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Fig. 1 · Structure
Cat. No.
A13890
CAS No.
202590-98-5
Formula
C25H22ClN5O2S
Mol. Weight
491.99

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Birabresib (OTX015)

Cat. No. A13890 CAS 202590-98-5

BET inhibitor

OTX015 is an orally bioavailable, small molecule inhibitor of BRD2, BRD3, and BRD4 (EC50s = 10-19 nM).

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Biological Activity

Target & Activity

Target Activity Value
BRDs (Cell-free assay) EC50 10-19 nM

Cellular Effect

Cell Line Activity Value Description Reference
CAKI-1 GI50 94.6 nM Antiproliferative activity against human CAKI-1 cells assessed as cell growth inhibition measured after 72 hrs by CellTiter-Glo assay [PMID: 34731760]
Daoy GI50 160 nM Antitumor activity against human Daoy cells assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo luminescent assay [PMID: 33636537]
HAL-01 IC50 2.53 μM Anticancer activity against human HAL-01 cells assessed as cell growth inhibition by CellTiter-Glo luminescent assay [PMID: 34582215]
HCT-15 GI50 178.6 nM Antiproliferative activity against human HCT-15 cells assessed as cell growth inhibition measured after 72 hrs by CellTiter-Glo assay [PMID: 34731760]
HL-60 IC50 0.82 μM Anticancer activity against human HL-60 cells assessed as cell growth inhibition by CellTiter-Glo luminescent assay [PMID: 34582215]
HL-60(TB) GI50 178.6 nM Antiproliferative activity against human HL-60(TB) cells assessed as cell growth inhibition measured after 72 hrs by CellTiter-Glo assay [PMID: 34731760]
HPBALL IC50 7.01 μM Anticancer activity against human HPBALL cells assessed as cell growth inhibition by CellTiter-Glo luminescent assay [PMID: 34582215]
K562 IC50 2.84 μM Anticancer activity against human K562 cells assessed as cell growth inhibition by CellTiter-Glo luminescent assay [PMID: 34582215]
Kasumi 1 IC50 135 nM Antiproliferative activity against human Kasumi-1 cells assessed as reduction in cell viability measured after 72 hrs by Celltitre-glo luminescence assay [PMID: 32208600]
MDA-MB-468 GI50 212.3 nM Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition measured after 72 hrs by CellTiter-Glo assay [PMID: 34731760]
MM1.S IC50 137 nM Antiproliferative activity against human MM1S cells assessed as reduction in cell viability measured after 72 hrs by Celltitre-glo luminescence assay [PMID: 32208600]
MM1.S IC50 22.7 nM Antiproliferative activity against human MM1S cells assessed as cell growth inhibition after 4 days by CCK8 assay [PMID: 31461688]
MM1.S IC50 6.3 nM Antiproliferative activity against human MM1S cells after 72 hrs by CCK8 or SRB assay [PMID: 31490070]
MOLM-14 EC50 0.08 μM Cytotoxicity against human MOLM-14 cells assessed as reduction in cell viability incubated for 72 hrs [PMID: 35348328]
MV4-11 IC50 0.2 μM Antiproliferative activity against human MV4-11 cells assessed as cell viability after 72 hrs by CCK8 assay [PMID: 33077265]
MV4-11 IC50 17.6 nM Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition after 4 days by CCK8 assay [PMID: 31461688]
MV4-11 IC50 46.3 nM Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability measured after 72 hrs by Celltitre-glo luminescence assay [PMID: 32208600]
NCI-H522 GI50 262.4 nM Antiproliferative activity against human NCI-H522 cells assessed as cell growth inhibition measured after 72 hrs by CellTiter-Glo assay [PMID: 34731760]
ONS-76 GI50 160 nM Antitumor activity against human ONS-76 cells assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo luminescent assay [PMID: 33636537]

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Specifications

Manufacturer Adooq Bioscience
Actions Inhibitor
CAS Number 202590-98-5
Applications BET inhibitor
Formula C25H22ClN5O2S
Molecular Weight 491.99
Synonyms OTX 015
SMILES
CC1=C(SC2=C1C(=N[C@H](C3=NN=C(N32)C)CC(=O)NC4=CC=C(C=C4)O)C5=CC=C(C=C5)Cl)C

Storage & Solubility

In Vitro Solubility

Reported Solubility

SolventReported Solubility
DMSO 89 mg/mL (180.9 mM)
Water Insoluble
Ethanol 89 mg/mL

Preparing Stock Solutions

Stock preparation is unavailable for this product molecular weight.

Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.

In Vivo Preparation

Concentration
4 mg/mL
Vehicle
2% DMSO+30% PEG 300+5% Tween 80+ddH2O

Storage

Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

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