GSK040 is a potent and highly selective BET BD2 inhibitor, with a pIC50 of 8.3. GSK040 shows more than 5000-fold selectivity for BET BD2 over BET BD1 (pIC50=4.6). GSK040 can be used for the research of oncology and immunology diseases.

Product information

Molecular Weight: 502.60

Formula: C29H34N4O4

Chemical Name: 1, 5-dimethyl-N-(2-(methylamino)-2-oxo-1-(tetrahydro-2H-pyran-4-yl)ethyl)-6-oxo-N-((S)-2-phenyl-2-(pyridin-2-yl)ethyl)-1, 6-dihydropyridine-3-carboxamide

Smiles: CN1C=C(C=C(C)C1=O)C(=O)N(C[C@@H](C1=CC=CC=N1)C1C=CC=CC=1)C(C1CCOCC1)C(=O)NC

InChiKey: MDCZQITXTAMNNV-RMVMEJTISA-N

InChi: InChI=1S/C29H34N4O4/c1-20-17-23(18-32(3)28(20)35)29(36)33(26(27(34)30-2)22-12-15-37-16-13-22)19-24(21-9-5-4-6-10-21)25-11-7-8-14-31-25/h4-11,14,17-18,22,24,26H,12-13,15-16,19H2,1-3H3,(H,30,34)/t24-,26?/m1/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vivo:

GSK040 (1 mg/kg; i.v.) exhibits t1/2 (0.19 h), CLb (50 mL/min/kg) and Vss (0.6 L/kg) in rats. GSK040 (3 mg/kg; p.o.) exhibits oral bioavailability (16%), tmax (0.25 h), Cmax (398 nM) in rats.

Products are for research use only. Not for human use.