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TAK-733

TAK-733

Item no.	S2617-10000
Manufacturer	Selleckchem
CASRN	1035555-63-5
Amount	10 g
Quantity options	10 mg 1 g 10 g 10 mM/1 mL 200 mg 5 mg 50 mg 5 g
Category	Oncology Neuroscience Neural Signaling Inhibitors & Compound Libraries Small Molecules By Organ Lung Cancer Skin Cancer Bladder Cancer Colorectal Cancer Breast Cancer Pancreatic Cancer
Type	Inhibitors
Specific against	other
Smiles	CN1C2=C(C(=C(C1=O)F)NC3=C(C=C(C=C3)I)F)C(=O)N(C=N2)CC(CO)O
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Alias	MEK1/2,MEK
Similar products	TAK-733
Available
Storage Conditions	2 years -80 in solvent
Molecular Weight	504, 23
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.
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.
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]
Solubility (25C)	DMSO 101 mg/mL, Water <1 mg/mL, Ethanol <1 mg/mL
Information	TAK-733 is a potent and selective MEK allosteric site inhibitor for MEK1 with IC50 of 3.2 nM, inactive to Abl1, AKT3, c-RAF, CamK1, CDK2, c-Met, etc. Phase 1.
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

Note: The presented information and documents (Manual, Product Datasheet, Safety Datasheet and Certificate of Analysis) correspond to our latest update and should serve for orientational purpose only. We do not guarantee the topicality. We would kindly ask you to make a request for specific requirements, if necessary.

All products are intended for research use only (RUO). Not for human, veterinary or therapeutic use.

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S2617-10000-datasheet.pdf

S2617-10000-safety-datasheet.pdf