Purvalanol A


Catalog No. size PriceQuantity
M7023-2 2mg solid $84
M7023-10 10mg solid $324

Description

Cas:212844-53-6

Product Information

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.

 

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

NG60

NG-60

NG 60

 

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).

HS Tariff Code: 2934.99.9001

 

In Vitro

Purvalanol A inhibits cdc28 (S. cerevisiae) and erk1 with IC50s of 80 and 9000 nM. Purvalanol A shows inhibitory activities against the NCI panel of 60 human tumor cell lines, with average GI50 of 2 μM; two cell lines show an -20-fold increase in sensitivity to purvalanol A: the KM12 colon cancer cell line with a GI50 of 76 nM and the NCI-H522 non–small cell lung cancer cell line with a GI50 of 347 nM[1]. Purvalanol A is a 2.5-fold more potent inhibitor of CDK2, but also inhibits DYRK1A potently and a number of other protein kinases in the low micromolar range. Purvalanol A inhibits MKK1, MAPK2/ERK2, JNK/SAPK1c with IC50s of 80, 26, 84 μM. Purvalanol A selectively inhibits the phosphorylation of cellular proteins. Purvalanol A prevents the increases of the contents of cyclins D and E during serum-induced G1 phase progression. Purvalanol A does not inhibit transcription under cell-free conditions.

 

 

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.

 

  1. 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.

 

  1. 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.

 

  1. 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.

 

  1. 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.

 

Products are for research use only. Not for human use.

 

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