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TAK-733 - 10mM in DMSO, high purity , CAS No.1035555-63-5(DMSO), Allosteric modulator of mitogen-activated protein kinase kinase 1

COA

Grade & Purity:

Moligand™

10mM in DMSO

Cas Number: 1035555-63-5(DMSO)
Molecular Weight: 504.23

In stock

Item Number

T408637

Grouped product items
SKU	Size	Availability	Price	Qty
T408637-1ml	1ml	Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!	$733.90

MEK1 Selective Inhibitors

View related series

Compound libraries (12325)

Basic Description

Synonyms	(R)-3-(2,3-dihydroxypropyl)-6-fluoro-5-(2-fluoro-4-iodophenylamino)-8-methylpyrido[2,3-d]pyrimidine-4,7(3H,8H)-dione
Specifications & Purity	Moligand™, 10mM in DMSO
Biochemical and Physiological Mechanisms	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.
Storage Temp	Store at -80°C
Shipped In	Dry ice packs + Cold packs This product requires cold chain shipping. Ground and other economy services are not available.
Grade	Moligand™
Action Type	ALLOSTERIC MODULATOR
Mechanism of action	Allosteric modulator of mitogen-activated protein kinase kinase 1
Product Description	Information TAK-733 is a potent and selectiveMEKallosteric site inhibitor for MEK1 withIC50of 3.2 nM, inactive to Abl1, AKT3, c-RAF, CamK1, CDK2, c-Met, etc. Phase 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. 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. TAK-733 shows maximally efficacious doses at once daily orally doses of 10 mg/kg. Cell Data cell lines： Concentrations： Incubation Time： Powder Purity:≥96%

Associated Targets(Human)

MAP2K2 Tclin Dual specificity mitogen-activated protein kinase kinase 2 (1 Activities)

Discover Target: MAP2K2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

MAP2K1 Tclin Dual specificity mitogen-activated protein kinase kinase 1 (5 Activities)

Discover Target: MAP2K1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Names and Identifiers

Smiles	CN1C(=O)C(=C(NC2=CC=C(I)C=C2F)C3=C1N=CN(CC(O)CO)C3=O)F
Molecular Weight	504.23

Certificates（CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):

Analytical Chart:

Chemical and Physical Properties

Solubility	Solubility (25°C) In vitro DMSO: 49 mg/mL (200.58 mM); Ethanol: 49 mg/mL (200.58 mM); Water: Insoluble;

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