217721

Cdk1 Inhibitor IV, RO-3306

InSolution, ≥95%

• Synonym(s): InSolution Cdk1 Inhibitor IV, RO-3306, 5-(6-Quinolinylmethylene)-2-((2-thienylmethyl)amino)-4(5H)-thiazolone, 5-(Quinolin-6-ylmethylene)-2-(thiophen-2-ylmethylamino)thiazol-4(5H)-one, 5-(Quinolin-6-ylmethylene)-2-(thiophen-2-ylmethylamino)thiazol-4(5H)-one, 5-(6-Quinolinylmethylene)-2-((2-thienylmethyl)amino)-4(5H)-thiazolone
• Empirical Formula (Hill Notation): C₁₈H₁₃N₃OS₂
• Molecular Weight: 351.45
• MDL number: MFCD17392573
• UNSPSC Code: 12352200

Properties

• Quality Level: 100
• Assay: ≥95% (HPLC)
• form: liquid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; avoid repeated freeze/thaw cycles; desiccated (hygroscopic); protect from light
• shipped in: dry ice
• storage temp.: −70°C

Description

General description

A cell-permeable quinolinyl thiazolinone compound that acts as a potent and ATP-competitive inhibitor of Cdk1 (K_i = 35 nM and 110 nM for Cdk1/B1 and Cdk1/A, respectively). It affects Cdk2/E, PKCδ, and SGK only at much higher concentrations (K_i = 340, 318, and 497 nM, respectively), and shows little effect against Cdk4/D and six other commonly studied kinases (K_i =2 M). Short-term treatment for up to 20 hrs results in fully reversible G2/M cell cycle arrest, while prolonged treament (>48 hrs) results in apoptotic cell death in proliferating cancer cells, but not in nontumorigenic epithelial cell lines. The solid form of this compound (Cat. No. 217699) is also available.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
Cdk1/B1 and Cdk1/A

Reversible: yes

Secondary Target
Cdk2/E, PKCδ, and SGK

Target K_i: 35 nM and 110 nM for Cdk1/B1 and Cdk1/A,

Packaging

Packaged under inert gas

Warning

Toxicity: Irritant (B)

Physical form

A 10 mM (2 mg/569 L) solution of Cdk1 Inhibitor IV, RO-3306 (Cat. No. 217699) in DMSO.

Reconstitution

Following initial thaw, aliquot and freeze (-70°C). Aliquots are stable for up to 6 months at -70°C.

Other Notes

Vassilev, L.T., et al. 2006. Proc. Natl. Acad. Sci. USA103, 10660.

Legal Information

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

Safety Information

• Storage Class Code: 10 - Combustible liquids
• WGK: WGK 2
• Flash Point(F): 188.6 °F - (refers to pure substance)
• Flash Point(C): 87 °C - (refers to pure substance)