AZD9496 maleate
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 | $1400 | Check With Us |
| 500mg | $2020 | Check With Us |
| 1g | $3030 | Check With Us |
: Cat #: V2643 CAS #: 1639042-28-6 Purity ≥ 98%
Description: AZD9496 (AZD-9496) maleate is a novel, potent, orally bioavailable, and selective estrogen receptor (ERα) downregulator and antagonist with anticancer activity.
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- Physicochemical and Storage Information
- Protocol
- Related Biological Data
- Stock Solution Preparation
- Quality Control Documentation
| Molecular Weight (MW) | 558.55 |
|---|---|
| Molecular Formula | C29H29F3N2O6 |
| CAS No. | 1639042-28-6 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 10 mMr |
| Water: N/Ar | |
| Ethanol: N/A | |
| SMILES Code | O=C(O)/C=C/C1=CC(F)=C([C@H]2N(CC(C)(F)C)[C@H](C)CC3=C2NC4=C3C=CC=C4)C(F)=C1.O=C(O)/C=CC(O)=O |
| Synonyms | AZD-9496 maleate; AZD9496; AZD 9496 maleate |
| Protocol | In Vitro | The potency of AZD9496 with IC50 of 0.82 nM, 0.14 nM, and 0.28 nM in ERα binding, downregulation, and antagonism, respectively. AZD9496 significantly inhibits MCF-7 cell growth with EC50 of 0.04 nM. |
|---|---|---|
| In Vivo | Significant tumor growth inhibition is observed as low as 0.5 mg/kg dose in the estrogen-dependent MCF-7 xenograft model, where this effect is accompanied by a dose-dependent decrease in PR protein levels, demonstrating potent antagonist activity. Combining AZD9496 with PI3K pathway and CDK4/6 inhibitors lead to further growth-inhibitory effects compared with monotherapy alone. AZD9496, given once daily orally at 5 and 25 mg/kg produced statistically significant increases in uterine weight compared with the ICI 182780 control (P<0.001) but significantly lower than ICI 47699 (P=0.001). |
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 | 1.7904 mL | 8.9518 mL | 17.9035 mL | 35.8070 mL |
| 5mM | 0.3581 mL | 1.7904 mL | 3.5807 mL | 7.1614 mL |
| 10mM | 0.1790 mL | 0.8952 mL | 1.7904 mL | 3.5807 mL |
| 20mM | 0.0895 mL | 0.4476 mL | 0.8952 mL | 1.7904 mL |
The molarity calculator equation
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The dilution calculator equation
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Step One: Enter information below
Dosage mg/kg
Average weight of animals g
Dosing volume per animal µL
Number of animals
Step Two: Enter the in vivo formulation
%DMSO
+
%
+
%Tween 80
+
%ddH2O
Calculation Results:
Working concentration:
mg/ml;
Method for preparing DMSO master liquid:
mg
drug pre-dissolved in
µL
DMSO(Master liquid concentration
mg/mL)
,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.