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TAK-733_Molecular_structure_CAS_1035555-63-5)
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TAK-733

Catalog No. S2617 Name Selleck Chemicals
CAS Number 1035555-63-5 Website http://www.selleckchem.com
M. F. C17H15F2IN4O4 Telephone (877) 796-6397
M. W. 504.2266764 Fax (832) 582-8590
Purity Email sales@selleckchem.com
Storage -20°C Chembase ID: 73117

SYNONYMS

IUPAC name
3-[(2R)-2,3-dihydroxypropyl]-6-fluoro-5-[(2-fluoro-4-iodophenyl)amino]-8-methyl-3H,4H,7H,8H-pyrido[2,3-d]pyrimidine-4,7-dione
IUPAC Traditional name
3-[(2R)-2,3-dihydroxypropyl]-6-fluoro-5-[(2-fluoro-4-iodophenyl)amino]-8-methylpyrido[2,3-d]pyrimidine-4,7-dione
Synonyms
TAK733

DATABASE IDS

CAS Number 1035555-63-5

PROPERTIES

Target MEK
Salt Data Free Base
Storage Condition -20°C

DETAILS

Description (English)
Research Area
Description Solid tumours
Biological Activity
Description TAK-733 is a potent, selective, non ATP-competitive MEK inhibitor with IC50 of 3.2 nM.
Targets MEK1/2
IC50 3.2 nM [1]
In Vitro TAK-733 is highly potent and selective MEK allosteric site inhibitor with IC50 of 3.2 nM. TAK-733 shows potent enzymatic and cell activity with an EC50 of 1.9 nM against ERK phosphorylation in cells. [1]
In Vivo TAK-733 demonstrates broad antitumor activity in mouse xenograft models of human cancer including models of melanoma, colorectal, NSCLC, pancreatic and breast cancer. TAK-733 is well tolerated with pharmacokinetics and pharmacodynamics that support once-daily oral dosing in humans. [1] TAK-733 shows maximally efficacious doses at once daily orally doses of 10 mg/kg. [2]
Clinical Trials A Multicenter, Open-label, Dose-escalation, Phase I Study of TAK-733, an Oral MEK Inhibitor, in Adult Patients With Advanced Nonhematologic Malignancies.
Features
Combination Therapy
Description Alisertib at dose of 30 mg/kg combine with TAK-733 at dose of 10 mg/kg result in additive to synergistic antitumor activity and in prolonged inhibition of tumor regrowth in experimental human solid tumor xenograft models including NSCLC (NCI H23 [KRAS and LKB1 mutations]), CRC (SW620 [KRAS, APC, p53 mutations]), and pancreatic cancer (Panc 1 and Capan 1 [KRAS mutations] and BxPC-3 [No MAPK mutations]) models in immunocompromised mice. [2]
Protocol
Animal Study [2]
Animal Models Human solid tumor xenograft models including NSCLC (NCI H23 [KRAS and LKB1 mutations]), CRC (SW620 [KRAS, APC, p53 mutations]) Pancreatic cancer (Panc 1 and Capan 1 [KRAS mutations] and BxPC-3 [No MAPK mutations]) models in immunocompromised mice.
Formulation Saline
Doses 10 mg/kg
Administration Orally administrated once daily for 21 days
References
[1] Qing Dong, et al. Bioorg Med Chem Lett, 2011, 21(5), 1315-1319.
[2] Fabrey R, et al. AACR Annual Meeting, 2012, Abs 3739.