Products

Enzymes for Research, Diagnostic and Industrial Use

Products
Online Inquiry

Our Products Cannot Be Used As Medicines Directly For Personal Use.

24 hour
Promise

Welcome! For price inquiries, please feel free to contact us through the form on the left side. We will get back to you as soon as possible.

TAK-733

Cat No.
CEI-0146
Description
As a novel allosteric, non-ATP-binding inhibitor, TAK-733 can potently and selectively inhibit MEK1/2 with IC50 of 3.2 nM.
CAS No.
1035555-63-5
Molecular Weight
504.23
Purity
>99%
Storage
2 years at -20 centigrade
Targets
MEK1/2
Molecular Formula
C17H15F2IN4O4
Chemical Name
(R)-3-(2,3-dihydroxypropyl)-6-fluoro-5-(2-fluoro-4-iodophenylamino)-8-methylpyrido[2,3-d]pyrimidine-4,7(3H,8H)-dione
Solubility
DSMO 101 mg/mL Water
In vitro
As a novel allosteric, non-ATP-binding inhibitor, TAK-733 can potently and selectively inhibit MEK1/2 with IC50 of 3.2 nM. TAK-733 belongs to 5-phenylamino-8-methylpyrido[2,3-d]pyrimidine-4,7(3H,8H)-dione series compound.[1] TAK733 shows strong inhibition to uveal melanoma cell lines with IC50 around 10 nM. Some uveal melanoma cell line is sensitive to TAK733, with IC50 less than 1 nM. TAK733 can induce cell cycle arrest. For both TAK733-sensitive( M207) and TAK733-highly resistant cell line, TAK733,with increasing concentrations, can induce a dose-dependent G1 arrest. TAK733 can induce G1 arrest in melanoma cell lines regardless of their origin, driver oncogenic mutations and in vitro sensitivity to TAK733. TAK733 also can induce a marked dose-dependent decrease of pERK, regardless of the driver oncogenic mutation or the sensitivity or resistance.
In vivo
TAK-733 shows potent inhibition to mouse xenograft models of human cancer, such as melanoma, colorectal, NSCLC, pancreatic and breast cancer.

Our Products Cannot Be Used As Medicines Directly For Personal Use.

0
Click unfold / close
Inquiry Basket
Delete selected Quote Check Out
Decide to move out of the shopping cart?
Sure No, Back

Please choose product!

< Go Back
You have already added to buy this product