MedKoo Cat#: 208412 | Name: Trotabresib
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Trotabresib, also known as CC-90010 and BMS-986378, is a novel, oral, reversible, small-molecule BET inhibitor. Trotabresib binds to the bromodomains of BET proteins (BRD2, BRD3, BRD4, and BRDT), disrupting their interaction with acetylated histones. This inhibition leads to suppression of oncogene transcription, particularly affecting MYC, BCL-2, and other genes involved in tumor progression.Trotabresib has shown potent antiproliferative effects in multiple cancer models, including hematologic malignancies and solid tumors. Preclinical and clinical studies indicate activity in glioblastoma, non-Hodgkin’s lymphoma, and other aggressive tumors. Inhibition of BRD4 by Trotabresib can lead to apoptosis and cell cycle arrest in tumor cells.

Chemical Structure

Trotabresib
Trotabresib
CAS# 1706738-98-8

Theoretical Analysis

MedKoo Cat#: 208412

Name: Trotabresib

CAS#: 1706738-98-8

Chemical Formula: C21H21NO4S

Exact Mass: 383.1191

Molecular Weight: 383.46

Elemental Analysis: C, 65.78; H, 5.52; N, 3.65; O, 16.69; S, 8.36

Price and Availability

Size Price Availability Quantity
5mg USD 350.00 2 Weeks
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Related CAS #
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Synonym
Trotabresib; CC-90010; CC 90010; CC90010; BMS-986378; BMS986378; BMS 986378;
IUPAC/Chemical Name
4-[2-(Cyclopropylmethoxy)-5-methylsulfonylphenyl]-2-methylisoquinolin-1-one
InChi Key
UWZAJPITKGWMFJ-UHFFFAOYSA-N
InChi Code
InChI=1S/C21H21NO4S/c1-22-12-19(16-5-3-4-6-17(16)21(22)23)18-11-15(27(2,24)25)9-10-20(18)26-13-14-7-8-14/h3-6,9-12,14H,7-8,13H2,1-2H3
SMILES Code
O=C1N(C)C=C(C2=CC(S(=O)(C)=O)=CC=C2OCC3CC3)C4=C1C=CC=C4
Appearance
To be determined
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
To be determined
Shelf Life
>2 years if stored properly
Drug Formulation
To be determined
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 383.46 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Moreno V, Sepulveda JM, Vieito M, Hernández-Guerrero T, Doger B, Saavedra O, Ferrero O, Sarmiento R, Arias M, De Alvaro J, Di Martino J, Zuraek M, Sanchez-Pérez T, Aronchik I, Filvaroff EH, Lamba M, Hanna B, Nikolova Z, Braña I. Phase I study of CC-90010, a reversible, oral BET inhibitor in patients with advanced solid tumors and relapsed/refractory non-Hodgkin's lymphoma. Ann Oncol. 2020 Jun;31(6):780-788. doi: 10.1016/j.annonc.2020.03.294. Epub 2020 Mar 30. PMID: 32240793. Sun Y, Han J, Wang Z, Li X, Sun Y, Hu Z. Safety and Efficacy of Bromodomain and Extra-Terminal Inhibitors for the Treatment of Hematological Malignancies and Solid Tumors: A Systematic Study of Clinical Trials. Front Pharmacol. 2021 Jan 26;11:621093. doi: 10.3389/fphar.2020.621093. PMID: 33574760; PMCID: PMC7870522. Pearson AD, DuBois SG, Buenger V, Kieran M, Stegmaier K, Bandopadhayay P, Bennett K, Bourdeaut F, Brown PA, Chesler L, Clymer J, Fox E, French CA, Germovsek E, Giles FJ, Bender JG, Hattersley MM, Ludwinski D, Luptakova K, Maris J, McDonough J, Nikolova Z, Smith M, Tsiatis AC, Vibhakar R, Weiner S, Yi JS, Zheng F, Vassal G. Bromodomain and extra-terminal inhibitors-A consensus prioritisation after the Paediatric Strategy Forum for medicinal product development of epigenetic modifiers in children-ACCELERATE. Eur J Cancer. 2021 Mar;146:115-124. doi: 10.1016/j.ejca.2021.01.018. Epub 2021 Feb 16. PMID: 33601323.