217721

RO-3306

≥95% (HPLC), liquid, Cdk1 inhibitor, Calbiochem^®

• 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
• UNSPSC Code: 12352200
• NACRES: NA.77
• MDL number: MFCD17392573
• Assay: ≥95% (HPLC)
• Form: liquid
• Storage condition: OK to freeze, avoid repeated freeze/thaw cycles, desiccated (hygroscopic), protect from light

Properties

• Product Name: Cdk1 Inhibitor IV, RO-3306, InSolution, ≥95%
• Quality Segment: 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
• SMILES string: [s]1c(ccc1)CNC2=NC(=O)\C(=C\c3cc4c(nccc4)cc3)\S2
• InChI: 1S/C18H13N3OS2/c22-17-16(24-18(21-17)20-11-14-4-2-8-23-14)10-12-5-6-15-13(9-12)3-1-7-19-15/h1-10H,11H2,(H,20,21,22)/b16-10-
• InChI key: XOLMRFUGOINFDQ-YBEGLDIGSA-N

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

Physical form

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

Preparation Note

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

Disclaimer

Toxicity: Irritant (B)

Safety Information

• Storage Class: 10 - Combustible liquids
• wgk: WGK 2
• flash_point_f: 188.6 °F - closed cup - (refers to pure substance)
• flash_point_c: 87 °C - closed cup - (refers to pure substance)