OTX-015

Catalog #

27636-1

$295 *

Size: 5 mg

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Description

OTX-015 is a potent new BRD-inhibitor with evident anti-proliferative activity in several cell lines representative of mature B-cell tumors.

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Synonyms

OTX 015; OTX015

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Product Info

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Citations

Purity

≥98% by HPLC

Formula

C₂₅H_{22ClN₅O₂S}

492 Da

Solubility

Soluble in DMSO

Biological Activity

OTX-015 is a potent BET bromodomain inhibitor with EC50 ranging from 10 to 19 nM for BRD2, BRD3, and BRD4. IC50 Value: 0.192 uM (DLBCL cell lines). In vitro, OTX-015 demonstrated anti-proliferative activity in DLBCL cell lines (median IC50 0.192 µM). Similar results were obtained on SMZL (median IC50 0.165 µM), and on MM cell lines (median IC50 0.449 µM). MCL cell lines appeared less sensitive to OTX-015 (median IC50 2.01 µM). Among DLBCL cell lines, there was no difference based upon the cell of origin of the cell lines.

CAS Registry #

202590-98-5

Background

Bromodomains have an important role in the targeting of chromatin-modifying enzymes to specific sites, including methyltransferases, HATs and transcription factors and regulate diverse biological processes from cell proliferation and differentiation to energy homeostasis and neurological processes.

References

1. Noel, J.K., et al. Mol. Cancer Ther. 12 , C244 (2013).
2. Braun, T., et al. Blood 122, 4218 (2014).

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OTX-015

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