7-CYCLOPENTYL-5-(4-PHENOXY)PHENYL-7H-PYR Property

Boiling point:

605.1±55.0 °C(Predicted)

Density 

1.30±0.1 g/cm3(Predicted)

storage temp. 

2-8°C

solubility 

DMSO: 17 mg/mL at ≤60 °C, soluble

form 

White solid

pka

5.75±0.30(Predicted)

color 

white

Safety

WGK Germany 

3

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

7-CYCLOPENTYL-5-(4-PHENOXY)PHENYL-7H-PYR Chemical Properties,Usage,Production

Uses

Lck Inhibitor is a cell-permeable ATP-competitive inhibitor of Lck.

Definition

ChEBI: RK-24466 is a member of the class of pyrrolopyrimidines that is 7H-pyrrolo[2,3-d]pyrimidine substituted by amino, 4-phenoxyphenyl, and cyclopentyl groups at positions 4, 5 and 7, respectively. It is a potent inhibitor of Lck that inhibits Lck (64-509) and LckCD isoforms (IC50 of less than 1 and 2 nM, respectively). It has a role as a geroprotector and an EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor. It is a primary amino compound, a pyrrolopyrimidine, an aromatic amine, an aromatic ether and a member of cyclopentanes.

General Description

A cell-permeable pyrrolopyrimidine compound that acts as a potent, reversible, selective, and ATP-competitive inhibitor of Lck (IC₅₀ at 5 μM ATP = <1 nM, 2 nM, 70 nM, 1.57 μM and 1.98 μM for lck_64-509 Y³⁹⁴, Lckcd pY³⁹⁴, Src, Kdr and Tie-2, respectively; IC₅₀ at 1 mM ATP = 16 μM, 66 nM, 126 nM, 420 nM and 5.18 μM for Lck_64-509 Y³⁹⁴, Blk, Fyn, Lyn and Csk, respectively). Only minimally affects the activities of other kinases (IC₅₀ = 3.2 μM, >33 μM, >50 μM and >50 μM for EGFR, PKC, CDC2/B and ZAP-70, respectively). Also shown to potently block T-cell receptor-stimulated IL-2 production in vitro (IC₅₀<1-40 nM in Jurkat T cells) and in vivo (ED₅₀ = 4 mg/kg in mice, ip.)

Biochem/physiol Actions

Primary TargetLck?????? Y3