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AZD8835

Chemical Structure : AZD8835

CAS No.: 1620576-64-8

AZD8835 (AZD-8835)

Catalog No.: PC-43269Not For Human Use, Lab Use Only.

AZD8835 (AZD-8835) is a potent, selective inhibitor of PI3Kα and PI3Kδ with IC50 of 6.2 and 5.7 nM, 15-fold and >100-fold selectivity over PI3Kγ and PI3Kβ.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

AZD8835 (AZD-8835) is a potent, selective inhibitor of PI3Kα and PI3Kδ with IC50 of 6.2 and 5.7 nM, 15-fold and >100-fold selectivity over PI3Kγ and PI3Kβ.
AZD8835 also potently inhibits PI3Kα mutants E545K and H1047R with IC50 of 6 nM.
AZD8835 preferentially inhibits growth in cells with mutant PIK3CA status inhibits AKT phosphorylation with IC50 of 58 nM in PIK3CA mutant human breast ductal carcinoma BT474 cell line.
AZD8835 suppresses tumour growth (93% tumour growth inhibition) in murine H1047R PI3Kα mutated SKOV-3 xenograft tumour model (25mg/kg b.i.d).

Physicochemical Properties

M.Wt 469.54
Formula C22H31N9O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: 16 mg/mL

Chemical Name/SMILES

1-Propanone, 1-[4-[5-[5-amino-6-[5-(1,1-dimethylethyl)-1,3,4-oxadiazol-2-yl]-2-pyrazinyl]-1-ethyl-1H-1,2,4-triazol-3-yl]-1-piperidinyl]-3-hydroxy-

References

1. Barlaam B, et al. Bioorg Med Chem Lett. 2015 Nov 15;25(22):5155-62.

2. Hudson K, et al. Mol Cancer Ther. 2016 May;15(5):877-89.

3. Lynch JT, et al. Oncotarget. 2016 Apr 19;7(16):22128-39.

4. Maynard J, et al. PLoS One. 2017 Aug 14;12(8):e0183048.

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