AST487 (NVP- AST487)
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 | $1350 | Check With Us |
| 500mg | $1980 | Check With Us |
| 1g | $2970 | Check With Us |
: Cat #: V3376 CAS #: 630124-46-8 Purity ≥ 98%
Description: AST487 (also known as NVP- AST487) is a novel and potent inhibitor of RET kinase with anticancer activity.
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- Physicochemical and Storage Information
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| Molecular Weight (MW) | 529.56 |
|---|---|
| Molecular Formula | C26H30F3N7O2 |
| CAS No. | 630124-46-8 |
| SMILES Code | O=C(NC1=CC=C(OC2=NC=NC(NC)=C2)C=C1)NC3=CC=C(CN4CCN(CC)CC4)C(C(F)(F)F)=C3 |
| Synonyms | NVP AST487; NVP AST-487; NVP AST 487; NVP-AST487; NVP-AST-487; NVP-AST 487; AST 487; AST487; AST-487 |
| Protocol | In Vitro | A number of other kinases are also similarly inhibited by AST 487 (NVP-AST487) in the in vitro kinase assays, including KDR (IC50=170 nM), Flt-4 (IC50=790 nM), Flt-3 (IC50=520 nM), c-Kit (IC50=500 nM), and c-Abl (IC50=20 nM). AST 487 potently inhibits the growth of human thyroid cancer cell lines with activating mutations of RET but not of lines without RET mutations. Both GDNF/GFRα1 and persephin-induced calcitonin mRNA are markedly inhibited by coincubation with 100 nM of AST 487 in MTC-M cells. |
|---|---|---|
| In Vivo | After a single oral administration of 15 mg/kg of AST 487 to OF1 mice, a mean peak plasma level (Cmax) of 0.505±0.078 μM SE is achieved after 0.5 h. Similar levels of AST 487 are found in the plasma of mice up to 6 h after oral administration, with a Clast of 21±4 nM at 24 h. The oral bioavailability is calculated to be 9.7% with a t1/2 terminal elimination of 1.5 h. |
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 | 1.8884 mL | 9.4418 mL | 18.8836 mL | 37.7672 mL |
| 5mM | 0.3777 mL | 1.8884 mL | 3.7767 mL | 7.5534 mL |
| 10mM | 0.1888 mL | 0.9442 mL | 1.8884 mL | 3.7767 mL |
| 20mM | 0.0944 mL | 0.4721 mL | 0.9442 mL | 1.8884 mL |
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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
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%
+
%Tween 80
+
%ddH2O
Calculation Results:
Working concentration:
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Method for preparing DMSO master liquid:
mg
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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.