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Tocris/SU 9516/2907/50/50 mg

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货号: 2907/50

品牌: Tocris

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Description: Potent cdk2 inhibitor

Chemical Name: (Z)-1,3-Dihydro-3-(1H-imidazol-4-ylmethylene)-5-methoxy-2H-indol-2-one

Purity: ≥99% (HPLC)

Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity

Potent, selective cdk2 inhibitor (IC₅₀ values are 0.022, 0.04, 0.2, >10, >10, 18 and >100 μM for cdk2, cdk1, cdk4, PKC, p38, PDGFR and EGFR respectively). Inhibits pRb phosphorylation causing enhanced pRB/E2F complex formation and induces G₁ and G₂-M cell cycle arrest. Transcriptionally downregulates Mcl-1 and has antiproliferative, cytostatic and pro-apoptotic effects in vitro.

Compound Libraries

SU 9516 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt	241.25
Formula	C₁₃H₁₁N₃O₂
Storage	Store at +4°C
Purity	≥99% (HPLC)
CAS Number	377090-84-1
PubChem ID	5289419
InChI Key	QNUKRWAIZMBVCU-WCIBSUBMSA-N
Smiles	O=C2NC1=CC=C(OC)C=C1/C2=C/C3=CNC=N3

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	24.12	100
	ethanol	4.83	20

Preparing Stock Solutions

The following data is based on the product molecular weight 241.25. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	4.15 mL	20.73 mL	41.45 mL
5 mM	0.83 mL	4.15 mL	8.29 mL
10 mM	0.41 mL	2.07 mL	4.15 mL
50 mM	0.08 mL	0.41 mL	0.83 mL

Product Datasheets

Certificate of Analysis / Product Datasheet

Safety Datasheet

References

References are publications that support the products' biological activity.

Lane et al (2001) A novel cdk2-selective inhibitor, SU9516, induces apoptosis in colon carcinoma cells. Cancer Res. 61 6170 PMID: 11507069

Yu et al (2002) SU9516, a cyclin-dependent kinase 2 inhibitor, promotes accumulation of high molecular weight E2F complexes in human colon carcinoma cells. Biochem.Pharmacol. 64 1091 PMID: 12234612

Gao et al (2006) The three-substituted indolinone cyclin-dependent kinase 2 inhibitor 3-[1-(3H-Imidazol-4-yl)-meth-(Z)-ylidene]-5-methoxy-1,3-dihydro-indol-2-one (SU9516) kills human leukemia cells via down-regulation of Mcl-1 through a transcriptional m Mol.Pharmacol. 70 645 PMID: 16672643

Keywords: SU 9516, supplier, Potent, cdk2, inhibitors, inhibits, Transcriptionally, downregulates, Mcl-1, proapoptotic, Cyclin-Dependent, Protein, Kinases, Bcl-2, Family, SU9516, Cyclin-dependent, Kinase, Bcl-2, Family, Cyclin-dependent, Kinase, Tocris Bioscience

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