TAK-733 Inhibitor CAS No. 1035555-63-5

Cat. No.	Name	Size	Price
KI0608	TAK-733	5 mg	$272
	TAK-733	10 mg	$512
	TAK-733	50 mg	$1552
	TAK-733	200 mg	$3952

Chemical Characteristic

Product Name	TAK-733
CAS No.	1035555-63-5
Molecular Weight	504.23
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
Smiles	(R)-3-(2,3-dihydroxypropyl)-6-fluoro-5-(2-fluoro-4-iodophenylamino)-8-methylpyrido[2,3-d]pyrimidine-4,7(3H,8H)-dione
Chemical Structure
Documents	HPLC MS COA

Biological activities

TAK-733 is a potent and selective MEK inhibitor. The IC50 of TAK-733 against MEK is 3.2 nM. TAK-733 is a non ATP-competitive inhibitor. In vitro, TAK-733 has significant enzymatic and cell activity with an EC50 of 1.9 nM against ERK phosphorylation.^[1] Furthermore, cells harboring BRAF(L597R) mutants are sensitive to TAK-733 treatment.^[2] In experimental human solid tumor xenograft models including NSCLC (NCI H23), CRC (SW620), and pancreatic cancer (Panc 1, Capan 1, and BxPC-3 ) models in immunocompromised mice, TAK-733 treatment (10 mg/kg) shows antitumor activity. Treatment with TAK-733 alone and in combination with alisertib also clearly inhibits phosphorylated ERK and produces a slight increase in phosphorylated histone H_3.^[3]

Protocols

In vitro: TAK-733 is dissolved in DMSO.^[4]

References

[1] Dong Q, et al. Discovery of TAK-733, a potent and selective MEK allosteric site inhibitor for the treatment of cancer. Bioorg Med Chem Lett. 2011, 21(5): 1315-1319. [2] Dahlman KB, et al. BRAF(L597) mutations in melanoma are associated with sensitivity to MEK inhibitors. Cancer Discov. 2012, 2(9): 791-797. [3] Robyn Fabrey, et al. Abstract 3739: TAK-733, an investigational, selective MEK1/2 inhibitor, in combination with alisertib (MLN8237), an investigational, selective Aurora A kinase inhibitor is tolerated and results in additive to synergistic antitumor activity: Results from In Vivo Studies. Proceedings: AACR 103rd Annual Meeting 2012. [4] von Euw E, et al. Antitumor effects of the investigational selective MEK inhibitor TAK733 against cutaneous and uveal melanoma cell lines. Mol Cancer. 2012, 11:22.

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