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Chemical Structure : OTX-015
CAS No.: 202590-98-5
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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 25 mg | $198 | In stock | |
| 100 mg | $498 | In stock | |
| 200 mg | $788 | In stock | |
| 1 g | Get quote | ||
| 5 g | Get quote |
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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.
| M.Wt | 491.99 | |
| Formula | C25H22ClN5O2S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
O=C(NC1=CC=C(O)C=C1)C[C@H]2C3=NN=C(C)N3C4=C(C(C)=C(C)S4)C(C5=CC=C(Cl)C=C5)=N2 |
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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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