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BMS-986242

Chemical Structure : BMS-986242

CAS No.: 1923844-48-7

BMS-986242 (BMS986242)

Catalog No.: PC-72378Not For Human Use, Lab Use Only.

BMS-986242 (BMS986242) is a potent, selective IDO1 inhibitor with IC50 of 2 nM in cellular IDO1 inhibition assays and IC50 of 25 nM in human whole blood (HWB) IDO1 inhibition assays.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

BMS-986242 (BMS986242) is a potent, selective IDO1 inhibitor with IC50 of 2 nM in cellular IDO1 inhibition assays and IC50 of 25 nM in human whole blood (HWB) IDO1 inhibition assays.
BMS-986242 shows activity against a variety of cancers including metastatic melanoma and renal cell carcinoma.
BMS-986242 elicited a PD effect comparable to linrodostat and epacadostat in a PD model of tumor kynurenine reduction at a lower level of exposure.
BMS-986242 is a structurally differentiated clinical candidate that performs comparably to linrodostat (BMS-986205) in terms of both in vitro potency and in vivo pharmacodynamic effect in a mouse xenograft model.

Physicochemical Properties

M.Wt 410.917
Formula C24H24ClFN2O
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

4-chloro-N-((R)-1-((1s,4S)-4-(6-fluoroquinolin-4-yl)cyclohexyl)ethyl)benzamide

References

1. Cherney EC, et al. ACS Med Chem Lett. 2021 Jan 28;12(2):288-294.

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