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.
AZD-8835, Bulk in stock, contact us by email for Bulk quotation.
For research use only. We do not sell to patients.
Name | AZD-8835 |
---|---|
Iupac Chemical Name | 1-(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 |
Synonyms | AZD 8835 ; AZD8835 |
Molecular Formula | C22H31N9O3 |
Molecular Weight | 469.55 |
Smile | O=C(N1CCC(C2=NN(CC)C(C3=NC(C4=NN=C(C(C)(C)C)O4)=C(N)N=C3)=N2)CC1)CCO |
InChiKey | ZGRDYKFVDCFJCZ-UHFFFAOYSA-N |
InChi | InChI=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 Number | 1620576-64-8 |
Related CAS |
Packaging | Price | Availability | Purity | Shipping Time |
---|---|---|---|---|
Bulk | Enquiry | Enquiry | Enquiry |
Formulation | off-white to light yellow solid |
---|---|
Purity | ≧98.0% |
Storage | 3 years -20ºCpowder 6 months-80ºCin solvent |
Solubility | Soluble in DMSO |
Handling | |
Shipping Condition | Shipped under ambient temperature |
HS Code |
Targets | |
---|---|
Mechanism | |
Cell study | |
Animal study | |
Clinical study |