商品编号


AG-CR1-2903-M005



品牌


Adipogen



公司


Adipogen



公司分类


Cancer



Size

5 mg


商品信息


More Information



Product Details



Synonyms

2-(1R-Isopropyl-2-hydroxyethylamino)-6-(3-chloroanilino)-9-isopropylpurine; NG 60



Product Type

Chemical



Properties



Formula


C
19
H
25
ClN
6
O




MW

388.9



CAS

212844-53-6



Purity Chemicals

≥98% (HPLC)



Appearance

Off-white powder.



Solubility

Soluble in DMSO (30mg/ml), ethanol (10mg/ml), DMF (50mg/ml), methanol or dichloromethane.



Identity

Determined by
1
H-NMR.



InChi Key

PMXCMJLOPOFPBT-HNNXBMFYSA-N



Shipping and Handling



Shipping

AMBIENT



Short Term Storage

+4°C



Long Term Storage

-20°C



Use/St
ABI
lity

Stable for at least 2 years after receipt when stored at -20°C.



Documents



MSD
S


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Product Specification Sheet



Datasheet


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Potent, cell permeable cyclin-dependent protein kinase (cdk) inhibitor. Inhibits human CDK1 (IC
50
=4nM), CDK2/cyclin A (IC
50
=70nM), Cdc2/cyclin B, CDK2/cyclin E (IC
50
=35nM), CDK4/cyclin D1 (IC
50
=850nM) as well as CDK5/p35 (IC
50
=75nM).

DYRK1A inhibitor (IC
50
=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.



Product References

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

The specificities of protein kinase inhibitors: An update: J. Bain, et al.; Biochem. J.
371,
199 (2003)

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

Purvalanol A induces apoptosis and downregulation of antiapoptotic proteins through abrogation of phosphorylation of JAK2/STAT3 and RNA polymerase II: D. Iizuka, et al.; Anticancer Drugs
19,
565 (2008)

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

Olomoucine II and purvalanol A inhibit ABCG2 transporter in vitro and in situ and synergistically potentiate cytostatic effect of mitoxantrone: J. Hofman, et al.; Pharmacol. Res.
65,
312 (2012)

Purvalanol A, olomoucine II and roscovitine inhibit ABCB1 transporter and synergistically potentiate cytotoxic effects of daunorubicin in vitro: D. Cihalova, et al.; PLoS One
8,
e83467 (2013)

Purvalanol induces endoplasmic reticulum stress-mediated apoptosis and autophagy in a time-dependent manner in HCT116 colon cancer cells: A. Coker-Gurkan, et al.; Oncol. Rep.
33,
2761 (2015)