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AZD-8835

Catalog No.: 102703
Cas No.: 1620576-64-8
Purity : ≧98.0%

AZD8835 is a potent and selective inhibitor of PI3Kalpha and PI3Kdelata with excellent general kinase selectivity. AZD8835 displayed low metabolic turnover and suitable physical properties for oral administration. At the enzyme level, AZD8835 is a potent mixed inhibitor of PI3Kα (IC50 0.0062 μM) and PI3Kδ (IC50 0.0057 μM), with selectivity against PI3Kβ (IC50 0.431 μM) and PI3Kγ (IC50 0.090 μM). In vivo, AZD8835 showed pharmacodynamic modulation of AKT phosphorylation and near complete inhibition of tumour growth (93% tumour growth inhibition) in a murine H1047R PI3Kalpha mutated SKOV-3 xenograft tumour model after chronic oral administration at 25 mg/kg b.i.d. 

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Chemical Information

NameAZD-8835
Iupac Chemical Name1-(4-(5-(5-amino-6-(5-(tert-butyl)-1,3,4-oxadiazol-2-yl)pyrazin-2-yl)-1-ethyl-1H-1,2,4-triazol-3-yl)piperidin-1-yl)-3-hydroxypropan-1-one 
SynonymsAZD 8835 ; AZD8835 
Molecular FormulaC22H31N9O3 
Molecular Weight469.55 
SmileO=C(N1CCC(C2=NN(CC)C(C3=NC(C4=NN=C(C(C)(C)C)O4)=C(N)N=C3)=N2)CC1)CCO
InChiKeyZGRDYKFVDCFJCZ-UHFFFAOYSA-N
InChiInChI=1S/C22H31N9O3/c1-5-31-19(26-18(29-31)13-6-9-30(10-7-13)15(33)8-11-32)14-12-24-17(23)16(25-14)20-27-28-21(34-20)22(2,3)4/h12-13,32H,5-11H2,1-4H3,(H2,23,24)
CAS Number1620576-64-8
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Formulationoff-white to light yellow solid 
Purity≧98.0%
Storage3 years -20ºCpowder 6 months-80ºCin solvent 
SolubilitySoluble in DMSO 
Handling
Shipping ConditionShipped under ambient temperature 
HS Code
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Targets
Mechanism
Cell study
Animal study
Clinical study
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Chemical Structure

102703 - AZD-8835 | CAS 1620576-64-8

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