OTX 015

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Cat.No. 6181 - OTX 015 | C25H22ClN5O2S | CAS No. 202590-98-5
Description: BET bromodomain inhibitor; orally bioavailable
Chemical Name: (6S)-4-(4-Chlorophenyl)-N-(4-hydroxyphenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide
Purity: ≥98% (HPLC)
Datasheet
Citations
Literature

Biological Activity

BET bromodomain inhibitor (IC50 values are in the range 92 - 112 nM). Inhibits proliferation and induces apoptosis of leukemia cell lines in vitro. Decreases BRD2, BRD4 and c-MYC protein expression. Orally bioavailable.

Technical Data

M. Wt 491.99
Formula C25H22ClN5O2S
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 202590-98-5
PubChem ID 9936746
InChI Key GNMUEVRJHCWKTO-FQEVSTJZSA-N
Smiles CC1=C(C2=C(N3C(C)=NN=C3[C@@H](N=C2C4=CC=C(C=C4)Cl)CC(NC5=CC=C(C=C5)O)=O)S1)C

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 49.2 100
ethanol 9.84 20

Preparing Stock Solutions

The following data is based on the product molecular weight 491.99. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.03 mL 10.16 mL 20.33 mL
5 mM 0.41 mL 2.03 mL 4.07 mL
10 mM 0.2 mL 1.02 mL 2.03 mL
50 mM 0.04 mL 0.2 mL 0.41 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

Berenguer-Daizé et al (2016) OTX015 (MK-8628), a novel BET inhibitor, displays in vitro and in vivo antitumor effects alone and in combination with conventional therapies in glioblastoma models. Int.J.Cancer 139 2047 PMID: 27388964

Coudé et al (2015) BET inhibitor OTX015 targets BRD2 and BRD4 and decreases c-MYC in acute leukemia cells. Oncotarget 6 17698 PMID: 25989842


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Keywords: OTX 015, supplier, OTX015, BET, bromodomain, extraterminal, BRD2, BRD3, BRD4, inhibitors, inhibits, leukemia, Bromodomains, Bromodomains, Tocris Bioscience

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