXRSCXGRPSTMW-CYBMUJFWSA-N

InChi: InChI=1S/C20H21N7O/c1-13-12-28-10-9-27(13)18-11-15(17-5-8-23-26(17)2)14-3-6-21-20(19(14)24-18)16-4-7-22-25-16/h3-8,11,13H,9-10,12H2,1-2H3,(H,22,25)/t13-/m1/s1

Technical Data

Appearance: Solid Power

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

Solubility: DMSO: 5.4 mg/mL (14.38 mM)

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:

BAY-1895344 inhibits tumor cell growth and viability and exhibits potent antiproliferative activity in a broad spectrum of human tumor cell lines.

In Vivo:

BAY 1895344 exhibits strong monotherapy efficacy in cancer xenograft models that carry DNA damage repair deficiencies.

References:

1. Ulrich T. Luecking, et al. Abstract 983: Identification of potent, highly selective and orally available ATR inhibitor BAY 1895344 with favorable PK properties and promising efficacy in monotherapy and combination in preclinical tumor models. Cancer Research. July 2017 Volume 77, Issue 13 Supplement.
2. Antje Margret Wengner, et al. Abstract 836: ATR inhibitor BAY 1895344 shows potent anti-tumor efficacy in monotherapy and strong combination potential with the targeted alpha therapy Radium-223 dichloride in preclinical tumor models. Cancer Research. July 2017 Volume 77, Issue 13 Supplement

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