TAK-733 - Moligand™, 10mM in DMSO , Allosteric modulator of mitogen-activated protein kinase kinase 1, CAS No.1035555-63-5, Allosteric modulator of mitogen-activated protein kinase kinase 1

CAS: 1035555-63-5 Cat. No.: T408637 Formula: C₁₇H₁₅F₂IN₄O₄ Molecular Weight: 504.23 PubChem CID: 24963252

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

(R)-3-(2,3-dihydroxypropyl)-6-fluoro-5-(2-fluoro-4-iodophenylamino)-8-methylpyrido[2,3-d]pyrimidine-4,7(3H,8H)-dione

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

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%

Specifications

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

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 Properties

ALogP

0.9

Names and Identifiers

Isomeric SMILES

CN1C2=C(C(=C(C1=O)F)NC3=C(C=C(C=C3)I)F)C(=O)N(C=N2)C[C@H](CO)O

Alternate CAS

1035555-63-5

PubChem CID

24963252

MeSH Entry Terms

TAK 733;TAK-733;TAK733

Molecular Weight

504.23

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)

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

Frequently Asked Questions

How should this product be stored?

Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.

What is Moligand??

Moligand? is one of Aladdin Scientific's premium product lines, formulated for high-purity applications across multiple workflows. Compared to standard grades in the same workflow, Moligand? products typically offer tighter specifications, more rigorous QC, and stronger lot-to-lot consistency.

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 1035555-63-5, the molecular formula is C17H15F2IN4O4, and the molecular weight is 504.23 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.