TAK-632
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 | $630 | Check With Us |
| 500mg | $999 | Check With Us |
| 1g | $1498 | Check With Us |
: Cat #: V1012 CAS #: 1228591-30-7 Purity ≥ 98%
Description: TAK-632 (TAK 632; TAK632) is a novel and potent pan-Raf inhibitor with potential antineoplastic activity.
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| Molecular Weight (MW) | 554.52 |
|---|---|
| Molecular Formula | C27H18F4N4O3S |
| CAS No. | 1228591-30-7 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 100 mg/mL (180.3 mM)r |
| Water: <1 mg/mLr | |
| Ethanol: 2 mg/mL (3.6 mM) | |
| Solubility In Vivo | 2% DMSO+98% PEG 300: 5 mg/mL |
| SMILES Code | O=C(C1CC1)NC(S2)=NC3=C2C(C#N)=C(OC4=CC(NC(CC5=CC=CC(C(F)(F)F)=C5)=O)=C(F)C=C4)C=C3 |
| Synonyms | TAK632, TAK 632, TAK-632; |
| Protocol | In Vitro | TAK-632 inhibits PDGFRβ, FGFR3, GSK3β, CDK2, P38α, PDGFRα, TIE2, and CDK1 with a range of IC50 values from 120-790 nM. CHK1, IKKβ, and MEK1 are inhibited over an IC50 range of 1400-1700 nM. With 1 h of preincubation time, TAK-632 inhibits BRAF and CRAF in an ATP competitive manner (at low ATP concentrations BRAF IC50: 15 nM; CRAF: 8.1 nM). The respective biochemical activity of TAK-632 against BRAF and CRAF reduces to IC50 values of 58 nM and 62 nM at high ATP concentrations.TAK-632 demonstrates strong inhibition of pMEK and pERK in HMVII cells with IC50 values of 49 nM and 50 nM, respectively. |
|---|---|---|
| In Vivo | TAK-632 demonstrates dramatically improved solubility (740 μg/mL) in pH 6.8 phosphate buffer and exhibits significant oral absorption (at a dose of 25 mg/kg, AUC, 32.47 μg h/mL; F, 51.7%) in rats. In a dog PK study, 10 mg/kg administration of TAK-632 also shows superior oral bioavailability (F: 108%).Oral single administration of TAK-632 inhibits pERK in tumors at 8 h after its administration over a dose range of 1.9-24.1 mg/kg. In particular, 9.7-24.1 mg/kg dosing with TAK-632 strongly inhibits pERK levels to 11% of the control. TAK-632 exhibits dose-dependent antitumor efficacy without severe body weight reduction over a dose range of 3.9-24.1 mg/kg. Significant tumor regression is observed at 9.7 mg/kg and 24.1 mg/kg (T/C=−2.1% and −12.1%, respectively). |
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 | 1.8034 mL | 9.0168 mL | 18.0336 mL | 36.0672 mL |
| 5mM | 0.3607 mL | 1.8034 mL | 3.6067 mL | 7.2134 mL |
| 10mM | 0.1803 mL | 0.9017 mL | 1.8034 mL | 3.6067 mL |
| 20mM | 0.0902 mL | 0.4508 mL | 0.9017 mL | 1.8034 mL |
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Step One: Enter information below
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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
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µL
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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.