Purvalanol A
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MedKoo CAT#: 406332

CAS#: 212844-53-6

Description: 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.


Price and Availability

Size
Price

10mg
USD 150
500mg
USD 1950
Size
Price

50mg
USD 450
1g
USD 2950
Size
Price

100mg
USD 850
5g
USD 7950

Purvalanol A, purity > 98%, is in stock. The same day shipping out after order is received. Note: the estimated shipping out time for order > 500mg may be 2 weeks.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 406332
Name: Purvalanol A
CAS#: 212844-53-6
Chemical Formula: C19H25ClN6O
Exact Mass: 388.17784
Molecular Weight: 388.89
Elemental Analysis: C, 58.68; H, 6.48; Cl, 9.12; N, 21.61; O, 4.11


Synonym: Purvalanol A, Purv.

IUPAC/Chemical Name: (R)-2-((6-((3-chlorophenyl)amino)-9-isopropyl-9H-purin-2-yl)amino)-3-methylbutan-1-ol

InChi Key: PMXCMJLOPOFPBT-HNNXBMFYSA-N

InChi Code: 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

SMILES Code: CC(C)[C@@H](NC1=NC(NC2=CC=CC(Cl)=C2)=C3N=CN(C(C)C)C3=N1)CO


Technical Data

Appearance:
Grey to green solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs

Storage Condition:
0 – 4 oC for short term (weeks to 1 month) or -20 oC for long terms (months to years).

Solubility:
Soluble in DMSO

Shelf Life:
>2 years if stored properly.

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:
293490


Additional Information

  
 
 
 


References

1: Obakan P, Arısan ED, Ozfiliz P, Coker-Gürkan A, Palavan-Ãœnsal N. Purvalanol A is a strong apoptotic inducer via activating polyamine catabolic pathway in MCF-7 estrogen receptor positive breast cancer cells. Mol Biol Rep. 2013 Nov 5. [Epub ahead of print] PubMed PMID: 24190492.

2: Hofman J, Kučera R, Cihalova D, Klimes J, Ceckova M, Staud F. Olomoucine II, but Not Purvalanol A, Is Transported by Breast Cancer Resistance Protein (ABCG2) and P-Glycoprotein (ABCB1). PLoS One. 2013 Oct 8;8(10):e75520. doi: 10.1371/journal.pone.0075520. PubMed PMID: 24116053; PubMed Central PMCID: PMC3792958.

3: Hofman J, Ahmadimoghaddam D, Hahnova L, Pavek P, Ceckova M, Staud F. Olomoucine II and purvalanol A inhibit ABCG2 transporter in vitro and in situ and synergistically potentiate cytostatic effect of mitoxantrone. Pharmacol Res. 2012 Mar;65(3):312-9. doi: 10.1016/j.phrs.2011.11.017. Epub 2011 Dec 6. PubMed PMID: 22173067.

4: Hikita T, Oneyama C, Okada M. 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. doi: 10.1111/j.1365-2443.2010.01439.x. Epub 2010 Sep 5. PubMed PMID: 20825494.

5: Agbottah E, Yeh WI, Berro R, Klase Z, Pedati C, Kehn-Hall K, Wu W, Kashanchi F. Two specific drugs, BMS-345541 and purvalanol A induce apoptosis of HTLV-1 infected cells through inhibition of the NF-kappaB and cell cycle pathways. AIDS Res Ther. 2008 Jun 10;5:12. doi: 10.1186/1742-6405-5-12. PubMed PMID: 18544167; PubMed Central PMCID: PMC2483717.

6: Iizuka D, Ogura A, Kuwabara M, Inanami O. Purvalanol A induces apoptosis and downregulation of antiapoptotic proteins through abrogation of phosphorylation of JAK2/STAT3 and RNA polymerase II. Anticancer Drugs. 2008 Jul;19(6):565-72. doi: 10.1097/CAD.0b013e3282fe330e. PubMed PMID: 18525315.

7: Iizuka D, Inanami O, Kashiwakura I, Kuwabara M. Purvalanol A enhances cell killing by inhibiting up-regulation of CDC2 kinase activity in tumor cells irradiated with high doses of X rays. Radiat Res. 2007 May;167(5):563-71. PubMed PMID: 17474786.

8: Maćkowiak M, Kolasiewicz W, Markowicz-Kula K, Wedzony K. Purvalanol A, inhibitor of cyclin-dependent kinases attenuates proliferation of cells in the dentate gyrus of the adult rat hippocampus. Pharmacol Rep. 2005 Nov-Dec;57(6):845-9. PubMed PMID: 16382206.

9: Villerbu N, Gaben AM, Redeuilh G, Mester J. Cellular effects of purvalanol A: a specific inhibitor of cyclin-dependent kinase activities. Int J Cancer. 2002 Feb 20;97(6):761-9. PubMed PMID: 11857351.