Cdk1/2 Inhibitor III-CAS 443798-55-8-Calbiochem

C₁₅H₁₃F₂N₇O₂S₂

425.44

A cell-permeable triazolo-diamine compound that displays anti-proliferative properties in various human cancer cells (IC₅₀ = 20 nM, 35 nM and 92 nM in HCT-116, HeLa, and A375 cells, respectively). Acts as a highly potent, reversible, ATP-competitive inhibitor of Cdk1/cyclin B and Cdk2/cyclin A (IC₅₀ = 600 pM and 500 pM, respectively) with selectivity over VEGF-R2 (IC₅₀ = 32 nM), GSK-3β (IC₅₀ = 140 nM), and a panel of eight other kinases (IC₅₀ ≥ 1 µM).

Cell permeable: yes
Target IC₅₀: 20 nM, 35 nM and 92 nM for anti-proliferative properties in HCT-116, HeLa, and A375 cells, respectively; 600 pM and 500 pM, against Cdk1/cyclin B and Cdk2/cyclin A, respectively
Primary Target
Cdk1/cyclin B, Cdk2/cyclin A
Product competes with ATP.
Reversible: yes

Toxicity: Harmful (C)

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

Lin, R., et al. 2005.J. Med. Chem.48, 4208.

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

100

≥95% (HPLC)

solid

Calbiochem^®

OK to freeze
protect from light

white

DMSO: 10 mg/mL
THF: soluble
acetone: soluble

ambient

2-8℃

1 mg in Plastic ampoule
Packaged under inert gas

11 - Combustible Solids

WGK 1