ALW-II-41-27

Names

[ CAS No. ]:
1186206-79-0

[ Name ]:
ALW-II-41-27

[Synonym ]:
hms2043h01
hms2218g07
cs-1203
alw-ii-41-27

Biological Activity

[Description]:

ALW-II-41-27 is a Eph family tyrosine kinase inhibitor with an IC50 of 11 nM for Eph2.

[Related Catalog]:

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> Ephrin Receptor

Research Areas >> Cancer

[Target]

IC50: 11 nM (Eph2)[1]

[In Vitro]

ALW-II-41-27 inhibits Ba/F3 cells transformed with Tel fusions of EphA3, Kit, Fms, KDR, FLT1, FGR, Src, Lyn, Bmx, and Bcr-Abl with an EC50 below 500 nM. ALW-II-41-27 exhibits cross reactivity with Bcr-Abl. ALW-II-41-27 inhibits b-raf, CSF1R, DDR1, DDR2, EphA2, EphA5, EphA8, EphB1, EphB2, EphB3, Frk, Kit, Lck, p38α, p38β, PDGFRα, PDGFRβ, and Raf1 and many more demonstrating how introduction of the thiophene group can have a tremendous impact on kinase selectivity[1].

[References]

[1]. Choi, et al. Discovery and structural analysis of Eph receptor tyrosine kinase inhibitors. Bioorganic & Medicinal Chemistry Letters (2009), 19(15), 4467-4470.

[2]. Song W, et al. Targeting EphA2 impairs cell cycle progression and growth of basal-like/triple-negative breast cancers. Oncogene. 2017 Jun 5.

[Related Small Molecules]

XL-647 | NVP-BHG712 | JI-101

Chemical & Physical Properties

[ Molecular Formula ]:
C₃₂H₃₂F₃N₅O₂S

[ Molecular Weight ]:
607.68900

[ Exact Mass ]:
607.22300

[ PSA ]:
112.79000

[ LogP ]:
7.42320

[ Storage condition ]:
2-8℃

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Related Compounds

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