A BRD2, BRD3, and BRD4 inhibitor
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OTX015

Item No. 15947

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal 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
CAS Number
202590-98-5
Synonyms
  • HY-15743
  • (−)-OTX015
Molecular Formula
C25H22ClN5O2S
Formula Weight
492.0
Purity
≥95%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 25 mg/mlDMSO: 25 mg/mlEthanol: 30 mg/mlEthanol:PBS (pH 7.2) (1:5): 0.1 mg/ml
λmax
254 nm
SMILES
ClC1=CC=C(C=C1)C2=N[C@@H](CC(NC3=CC=C(O)C=C3)=O)C4=NN=C(C)N4C5=C2C(C)=C(C)S5
InChi Code
InChI=1S/C25H22ClN5O2S/c1-13-14(2)34-25-22(13)23(16-4-6-17(26)7-5-16)28-20(24-30-29-15(3)31(24)25)12-21(33)27-18-8-10-19(32)11-9-18/h4-11,20,32H,12H2,1-3H3,(H,27,33)/t20-/m0/s1
InChi Key
GNMUEVRJHCWKTO-FQEVSTJZSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Cayman Chemical
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    Product Description

    The bromodomain and extra terminal domain (BET) family of proteins, including BRD2, BRD3, and BRD4, play a key role in many cellular processes, including inflammatory gene expression, mitosis, and viral/host interaction by controlling the assembly of histone acetylation-dependent chromatin complexes. OTX015 is an orally bioavailable, small molecule inhibitor of BRD2, BRD3, and BRD4 (EC50s = 10-19 nM).1 It displays antiproliferative effects at a sub-micromolar range in vitro in a wide range of solid tumor types and leukemias, downregulating c-Myc expression and inducing cell cycle arrest and apoptosis.1,2,3 At 100 mg/kg, OTX015 has been shown to inhibit the growth of Ty82 BRD-NUT midline carcinoma tumors in nude mice by 79%.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Noel, J.K., Iwata, K., Ooike, S., et al. Development of the BET bromodomain inhibitor OTX015. Mol. Cancer Ther. 12, C244 (2013).

    2. Braun, T., Coude, M.M., Berrou, J., et al. Preclinical study of the bromodomain inhibitor OTX015 in acute myeloid (AML) and lymphoid (ALL) leukemias. Blood 122, 4218 (2014).

    3. Boi, M., Todaro, M., Vurchio, V., et al. OTX015, a bromodomain and extraterminal inhibitor, represents a novel agent for ALK positive anaplastic large cell lymphoma. Mol. Cancer Ther. 12, A219 (2013).