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Birabresib

Chemical Structure : Birabresib

CAS No.: 202590-98-5

Birabresib (OTX-015, MK-8628)

Catalog No.: PC-20573Not For Human Use, Lab Use Only.

Birabresib (OTX-015) is a potent, competitive inhibitor of BET bromodomain BRD2, BRD3, and BRD4 with EC50 of 10-19 nM, inhibits binding of BRD2, BRD3, and BRD4 to acetylated histone H4 (AcH4) with IC50 of 92-112 nM.

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

Biological Activity

Birabresib (OTX-015) is a potent, competitive inhibitor of BET bromodomain BRD2, BRD3, and BRD4 with EC50 of 10-19 nM, inhibits binding of BRD2, BRD3, and BRD4 to acetylated histone H4 (AcH4) with IC50 of 92-112 nM.
OTX015 inhibits cell growth of a variety of human cancer cell lines with IC50 of 60-200 nM for hematologic malignancies cells.
Oral administration of OTX015 significantly inhibited the growth of Ty82 BRD-NUT midline carcinoma tumors in nude mice, showing 79% TGI at 100 mg/kg qd and 61% TGI at 10 mg/kg bid.

Physicochemical Properties

M.Wt 491.99
Formula C25H22ClN5O2S
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

(S)-2-(4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)-N-(4-hydroxyphenyl)acetamide

References

1. J. Kay Noel, et al. Mol Cancer Ther (2013) 12 (11_Supplement): C244.

2. Klingbeil O, et al. Cell Death Dis. 2016 Sep 8;7(9):e2365.

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