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802539-81-7,MFCD17169990
Catalog No.:AA00G3MP

802539-81-7 | PHA-848125

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Purity
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Price(USD)
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1mg
98%
in stock  
$56.00   $39.00
- +
5mg
98%
in stock  
$139.00   $97.00
- +
25mg
98%
in stock  
$450.00   $315.00
- +
100mg
98%
in stock  
$1,291.00   $904.00
- +
  • Technical Information
  • Properties
  • Downstream Synthesis Route
  • Literature
  • Request for Quotation
  • Download SDS
  • Technical Information
  • Properties
  • Downstream Synthesis Route
  • Literature
Technical Information
Catalog Number:
AA00G3MP
Chemical Name:
PHA-848125
CAS Number:
802539-81-7
Molecular Formula:
C25H32N8O
Molecular Weight:
460.5746
MDL Number:
MFCD17169990
SMILES:
CNC(=O)c1nn(c2c1C(C)(C)Cc1c2nc(nc1)Nc1ccc(cc1)N1CCN(CC1)C)C
Properties
Computed Properties
 
Complexity:
718  
Covalently-Bonded Unit Count:
1  
Heavy Atom Count:
34  
Hydrogen Bond Acceptor Count:
7  
Hydrogen Bond Donor Count:
2  
Rotatable Bond Count:
4  
XLogP3:
2.8  

Downstream Synthesis Route
CASUnavailable 
  74-89-5    802539-81-7 

[1]CurrentPatentAssignee:NERVIANOMEDICALSCIENCESS.R.L.-WO2004/104007,2004,A1Locationinpatent:Page179-180;187

[1]CurrentPatentAssignee:NERVIANOMEDICALSCIENCESS.R.L.-WO2004/104007,2004,A1Locationinpatent:Page182-183

[1]Locationinpatent:experimentalpartBrasca,MariaGabriella;Amboldi,Nadia;Ballinari,Dario;Cameron,Alexander;Casale,Elena;Cervi,Giovanni;Colombo,Maristella;Colotta,Francesco;Croci,Valter;D'Alessio,Roberto;Fiorentini,Francesco;Isacchi,Antonella;Mercurio,Ciro;Moretti,Walter;Panzeri,Achille;Pastori,Wilma;Pevarello,Paolo;Quartieri,Francesca;Roletto,Fulvia;Traquandi,Gabriella;Vianello,Paola;Vulpetti,Anna;Ciomei,Marina[JournalofMedicinalChemistry,2009,vol.52,#16,p.5152-5163]

[1]CurrentPatentAssignee:NERVIANOMEDICALSCIENCESS.R.L.-WO2010/125004,2010,A1Locationinpatent:Page/Pagecolumn14

[1]CurrentPatentAssignee:NERVIANOMEDICALSCIENCESS.R.L.-WO2010/125004,2010,A1Locationinpatent:Page/Pagecolumn13-14

Literature

Title: Phase I study of the safety, tolerability and pharmacokinetics of PHA-848125AC, a dual tropomyosin receptor kinase A and cyclin-dependent kinase inhibitor, in patients with advanced solid malignancies.

Journal: Investigational new drugs 20121201

Title: Down-regulation of the PTTG1 proto-oncogene contributes to the melanoma suppressive effects of the cyclin-dependent kinase inhibitor PHA-848125.

Journal: Biochemical pharmacology 20120901

Title: Dual targeting of CDK and tropomyosin receptor kinase families by the oral inhibitor PHA-848125, an agent with broad-spectrum antitumor efficacy.

Journal: Molecular cancer therapeutics 20100801

Title: The cyclin-dependent kinase inhibitor PHA-848125 suppresses the in vitro growth of human melanomas sensitive or resistant to temozolomide, and shows synergistic effects in combination with this triazene compound.

Journal: Pharmacological research 20100501

Title: Efficacy of PHA-848125, a cyclin-dependent kinase inhibitor, on the K-Ras(G12D)LA2 lung adenocarcinoma transgenic mouse model: evaluation by multimodality imaging.

Journal: Molecular cancer therapeutics 20100301

Title: Identification of N,1,4,4-tetramethyl-8-{[4-(4-methylpiperazin-1-yl)phenyl]amino}-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide (PHA-848125), a potent, orally available cyclin dependent kinase inhibitor.

Journal: Journal of medicinal chemistry 20090827

Title: Caporali S, Alvino E, Levati L, Esposito AI, Ciomei M, Brasca MG, Del Bufalo D, Desideri M, Bonmassar E, Pfeffer U, D'Atri S.Down-regulation of the PTTG1 proto-oncogene contributes to the melanoma suppressive effects of the cyclin-dependent kinase inhibitor PHA-848125.Biochem Pharmacol. 2012 Sep 1;84(5):598-611.

Title: Albanese C, Alzani R, Amboldi N, Avanzi N, Ballinari D, Brasca MG, Festuccia C, Fiorentini F, Locatelli G, Pastori W, Patton V, Roletto F, Colotta F, Galvani A, Isacchi A, Moll J, Pesenti E, Mercurio C, Ciomei M.Dual targeting of CDK and tropomyosin receptor kinase families by the oral inhibitor PHA-848125, an agent with broad-spectrum antitumor efficacy.Mol Cancer Ther. 2010 Aug;9(8):2243-54.

Title: Degrassi A, et al.Efficacy of PHA-848125, a cyclin-dependent kinase inhibitor, on the K-Ras(G12D)LA2 lung adenocarcinoma transgenic mouse model: evaluation by multimodality imaging.Mol Cancer Ther. 2010 Mar;9(3):673-81.

Title: Brasca, M.G., et al. Identification of N,1,4,4-tetramethyl-8-{-(4-methylpiperazin-1-yl)phenylamino}-4,5-dihydro-1H-pyrazolo,3-hquinazoline-3-carboxamide (PHA-848125), a potent, orally available cyclin dependent kinase inhibitor. J. Med. Chem. 52(16), 5152-5163 (2009).

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