TAK-733
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 | $1160 | Check With Us |
| 500mg | $1750 | Check With Us |
| 1g | $2625 | Check With Us |
: Cat #: V0459 CAS #: 1035555-63-5 Purity ≥ 98%
Description: TAK-733 is a novel, potent, selective and orally bioavailable allosteric (non-ATP competitive) inhibitor of MEK with potential anticancer activity.
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- Physicochemical and Storage Information
- Protocol
- Related Biological Data
- Stock Solution Preparation
- Quality Control Documentation
| Molecular Weight (MW) | 504.23 |
|---|---|
| Molecular Formula | C17H15F2IN4O4 |
| CAS No. | 1035555-63-5 |
| Storage | -20℃ for 3 years in powder formrrr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 101 mg/mL (200.3 mM)rrr |
| Water: <1 mg/mLrrr | |
| Ethanol: <1 mg/mL | |
| SMILES Code | O=C1C(C(NC2=CC=C(I)C=C2F)=C(F)C(N3C)=O)=C3N=CN1C[C@@H](O)CO |
| Synonyms | TAK 733; TAK733; TAK-733 |
| Protocol | In Vitro | TAK-733 exhibits potent enzymatic and cell activity with an IC50 of 3.2 nM against constitutively active MEK enzyme and an EC50 of 1.9 nM against ERK phosphorylation in cells. TAK-733 does not inhibit any other kinases, receptors or ion channels that are tested with inhibitor concentrations up to 10 μM. TAK-733 is found to bind plasma protein moderately (ca. 97% for human and 96% for mouse), and exhibits high permeability and high microsomal stability across species. It does not inhibit P450s up to 30 μM. |
|---|---|---|
| In Vivo | The pharmacokinetics of TAK-733 is evaluated in nude mouse, rat, dog and monkey. Low clearance and high oral bioavailability are observed in all species. TAK-733 demonstrates broad antitumor activity in mouse xenograft models of human cancer including models of melanoma, colorectal, NSCLC, pancreatic and breast cancer. |
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 | 1.9832 mL | 9.9161 mL | 19.8322 mL | 39.6644 mL |
| 5mM | 0.3966 mL | 1.9832 mL | 3.9664 mL | 7.9329 mL |
| 10mM | 0.1983 mL | 0.9916 mL | 1.9832 mL | 3.9664 mL |
| 20mM | 0.0992 mL | 0.4958 mL | 0.9916 mL | 1.9832 mL |
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
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Volume
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Molecular Weight*
The dilution calculator equation
Concentration(start)
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Volume(start)
=
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Volume(final)
This equation is commonly abbreviated as: C1 V1 = C2 V2
Concentration(start)
C1
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V1
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C2
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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.