343022

Flt-3 Inhibitor III

The Flt-3 Inhibitor III, also referenced under CAS 852045-46-6, controls the biological activity of Flt-3. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• Synonym(s): Flt-3 Inhibitor III, (5-Phenyl-thiazol-2-yl)-(4-(2-pyrrolidin-1-yl-ethoxy)-phenyl)-amine, 5-Phenyl-N-(4-(2-(1-pyrrolidinyl)ethoxy)phenyl)-2-thiazolamine, 5-Phenyl-N-(4-(2-(1-pyrrolidinyl)ethoxy)phenyl)-2-thiazolamine, (5-Phenyl-thiazol-2-yl)-(4-(2-pyrrolidin-1-yl-ethoxy)-phenyl)-amine
• Empirical Formula (Hill Notation): C₂₁H₂₃N₃OS
• CAS Number: 852045-46-6
• Molecular Weight: 365.49
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 100
• assay: ≥95% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: off-white
• solubility: DMSO: 10 mg/mL
• shipped in: ambient
• storage temp.: −20°C

Description

General description

A cell-permeable 5-phenyl-2-thiazolamine compound that acts as a potent, ATP binding site-targeting inhibitor of Flt3 (IC₅₀ = 50 nM). It inhibits c-Kit, KDR, c-Abl, Cdk1, c-Src, and Tie-2 only at much higher concentrations (IC₅₀ = 0.26, 0.91, 1.2, 2.1, 2.8, and 8.0 µM, respectively) and exhibits little activity against a panel of 12 other commonly studied kinases even at concentrations as high as 10 µM. Blocks FLT3-dependent cell proliferation in a dose-dependent manner (IC₅₀ = 52, 240, and 760 nM in MV4:11-ITD, BaF3-ITD, and BaF3-D835/Y cells).

Biochem/physiol Actions

Cell permeable: yes

Primary Target
Flt-3

Product competes with ATP.

Reversible: no

Target IC₅₀: 50 nM against Flt3

Packaging

Packaged under inert gas

Warning

Toxicity: Harmful (C)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Furet, P., et al. 2006. J. Med. Chem.49, 4451.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable