PHA-680632

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 406160

CAS#: 398493-79-3

Description: PHA-680632 is a is potent inhibitor of Aurora A, Aurora B and Aurora C with IC50 of 27 nM, 135 nM and 120 nM, respectively. PHA-680632 is also the first representative of a new class of Aurora inhibitors with a high potential for further development as an anticancer therapeutic. PHA-680632 is active on a wide range of cancer cell lines and shows significant tumor growth inhibition in different animal tumor models at well-tolerated doses.


Price and Availability

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PHA680632 is not in stock, may be available through custom synthesis. For cost-effective reason, minimum 1 gram order is requested. The product will be characterized by NMR, HPLC and MS analysis. Purity (HPLC) is usually >98%. CoA, QC data, MSDS will be provided when product is successfully made. The estimated lead time is 2-3 months. Please send email to sales@medkoo.com to inquire quote.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 406160
Name: PHA-680632
CAS#: 398493-79-3
Chemical Formula: C28H35N7O2
Exact Mass: 501.28522
Molecular Weight: 501.62
Elemental Analysis: C, 67.04; H, 7.03; N, 19.55; O, 6.38


Synonym: PHA680632; PHA 680632; PHA-680632.

IUPAC/Chemical Name: N-(2,6-diethylphenyl)-3-(4-(4-methylpiperazin-1-yl)benzamido)pyrrolo[3,4-c]pyrazole-5(1H,4H,6H)-carboxamide

InChi Key: OBWNXGOQPLDDPS-UHFFFAOYSA-N

InChi Code: InChI=1S/C28H35N7O2/c1-4-19-7-6-8-20(5-2)25(19)29-28(37)35-17-23-24(18-35)31-32-26(23)30-27(36)21-9-11-22(12-10-21)34-15-13-33(3)14-16-34/h6-12H,4-5,13-18H2,1-3H3,(H,29,37)(H2,30,31,32,36)

SMILES Code: O=C(N(C1)CC2=C1C(NC(C3=CC=C(N4CCN(C)CC4)C=C3)=O)=NN2)NC5=C(CC)C=CC=C5CC


Technical Data

Appearance:
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:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
soluble in DMSO

Shelf Life:
>5 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: Polacchini A, Albani C, Baj G, Colliva A, Carpinelli P, Tongiorgi E. Combined cisplatin and aurora inhibitor treatment increase neuroblastoma cell death but surviving cells overproduce BDNF. Biol Open. 2016 Jun 2. pii: bio.016725. doi: 10.1242/bio.016725. [Epub ahead of print] PubMed PMID: 27256407.

2: Mazzera L, Lombardi G, Abeltino M, Ricca M, Donofrio G, Giuliani N, Cantoni AM, Corradi A, Bonati A, Lunghi P. Aurora and IKK kinases cooperatively interact to protect multiple myeloma cells from Apo2L/TRAIL. Blood. 2013 Oct 10;122(15):2641-53. doi: 10.1182/blood-2013-02-482356. Epub 2013 Aug 23. PubMed PMID: 23974204.

3: Ratushny V, Pathak HB, Beeharry N, Tikhmyanova N, Xiao F, Li T, Litwin S, Connolly DC, Yen TJ, Weiner LM, Godwin AK, Golemis EA. Dual inhibition of SRC and Aurora kinases induces postmitotic attachment defects and cell death. Oncogene. 2012 Mar 8;31(10):1217-27. doi: 10.1038/onc.2011.314. Epub 2011 Jul 25. PubMed PMID: 21785464; PubMed Central PMCID: PMC3204164.

4: Tao Y, Zhang P, Frascogna V, Lecluse Y, Auperin A, Bourhis J, Deutsch E. Enhancement of radiation response by inhibition of Aurora-A kinase using siRNA or a selective Aurora kinase inhibitor PHA680632 in p53-deficient cancer cells. Br J Cancer. 2007 Dec 17;97(12):1664-72. Epub 2007 Nov 20. PubMed PMID: 18026198; PubMed Central PMCID: PMC2360282.

5: Soncini C, Carpinelli P, Gianellini L, Fancelli D, Vianello P, Rusconi L, Storici P, Zugnoni P, Pesenti E, Croci V, Ceruti R, Giorgini ML, Cappella P, Ballinari D, Sola F, Varasi M, Bravo R, Moll J. PHA-680632, a novel Aurora kinase inhibitor with potent antitumoral activity. Clin Cancer Res. 2006 Jul 1;12(13):4080-9. PubMed PMID: 16818708.