IPI-549 - CAS 1693758-51-8
Catalog number: B0084-475947
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C30H24N8O2
Molecular Weight:
528.58
COA:
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Targets:
PI3K
Description:
IPI-549, a dihydroisoquinolin derivative, has been found to be a phosphatidylinositol 3 kinase gamma inhibitor, could exhibit antineoplastic activity in solid tumors. It is still under Phase I trial. IC50: 16 nM (PI3Kγ), 3.2 μM (PI3Kα), 3.5 μM (PI3Kβ), >8.4 μM (PI3Kδ).
Ordering Information
Catalog Number Size Price Stock Quantity
B0084-475947 50 mg $239 In stock
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Purity:
98%
Appearance:
Powder
Synonyms:
IPI-549; IPI 549; IPI549; SCHEMBL16629991; (S)-2-amino-N-(1-(8-((1-methyl-1H-pyrazol-4-yl)ethynyl)-1-oxo-2-phenyl-1,2-dihydroisoquinolin-3-yl)ethyl)pyrazolo[1,5-a]pyrimidine-3-carboxamide
Storage:
Store in a cool and dry place and at 0 - 4 °C for short term (days to weeks) or -20 °C for long term (months to years).
MSDS:
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Quality Standard:
In-house standard
Quantity:
Milligram-Grams
InChIKey:
XUMALORDVCFWKV-IBGZPJMESA-N
InChI:
InChI=1S/C30H24N8O2/c1-19(34-29(39)26-27(31)35-37-15-7-14-32-28(26)37)24-16-22-9-6-8-21(13-12-20-17-33-36(2)18-20)25(22)30(40)38(24)23-10-4-3-5-11-23/h3-11,14-19H,1-2H3,(H2,31,35)(H,34,39)/t19-/m0/s1
Canonical SMILES:
CC(C1=CC2=CC=CC(=C2C(=O)N1C3=CC=CC=C3)C#CC4=CN(N=C4)C)NC(=O)C5=C6N=CC=CN6N=C5N
1.Discovery of a Selective Phosphoinositide-3-Kinase (PI3K)-γ Inhibitor (IPI-549) as an Immuno-Oncology Clinical Candidate.
Evans CA;Liu T;Lescarbeau A;Nair SJ;Grenier L;Pradeilles JA;Glenadel Q;Tibbitts T;Rowley AM;DiNitto JP;Brophy EE;O'Hearn EL;Ali JA;Winkler DG;Goldstein SI;O'Hearn P;Martin CM;Hoyt JG;Soglia JR;Cheung C;Pink MM;Proctor JL;Palombella VJ;Tremblay MR;Castro AC ACS Med Chem Lett. 2016 Jul 22;7(9):862-7. doi: 10.1021/acsmedchemlett.6b00238. eCollection 2016 Sep 8.
Optimization of isoquinolinone PI3K inhibitors led to the discovery of a potent inhibitor of PI3K-γ (26 or IPI-549) with >100-fold selectivity over other lipid and protein kinases. IPI-549 demonstrates favorable pharmacokinetic properties and robust inhibition of PI3K-γ mediated neutrophil migration in vivo and is currently in Phase 1 clinical evaluation in subjects with advanced solid tumors.
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CAS 1693758-51-8 IPI-549

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