AZD8835
This product is for research use only, not for human use. We do not sell to patients.
For small sizes, please check our retail website as below: www.invivochem.com
| Size | Price | Stock |
|---|---|---|
| 250mg | $1150 | Check With Us |
| 500mg | $1750 | Check With Us |
| 1g | $2625 | Check With Us |
: Cat #: V2544 CAS #: 1620576-64-8 Purity ≥ 98%
Description: AZD8835 is a novel, selective, and orally bioavailable inhibitor of the class I (PI3K) catalytic subunit alpha (PIK3CA) PI3Kα and PI3Kδ with IC50s of 6.2 and 5.7 nM, respectively with potential antineoplastic activity.
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| Molecular Weight (MW) | 469.54 |
|---|---|
| Molecular Formula | C22H31N9O3 |
| CAS No. | 1620576-64-8 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 93 mg/mL (198.1 mM) r |
| Water: <1 mg/mLr | |
| Ethanol: <1 mg/ | |
| 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 |
| Synonyms | AZD-8835; AZD 8835; AZD8835 |
| Protocol | In Vitro | The selectivity profile of AZD8835 (Compound 25) among the class I PI3K isoforms is tested in enzyme and cell based assays. At the enzyme level, AZD8835 is a potent mixed inhibitor of PI3Kα (IC50 6.2 nM) and PI3Kδ (IC50 5.7 nM), with selectivity against PI3Kβ (IC50 431 nM) and PI3Kγ (IC50 90 nM). AZD8835 is also a potent inhibitor of the commonly occurring PI3Kα mutants, PI3Kα- E545K (IC50 6 nM) and PI3Kα-H1047R (IC50 5.8 nM). In cell-based assays assessing the ability to inhibit Akt phosphorylation, AZD8835 is a potent inhibitor in cells sensitive to PI3Kα inhibition (IC50 57 nM in PIK3CA mutant human breast ductal carcinoma BT474 cell line) and in cells sensitive to PI3Kδ inhibition (IC50 49 nM 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 530 nM in monocytic RAW264 cell line) |
|---|---|---|
| In Vivo | AZD8835 (Compound 25) displays good solubility, good permeability and low turnover in hepatocytes from various species. As expected from the in vitro data, low in vivo clearance associated with high bioavailability is seen in both rat and dog. AZD8835 shows high exposure following oral administration to SCID mice (AUC: 137 μM.h and Cmax 34 μM at 50 mg/kg p.o.) and is selected for further in vivo evaluation. In a pharmacodynamic experiment following chronic oral dosing (25 mg/kg b.i.d. or 6 mg/kg b.i.d. of AZD8835) in nude mice bearing mutant H1047R PI3Kα SKOV-3 tumour xenografts, target modulation is assessed by measuring Akt phosphorylation levels at Ser473 at 30 minutes and 8 hours. At both doses, strong inhibition of Akt phosphorylation is observed at the 30 minute timepoint. At 8 hours, significant inhibition is still seen at the 25 mg/kg dose, whereas no inhibition is seen at the lower dose of 6 mg/kg, consistent with the lower plasma concentrations observed. |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 2.1297 mL | 10.6487 mL | 21.2974 mL | 42.5949 mL |
| 5mM | 0.4259 mL | 2.1297 mL | 4.2595 mL | 8.5190 mL |
| 10mM | 0.2130 mL | 1.0649 mL | 2.1297 mL | 4.2595 mL |
| 20mM | 0.1065 mL | 0.5324 mL | 1.0649 mL | 2.1297 mL |
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Step Two: Enter the in vivo formulation
%DMSO
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%Tween 80
+
%ddH2O
Calculation Results:
Working concentration:
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Method for preparing DMSO master liquid:
mg
drug pre-dissolved in
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,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:
Take
µL
DMSO master liquid, next add
µL
PEG300, mix and clarify, next add
µL
Tween 80,mix and clarify, next add
µL
ddH2O,mix and clarify.
Note:
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
- (2) Be sure to add the solvent(s) in order.