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212844-53-6 (Purvalanol A)

1

Identification

Purvalanol A Purvalanol A
Name Purvalanol A
Formula C19H25ClN6O
MW 388.89
CAS No. 212844-53-6
EINECS
Smiles CC([[email protected]@H](NC1=NC(NC2=CC=CC(Cl)=C2)=C3N=CN(C(C)C)C3=N1)CO)C
Synonyms NG-60; (R)-2-((6-((3-chlorophenyl)amino)-9-isopropyl-9H-purin-2-yl)amino)-3-methylbutan-1-ol
InChI InChI=1S/C19H25ClN6O/c1-11(2)15(9-27)23-19-24-17(22-14-7-5-6-13(20)8-14)16-18(25-19)26(10-21-16)12(3)4/h5-8,10-12,15,27H,9H2,1-4H3,(H2,22,23,24,25)/t15-/m0/s1
2

Introduction

Purvalanol A(NG-60) is a potent, cell-permeable, and selective inhibitor of cyclin-dependent kinases (CDKs) with IC50 values of 4, 70, 35, 850, and 75 nM for cdc2/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E, Cdk4/cyclin D1 and Cdk5-p35, respectively. IC50 value: [1] [2] Target: CDKs inhibitor in vitro: Purvalanol A reversibly arrests synchronized cells in the G1 and G2 phase of the cell cycle, inhibiting both cell proliferation and cell death [3].

Background Information

Potent, cell permeable cyclin-dependent protein kinase (cdk) inhibitor. Inhibits human CDK1 (IC50=4nM), CDK2/cyclin A (IC50=70nM), Cdc2/cyclin B, CDK2/cyclin E (IC50=35nM), CDK4/cyclin D1 (IC50=850nM) as well as CDK5/p35 (IC50=75nM). DYRK1A inhibitor (IC50=300nM). Anticancer agent. Strong apoptotic and autophagy inducer which causes cell cycle arrest in the G1 and G2 phase in various cancer cell lines. More membrane permeable than purvalanol B. Shown to inhibit ABCB1 and ABCB2 transporters and useful in co-treatment with selected anticancer drugs. ......by Adipogen Corporation
Purvalanol A is a potent, cell-permeable cyclin-dependent protein kinase (cdk) inhibitor. IC50 values are 4, 70, 35, 850 and 75 nM for cdc2/cyclin B, cdk2/cyclin A, cdk2/cyclin E, cdk4/cyclin D1 and cdk5-p35 respectively. ......by AdooQ BioScience, LLC
Purvalanol A is a potent CDK inhibitor, which effectively suppresses Src-mediated transformation by inhibiting both CDKs and c-Src. indicating that the activation of CDKs contributes to the c-Src transformation. Purvalanol A suppressed the c-Src activity ......by BOC Sciences
Purvalanol A is a potent CDK inhibitor, which inhibits cdc2-cyclin B, cdk2-cyclin A, cdk2-cyclin E, cdk4-cyclin D1, and cdk5-p35 with IC50s of 4, 70, 35, 850, 75 nM, resepctively. ......by MedChemexpress Co., Ltd.
Purvalanol A is a potent CDK inhibitor, which effectively suppresses Src-mediated transformation by inhibiting both CDKs and c-Src. indicating that the activation of CDKs contributes to the c-Src transformation. Purvalanol A suppressed the c-Src activity as effectively as the Src-selective inhibitor PP2, and that it reverted the transformed morphology to a nearly normal shape with less cytotoxicity than PP2. Purvalanol A induced a strong G2-M arrest, whereas PP2 weakly acted on the G1-S transition. Furthermore, when compared with PP2, purvalanol A more effectively suppressed the growth of human colon cancer HT29 and SW480 cells, in which Src family kinases and CDKs are activated. ......by MedKoo Biosciences, Inc.
A potent, cell-permeable, selective inhibitor of CDK with IC50s of 4, 70, 35, 850, and 75 nM for cdc2/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E, Cdk4/cyclin D1 and Cdk5-p35, respectively; also inhibits Saccharomyces cerevisiae Cdc28p (IC50=80 nM) and has no effect on PKC, Raf, CK1, CK2. ......by ProbeChem
Purvalanol A is a potent, and cell-permeable CDK inhibitor with IC50 of 4 nM, 70 nM, 35 nM, and 850 nM for cdc2-cyclin B, cdk2-cyclin A, cdk2-cyclin E, and cdk4-cyclin D1, respectively. ......by Selleck Chemicals LLC
Cyclin-dependent kinase inhibitor. IC50 values are 4, 70, 35, 850 and 75 nM for cdc2/cyclin B, cdk2/cyclin A, cdk2/cyclin E, cdk4/cyclin D1 and cdk5-p35 respectively. Reversibly arrests synchronised cells in G1 and G2, and inhibits cell proliferation and cell death. ......by Tocris Bioscience Inc.
3

Protocol(Only for Reference)

Cell Experiment

Animal Experiment

4

Physical and Chemical Properties

Appearance:Light yellow to yellow Solid EBNumber:EB000071430

Storage condition

4°C by MedChemexpress Co., Ltd.
Store at +4°C by Tocris Bioscience Inc.

Solubility

100 mM in DMSO by CHEMSCENE, LLC
100 mM in DMSO by MedChemexpress Co., Ltd.
Soluble to 50 mM in ethanol and to 100 mM in DMSO by Tocris Bioscience Inc.
5

Mechanism and Indication

Signaling Pathways Cell Cycle/DNA Damage Autophagy
Target CDK Autophagy
Research Area Cancer
Indications
6

Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
Purvalanol A - No Development Reported
7

Safety Data of Purvalanol A

WGKGermany : 3
8

Spectral Information

9

Suppliers List

Company Price and Availability Country/Region
Adipogen Corporation USA
AdooQ BioScience, LLC USA
Apexbio Technology LLC USA
Ark Pharm, Inc. USA
BOC Sciences
Biochempartner Co., Ltd China
CHEMSCENE, LLC 10mg/USD84();50mg/USD192() USA
Cayman Chemical Company USA
LC Laboratoies 10mg/USD68(In stock);25mg/USD89(In stock);50mg/USD153(In stock);100mg/USD222(In stock);300mg/USD420(In stock);1g/USD998(In stock);2g/USD1720(In stock) USA
MedChemexpress Co., Ltd. 5mg/USD60();10mg/USD84() USA
MedKoo Biosciences, Inc. USA
ProbeChem
Selleck Chemicals LLC USA
Shanghai Haoyuan Chemexpress Co., Ltd. 5mg/USD60();10mg/USD84() China
Tocris Bioscience Inc. USA
10

Related Products

Other Forms of 212844-53-6

Name CAS No Formula MW
Purvalanol B 212844-54-7 C20H25ClN6O3 432.9

Recommended Compounds in CDK Autophagy

Name CAS No Formula MW
LY2857785 1619903-54-6 C26H36N6O 448.6
THZ2 1604810-84-5 C31H28ClN7O2 566.0527
Palbociclib (isethionate) 827022-33-3 C26H35N7O6S 573.66
CDK9-IN-6 1391855-95-0 C27H37ClN6O2 513.07468
ML167 1285702-20-6 C19H17N3O3 335.36
AMG 925 1401033-86-0 C26H29N7O2 471.55
LDC000067 1073485-20-7 C18H18N4O3S 370.43
LEE011 (succinate hydrate) 1374639-79-8 C27H38N8O6X 570.64
LEE011 (succinate) 1374639-75-4 C27H36N8O5 552.63
LEE011 (hydrochloride) 1211443-80-9 C23H31ClN8O 471.0
LEE011 1211441-98-3 C23H30N8O 434.54
WHI-P180 (hydrochloride) 153437-55-9 C16H16ClN3O3 333.77
Wogonin 632-85-9 C16H12O5 284.26
1-NM-PP1 221244-14-0 C20H21N5 331.41
WHI-P180 211555-08-7 C16H15N3O3 297.31
THZ1 1604810-83-4 C31H28ClN7O2 566.05
Senexin A 1366002-50-7 C17H14N4 274.32
CDK4-IN-1 1256963-02-6 C22H29ClN8 440.97
Palbociclib (hydrochloride) 827022-32-2 C24H30ClN7O2 483.99
Purvalanol B 212844-54-7 C20H25ClN6O3 432.9

Recommended Compounds in Same Indication

Name CAS No Formula MW
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Route of Synthesis

12

References

[1]. Gray NS, et al. Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors. Science. 1998 Jul 24;281(5376):533-8.

[2]. Bain J, et al. The specificities of protein kinase inhibitors: an update. Biochem J. 2003 Apr 1;371(Pt 1):199-204.

[3]. Villerbu N, et al. Cellular effects of purvalanol A: a specific inhibitor of cyclin-dependent kinase activities. Int J Cancer. 2002 Feb 20;97(6):761-9.

[4]. Hikita T, et al. Purvalanol A, a CDK inhibitor, effectively suppresses Src-mediated transformation by inhibiting both CDKs and c-Src. Genes Cells. 2010 Oct;15(10):1051-62.

Protocol Reference

Gray et al (1998) Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors. Science 281 533. PMID: 9677190.

Gray et al (1999) ATP-site directed inhibitors of cyclin-dependent kinases. Curr.Med.Chem. 6 859. PMID: 10495356.

Villerbu et al (2002) Cellular effects of purvalanol A: a specific inhibitor of cyclin-dependent kinase activities. Int.J.Cancer 97 761. PMID: 11857351.

Bain et al (2003) The specificitie ......by Tocris Bioscience Inc.

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More Information

Purvalanol A

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