202590-98-5 Usage
Description
OTX015 is a potent BET bromodomain inhibitor that targets BRD2, BRD3, and BRD4 proteins, which play a crucial role in various cellular processes such as inflammatory gene expression, mitosis, and viral/host interaction. It is an orally bioavailable small molecule with an EC50 ranging from 10 to 19 nM for BRD2, BRD3, and BRD4 in cell-free assays. OTX015 has demonstrated antiproliferative effects in a wide range of solid tumor types and leukemias, downregulating c-Myc expression and inducing cell cycle arrest and apoptosis.
Uses
Used in Oncology:
OTX015 is used as an anti-tumor agent for its ability to inhibit the growth of various solid tumors and leukemias. It works by targeting the BET bromodomain proteins, leading to downregulation of c-Myc expression, cell cycle arrest, and apoptosis. In preclinical studies, OTX015 has shown significant tumor growth inhibition in Ty82 BRD-NUT midline carcinoma tumors in nude mice at a dosage of 100 mg/kg.
Used in Drug Development:
OTX015 is used as a lead compound in the development of novel therapeutics for cancer treatment. Its potent inhibition of BET bromodomain proteins and demonstrated anti-tumor activity make it a promising candidate for further research and development in the field of oncology.
Features
Orally bioavailable BRD2/3/4-selective inhibitor that has been tested in Phase I clinical trials for treatment of Haematological Malignancies.
In vitro
OTX015 inhibits the binding of BRD2, BRD3, and BRD4 to AcH4 with IC50 ranging from 92 to 112 nM, and inhibits the growth of a variety of human cancer cell lines with GI50 ranging from 60 to 200 nM. OTX015 results in rapid down-regulation of c-MYC expression, and show the synergistic anti-proliferative effects in combination with ALK inhibitors in ALKpos ALCL cell lines.
In vivo
OTX015 (p.o.) significantly inhibits the growth of Ty82 BRD-NUT midline carcinoma tumors in nude mice by 79% at 100 mg/kg qd and 61% at 10 mg/kg bid, respectively.
Biochem/physiol Actions
It binds to bromodomain and extra-terminal domain (BET) proteins and inhibits their binding to the chromatin. This in turn prevents gene transcription. OTX015 has been shown to inhibit proliferation of cells in haematological malignancies.
Check Digit Verification of cas no
The CAS Registry Mumber 202590-98-5 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 2,0,2,5,9 and 0 respectively; the second part has 2 digits, 9 and 8 respectively.
Calculate Digit Verification of CAS Registry Number 202590-98:
(8*2)+(7*0)+(6*2)+(5*5)+(4*9)+(3*0)+(2*9)+(1*8)=115
115 % 10 = 5
So 202590-98-5 is a valid CAS Registry Number.
202590-98-5Relevant articles and documents
METHODS AND COMPOUNDS FOR THE TREATMENT OF GENETIC DISEASE
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, (2021/08/13)
The present disclosure relates to compounds and methods for modulating the expression of dmpk, and treating diseases and conditions in which dmpk plays an active role. The compound can be a transcription modulator molecule having a first terminus, a second terminus, and oligomeric backbone, wherein: a) the first terminus comprises a DNA-binding moiety capable of noncovalently binding to a nucleotide repeat sequence CAG or CTG; b) the second terminus comprises a protein-binding moiety binding to a regulatory molecule that modulates an expression of a gene comprising the nucleotide repeat sequence CAG or CTG; and c) the oligomeric backbone comprising a linker between the first terminus and the second terminus.
Thienotriazolodiazepine compounds and their pharmaceutical use
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, (2008/06/13)
Thienotriazolodiazepine compounds of the formula (1) STR1 wherein each symbol is as defined in the specification, pharmaceutically acceptable salts thereof, and pharmaceutical use thereof. The compounds of the present invention are useful as preventive an
