AZD8835
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MedKoo CAT#: 206479

CAS#: 1620576-64-8

Description: 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. AZD8835, is currently in phase I clinical trials.


Chemical Structure

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AZD8835
CAS# 1620576-64-8

Theoretical Analysis

MedKoo Cat#: 206479
Name: AZD8835
CAS#: 1620576-64-8
Chemical Formula: C22H31N9O3
Exact Mass: 469.25499
Molecular Weight: 469.55
Elemental Analysis: C, 56.28; H, 6.65; N, 26.85; O, 10.22

Price and Availability

Size Price Availability Quantity
10.0mg USD 150.0 Same Day
25.0mg USD 250.0 Same Day
50.0mg USD 450.0 Same Day
100.0mg USD 750.0 Same Day
200.0mg USD 1250.0 Same Day
500.0mg USD 1950.0 Same Day
1.0g USD 2850.0 2 Weeks
2.0g USD 3850.0 2 Weeks
5.0g USD 6950.0 2 Weeks
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Synonym: AZD-8835; AZD 8835; AZD8835.

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

InChi Key: ZGRDYKFVDCFJCZ-UHFFFAOYSA-N

InChi Code: 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)

SMILES Code: O=C(N1CCC(C2=NN(CC)C(C3=NC(C4=NN=C(C(C)(C)C)O4)=C(N)N=C3)=N2)CC1)CCO

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

Preparing Stock Solutions

The following data is based on the product molecular weight 469.55 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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AZD8835

10.0mg / USD 150.0


Additional Information

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). AZD8835 is also a potent inhibitor of the commonly occurring PI3Kα mutants, PI3Kα - E545K (IC50 0.0060 μM) and PI3Kα - H1047R (IC50 0.0058 μM). In cell-based assays assessing the ability to inhibit AKT phosphorylation, AZD8835 was a potent inhibitor in cells sensitive to PI3Kα inhibition (IC50 0.057 μM in PIK3CA mutant human breast ductal carcinoma BT474 cell line) and in cells sensitive to PI3Kδ inhibition (IC50 0.049 μM in Jeko-1 B cell line), but not to cells sensitive to PI3Kβ inhibition (IC50 3.5 μM in PTEN null breast adenocarcinoma MDA-MB-468 cells) or to PI3Kγ inhibition (IC50 0.53 μM in monocytic RAW264 cell line).