[CAS NO. 1035555-63-5] TAK-733

Name: TAK-733
Brand: Arctom Scientific
SKU: SLK-S2617

Ships within

Stock

Price

Qty

Total

$0.00

Please click "REQUEST A QUOTE" button if you need other sizes or custom synthesis

request a quote

If there is no stock, or you need other sizes or custom synthesis, please:

PRODUCTS SPECIFICATIONS [1035555-63-5]

Distributor

Catalog

SLK-S2617

Brand

Selleck

CAS

1035555-63-5

DESCRIPTION [1035555-63-5]

Overview

MDL	MFCD24386349
Molecular Weight	504.23
Molecular Formula	C17H15F2IN4O4
SMILES	O=C1C(C(NC2=CC=C(I)C=C2F)=C(F)C(N3C)=O)=C3N=CN1C[C@@H](O)CO

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	1.9832 mL	9.9161 mL	19.8322 mL
5 mM	0.3966 mL	1.9832 mL	3.9664 mL
10 mM	0.1983 mL	0.9916 mL	1.9832 mL
50 mM	0.0397 mL	0.1983 mL	0.3966 mL

Description

TAK-733 is a potent and selective allosteric site inhibitor for MEK1 with of 3.2 nM, inactive to Abl1, AKT3, c-RAF, CamK1, CDK2, c-Met, etc. Phase 1.

Targets

MEK1 ^[1]
(Cell-free assay)

3.2 nM

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.

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.