TAK-733

ArtNr	S2617-10
Hersteller	Selleckchem
CAS-Nr.	1035555-63-5
Menge	10 mg
Kategorie	Oncology Neuroscience Neural Signaling Inhibitors & Compound Libraries Small Molecules By Organ Lung Cancer Skin Cancer Bladder Cancer Colorectal Cancer Breast Cancer Pancreatic Cancer
Typ	Inhibitors
Specific against	other
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Alias	MEK1/2;MEK
Similar products	TAK-733
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Administration	Orally administrated once daily for 21 days
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.
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
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.
Description	TAK-733 is a potent, selective, non ATP-competitive MEK inhibitor with IC50 of 3.2 nM.
Dosages	10 mg/kg
Formulation	Saline
IC50	3.2 nM [1], 3.2 nM [1], 3.2 nM [1], 3.2 nM [1], 3.2 nM [1], 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]
Molecular Weight (MW)	504, 23
Picture ChemicalStructure Description	TAK-733 Chemical Structure
Picture Description 1	, , one customer, TAK-733purchased from Selleck, Mouse carcinoma cells were treated with the inhibitors for 16 and 40 h at the concentrations indicated. The effect on S-phase was evident at 16 hrs. (A) whereas apoptosis was induced at 40h. (B) Biological effects of the compounds correlated with effects on phosphorylation of the MEK target ERK. (C) IC50 on S-phase and ERK-posphorylation: TAK-733=1-10nM, GSK1120212=1nM.
Picture Description 2	, , Dr. Zhang, of Tianjin Medical University, TAK-733purchased from Selleck, After starved in serum-free medium for 24 h, T47D cells incubated with the indicated concentrations of TAK-733 for 3 h, followed by 20-minute stimolation of 100ng/ml EGF.
Solubility (25C)	DMSO 101 mg/mL, Water <1 mg/mL, Ethanol <1 mg/mL
Storage	2 years -20CPowder, 2 weeks4Cin DMSO, 2 months-80Cin DMSO

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Menge: 10 mg

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