[CAS NO. 366017-09-6] Mubritinib (TAK 165)

Name: Mubritinib (TAK 165)
Brand: Arctom Scientific
SKU: SLK-S2216

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PRODUCTS SPECIFICATIONS [366017-09-6]

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Catalog

SLK-S2216

Brand

Selleck

CAS

366017-09-6

DESCRIPTION [366017-09-6]

Overview

MDL	MFCD09954135
Molecular Weight	468.47
Molecular Formula	C25H23F3N4O2
SMILES	C(=C/C1=CC=C(C(F)(F)F)C=C1)\C2=NC(COC3=CC=C(CCCCN4C=CN=N4)C=C3)=CO2

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	2.1346 mL	10.6730 mL	21.3461 mL
5 mM	0.4269 mL	2.1346 mL	4.2692 mL
10 mM	0.2135 mL	1.0673 mL	2.1346 mL
50 mM	-	-	-

Description

Mubritinib (TAK-165) is a potent inhibitor of with of 6 nM in BT-474 cell; no activity to EGFR, FGFR, PDGFR, JAK1, Src and Blk in BT-474 cell line.

Targets

HER2/ErbB2 ^[1]
(BT-474 cells)

6.0 nM

In vitro

Mubritinib displays > 4000-fold selectivity over other tyrosine kinases, such as EGFR, FGFR, PDGFR, Jak1, Src and Blk. Mubritinib even at low concentration of 0.1 μM significantly blocks HER2 phosphorylation, leading to the downregulation of PI3K-Akt and MAPK pathway in cell line BT474 with high level of HER2. Mubritinib not only exhibits highly potent antiproliferative effect in ErbB2-overexpressing cancer cell line BT474 with an IC50 of 5 nM, but also displays marked antiproliferative effects in cell lines with HER2 expressed weakly with IC50 of 53 nM, 90 nM and 91 nM for LNCaP, LN-REC4 and T24, respectively. Mubritinib displays no inhibitory activities against PC-3 cells with HER2 expressed very faintly with IC50 of 4.62 μM, as well as EGFR-overexpressing HT1376 and ACHN cell lines with IC50 of >25 μM.

References

[1] Nagasawa J, et al. Int J Urol, 2006, 13(5), 587-592.

Synonyms

1H-1,2,3-Triazole, 1-[4-[4-[[2-[(1E)-2-[4-(trifluoromethyl)phenyl]ethenyl]-4-oxazolyl]methoxy]phenyl]butyl]-

1-[4-[4-[[2-[(1E)-2-[4-(Trifluoromethyl)phenyl]ethenyl]-4-oxazolyl]methoxy]phenyl]butyl]-1H-1,2,3-triazole

1-(4-[4-[(2-[(E)-2-[4-(Trifluoromethyl)phenyl]ethenyl]-1,3-oxazol-4-yl)methoxy]phenyl]butyl)-1H-1,2,3-triazole

TAK 165

Mubritinib