Description
I-BET282E is a pan-inhibitor of all eight BET bromodomains, and selectivity over other representative bromodomain-containing proteins. I-BET282E shows pIC50s ranging 6.4-7.7 for BRD2 (BD1/BD2), BRD2 (BD1/BD), BRD3 (BD1/BD), and BRD4 (BD1/BD).
Product information
CAS Number: 2885162-99-0
Molecular Weight: 546.64
Formula: C26H34N4O7S
Chemical Name: 4-{8-methoxy-1-[(2R)-1-methoxypropan-2-yl]-2-(oxan-4-yl)-1H-imidazo[4,5-c]quinolin-7-yl}-3,5-dimethyl-1,2-oxazole; methanesulfonic acid
Smiles: C[C@H](COC)N1C2C(=CN=C3C=C(C(=CC3=2)OC)C2C(C)=NOC=2C)N=C1C1CCOCC1.CS(O)(=O)=O
InChiKey: RNDJPURPXAOCHW-PFEQFJNWSA-N
InChi: InChI=1S/C25H30N4O4.CH4O3S/c1-14(13-30-4)29-24-18-11-22(31-5)19(23-15(2)28-33-16(23)3)10-20(18)26-12-21(24)27-25(29)17-6-8-32-9-7-17;1-5(2,3)4/h10-12,14,17H,6-9,13H2,1-5H3;1H3,(H,2,3,4)/t14-;/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 Vitro:
I-BET282E has a weak inhibition of the hERG potassium ion channel (pIC50 4.4-5.1 in a variety of assay formats). I-BET282E shows a low potential to inhibit CYP proteins in vitro, with no evidence of time-dependent inhibition of 2D6 or 3A4.
In Vivo:
I-BET282E (Male CD1 Mice; 3 mg/kg-p.o.; 1 mg/kg-i.v.) treatment shows the Clb, LBF, Vss, t1/2 (i.v.), and F values of 23 mL/min/kg, 19%, 1.9 L/kg, and 51%, respectively. I-BET282E (Male Wistar Han Rats; 1 mg/kg; p.o.) treatment shows the AUC0-t, Cmax and Tmax values of 467 ng h/mL, 125 ng/mL, and 1 hour, respectively.
Products are for research use only. Not for human use.
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