Apalutamide (ARN-509)
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 |
|---|---|---|
| 500mg | $550 | In Stock |
| 1g | $950 | In Stock |
| 5g | $2565 | In Stock |
: Cat #: V1760 CAS #: 956104-40-8 Purity ≥ 98%
Description: Apalutamide (formerly JNJ56021927; ARN509; JNJ-56021927; ARN-509; trade name Erleada), an approved anticancer drug, is a potent, selective and competitive, orally bioavailable AR/androgen receptor inhibitor with an IC50 of 16 nM in a cell-free assay.
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- Related Biological Data
- Stock Solution Preparation
- Quality Control Documentation
| Molecular Weight (MW) | 477.43 |
|---|---|
| Molecular Formula | C21H15F4N5O2S |
| CAS No. | 956104-40-8 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: >20 mg/mLr |
| Water: <1 mg/mLr | |
| Ethanol: 5 mg/mL (10.5 mM) | |
| Solubility In Vivo | 0.5% CMC, pH4.0: 14 mg/mL |
| Synonyms | JNJ56021927; ARN509; JNJ-56021927; ARN 509; JNJ 56021927; ARN-509; Apalutamide; Brand name: Erleada Chemical Name: 4-(7-(6-cyano-5-(trifluoromethyl)pyridin-3-yl)-8-oxo-6-thioxo-5,7-diazaspiro[3.4]octan-5-yl)-2-fluoro-N-methylbenzamide SMILES Code: O=C(NC)C1=CC=C(N(C(N(C2=CC(C(F)(F)F)=C(C#N)N=C2)C3=O)=S)C43CCC4)C=C1F Exact Mass: 477.08826 |
| Protocol | In Vitro | Apalutamide (ARN-509) for GABA in a radioligand binding assayA The receptor also exhibits low micromolar affinity (IC50 3 μM), and therefore potentially antagonistic GABAA At inhibitor dose levels |
|---|---|---|
| In Vivo | Apalutamide (ARN-509) exhibits low systemic clearance, high oral bioavailability, and long plasma half-life in both mice and dogs, supporting once-daily oral administration. Consistent with its long terminal half-life, Apalutamide steady-state plasma levels increased in repeated dose studies, resulting in high C24hr Horizontal and low peak-to-Zig ratio (ratio: 2.5). Castrated male mice carrying LNCaP/AR xenograft tumors are treated with Apalutamide at doses of 1, 10, or 30 mg/kg/day. Thirteen of the 20 Apalutamide (30 mg/kg/day) treated animals showed a >13% reduction in tumor volume at day 28, compared with 50 of the 19 MDV3100 (30 mg/kg/day) treated mice |
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 | 2.0945 mL | 10.4727 mL | 20.9455 mL | 41.8910 mL |
| 5mM | 0.4189 mL | 2.0945 mL | 4.1891 mL | 8.3782 mL |
| 10mM | 0.2095 mL | 1.0473 mL | 2.0945 mL | 4.1891 mL |
| 20mM | 0.1047 mL | 0.5236 mL | 1.0473 mL | 2.0945 mL |
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
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Concentration
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Volume
×
Molecular Weight*
The dilution calculator equation
Concentration(start)
×
Volume(start)
=
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Volume(final)
This equation is commonly abbreviated as: C1 V1 = C2 V2
Concentration(start)
C1
×
Volume(start)
V1
=
Concentration(final)
C2
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Volume(final)
V2
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.