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Merck

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

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About This Item

Empirical Formula (Hill Notation):
C18H13N3OS2
Molecular Weight:
351.45
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
Assay:
≥95% (HPLC)
Form:
liquid
Storage condition:
OK to freeze, avoid repeated freeze/thaw cycles, desiccated (hygroscopic), protect from light
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Product Name

Cdk1 Inhibitor IV, RO-3306, InSolution, ≥95%

Quality Segment

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

General description

A cell-permeable quinolinyl thiazolinone compound that acts as a potent and ATP-competitive inhibitor of Cdk1 (Ki = 35 nM and 110 nM for Cdk1/B1 and Cdk1/A, respectively). It affects Cdk2/E, PKCδ, and SGK only at much higher concentrations (Ki = 340, 318, and 497 nM, respectively), and shows little effect against Cdk4/D and six other commonly studied kinases (Ki =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 Ki: 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)


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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)



Certificates of Analysis (COA)

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