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CGP60474

Catalog No. T14943 CAS 164658-13-3

CGP60474 is an inhibitor of VEGFR-2 (IC50 = 84 nM) and an inhibitor of ATP-competitive PKC. CGP60474 is also a highly potent anti-endotoxemic agent and inhibits cyclin-dependent kinase (CDK) potently.

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CGP60474, CAS 164658-13-3

Pack Size	Availability	Price/USD
1 mg	In stock	$ 30.00
2 mg	In stock	$ 40.00
5 mg	In stock	$ 68.00
10 mg	In stock	$ 98.00
25 mg	In stock	$ 197.00
50 mg	In stock	$ 349.00
100 mg	In stock	$ 576.00
1 mL * 10 mM (in DMSO)	In stock	$ 75.00

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Biological Description

Chemical Properties

Storage & Solubility Information

Description	CGP60474 is an inhibitor of VEGFR-2 (IC50 = 84 nM) and an inhibitor of ATP-competitive PKC. CGP60474 is also a highly potent anti-endotoxemic agent and inhibits cyclin-dependent kinase (CDK) potently.
Targets&IC50	CDK9-CyclinT:13 nM, CDK5-p25:10 nM, CDK4-CyclinD:216 nM, CDK2-CyclinE:3 nM, CDK7-CyclinH:200 nM, CDK2-CyclinA:4 nM, CDK1-CyclinB:26 nM, VEGFR2:84 nM
In vitro	The IC50 values are 26, 3, 4, 216, 10, 200 and 13 nM for CDK1/CyclinB, CDK2/CyclinE, CDK2/CyclinA, CDK5/p25, CDK7/CyclinH, CDK4/CyclinD and CDK9/cycT, respectively[4].
In vivo	In the LPS endotoxemia model, CGP60474 (10?mg/kg; i.p.) inhibits the IL-6 level and increases the survival rate[3].

Molecular Weight	355.82
Formula	C18H18ClN5O
CAS No.	164658-13-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (140.52 mM)

H2O: < 0.1 mg/mL (insoluble)

References and Literature

1. Kuo GH, et al. Synthesis and identification of [1,3,5]triazine-pyridine biheteroaryl as a novel series of potent cyclin-dependent kinase inhibitors. J Med Chem. 2005 Jul 14;48(14):4535-46. 2. Stanetty P, et al. Novel and efficient access to phenylamino-pyrimidine type protein kinase C inhibitors utilizing a Negishi cross-coupling strategy. J Org Chem. 2005 Jun 24;70(13):5215-20. 3. Han HW, et al. LINCS L1000 dataset-based repositioning of CGP-60474 as a highly potent anti-endotoxemic agent. Sci Rep. 2018;8(1):14969. Published 2018 Oct 8. 4. Jorda R, et al. How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases?. J Med Chem. 2018;61(20):9105-9120.

Related compound libraries

This product is contained In the following compound libraries：

Kinase Inhibitor Library Tyrosine Kinase Inhibitor Library Inhibitor Library TGF-beta/Smad Compound Library Anti-Breast Cancer Compound Library Anti-Colorectal Cancer Compound Library Anti-Cardiovascular Disease Compound Library Epigenetics Compound Library Anti-Liver Cancer Compound Library Cytoskeletal Signaling Pathway Compound Library

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Keywords

CGP60474 164658-13-3 Angiogenesis Cell Cycle/Checkpoint Chromatin/Epigenetic Cytoskeletal Signaling Tyrosine Kinase/Adaptors VEGFR CDK PKC inhibit endotoxemic CGP-60474 Cyclin dependent kinase LPS Inhibitor Protein kinase C selective survival ATP-competitive IL-6 level CGP 60474 inhibitor

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