TAK-733
- CAS NO.:1035555-63-5
- Empirical Formula: C17H15F2IN4O4
- Molecular Weight: 504.23
- MDL number: MFCD24386349
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-07-02 08:55:08
What is TAK-733?
What are the applications of Application
TAK-733 is a highly potent allosteric inhibitor of MEK
Biological Activity
tak-733 is a potent, atp-noncompetitive and selective inhibitor of mek allosteric site with the ic50 value of 3.2nm [1].tak-733 has been shown potent enzymatic and cell activity with an ic50 value of 3.2nm against constitutively active mek enzyme and an ec50 of 1.9nm against erk phosphorylation in cells. in addition, tak-733 has also shown the low clearance and high oral bioavailability based on the pharmacokinetics of tak-733 in all species (mouse, rat, dog and monkey). furthermore, tak-733 has been reported to broad inhibit tumor activity in mouse xenograft models of human cancer (melanoma, colorectal, nsclc, pancreatic and breast cancer) [1].
References
[1] dong q1, dougan dr, gong x, halkowycz p, jin b, kanouni t, o'connell sm, scorah n, shi l, wallace mb, zhou f. discovery of tak-733, a potent and selective mek allosteric site inhibitor for the treatment of cancer. bioorg med chem lett. 2011 mar 1;21(5):1315-9. doi: 10.1016/j.bmcl.2011.01.071. epub 2011 jan 22.
Properties of TAK-733
Boiling point: | 530.5±60.0 °C(Predicted) |
Density | 1.91±0.1 g/cm3(Predicted) |
storage temp. | Store at -20°C |
solubility | ≥25.2 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O |
form | solid |
pka | 13.72±0.20(Predicted) |
color | White to light yellow |
Safety information for TAK-733
Signal word | Warning |
Pictogram(s) |
Exclamation Mark Irritant GHS07 |
GHS Hazard Statements |
H302:Acute toxicity,oral H315:Skin corrosion/irritation H319:Serious eye damage/eye irritation H335:Specific target organ toxicity, single exposure;Respiratory tract irritation |
Precautionary Statement Codes |
P261:Avoid breathing dust/fume/gas/mist/vapours/spray. P280:Wear protective gloves/protective clothing/eye protection/face protection. P301+P312:IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell. P302+P352:IF ON SKIN: wash with plenty of soap and water. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing. |
Computed Descriptors for TAK-733
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