Description
PI3kδ inhibitor 1 is a selective inhibitor of PI3Kδ (IC50 of 3.8 nM).
Product information
CAS Number: 1332075-63-4
Molecular Weight: 504.60
Formula: C28H33FN6O2
Synonym:
2-[1-[[2-(5-Fluoro-1H-indol-4-yl)-4-(morpholin-4-yl)pyrido[3,2-d]pyrimidin-6-yl]methyl]piperidin-4-yl]propan-2-ol
Chemical Name: 2-(1-{[2-(5-fluoro-1H-indol-4-yl)-4-(morpholin-4-yl)pyrido[3,2-d]pyrimidin-6-yl]methyl}piperidin-4-yl)propan-2-ol
Smiles: CC(C)(O)C1CCN(CC2=CC=C3N=C(N=C(C3=N2)N2CCOCC2)C2C(F)=CC=C3NC=CC3=2)CC1
InChiKey: ONEJEIKQLAZPNN-UHFFFAOYSA-N
InChi: InChI=1S/C28H33FN6O2/c1-28(2,36)18-8-11-34(12-9-18)17-19-3-5-23-25(31-19)27(35-13-15-37-16-14-35)33-26(32-23)24-20-7-10-30-22(20)6-4-21(24)29/h3-7,10,18,30,36H,8-9,11-17H2,1-2H3
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: Soluble in DMSO
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:
Mice and Rats[1]Female mice are dosed IV (intravenously) with PI3kδ inhibitor 1 in 5% DMSO/5% Cremephor and PO (orally) as an MCT suspension (0.5% methylcellulose/0.2% Tween-80). The IV (1 mg/kg) and PO (5, 20 and 40 mg/kg) studies are performed in CD-1 mice while the higher dose studies are performed in the Balb/c strain. Male Sprague-Dawley rats are dosed with the same IV (1 mg/kg) and PO (5, 10 and 30 mg/kg) formulations as those used for mice.
References:
- Sutherlin DP, et al. Potent and selective inhibitors of PI3Kδ: obtaining isoform selectivity from the affinity pocket and tryptophan shelf. Bioorg Med Chem Lett. 2012 Jul 1;22(13):4296-302.
Products are for research use only. Not for human use.
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