WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H406160
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.
Hodoodo Cat#: H406160
Name: PHA-680632
CAS#: 398493-79-3
Chemical Formula: C28H35N7O2
Exact Mass: 501.29
Molecular Weight: 501.635
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
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).
HS Tariff Code: 2934.99.9001
More Info:
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| In vitro activity: | |
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The following data is based on the product molecular weight 501.64 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | |
| In vitro protocol: | |
| In vivo protocol: |
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.
