产品资料

MedKoo Biosciences/P505-15 hydrochloride/406272/1g

P505-15, also known as PRT2607, PRT062607, and BIIB057, is a novel, highly selective, and orally bioavailable small molecule SYK inhibitor (SYK IC(50) = 1 nM) with anti-SYK activity that is at least 80-fold greater than its affinity for other kinases. P505-15 successfully inhibited SYK-mediated B-cell receptor signaling and decreased cell viability in NHL and CLL.

MedKoo Cat#: 406272
Name: P505-15 hydrochloride
CAS#: 1370261-97-4 (HCl)
Chemical Formula: C19H24ClN9O
Exact Mass: 393.20256
Molecular Weight: 429.913
Elemental Analysis: C, 53.08; H, 5.63; Cl, 8.25; N, 29.32; O, 3.72

Related CAS #: 1370261-97-4 (HCl) 1370261-96-3 (free base)

Synonym: PRT2607; PRT-2607; PRT 2607; PRT062607; PRT-062607; PRT 062607; P-505-15; P 505-15; P505-15; BIIB057; BIIB-057; BIIB 057.

IUPAC/Chemical Name: 4-((3-(2H-1,2,3-triazol-2-yl)phenyl)amino)-2-(((1R,2S)-2-aminocyclohexyl)amino)pyrimidine-5-carboxamide hydrochloride

InChi Key: RMNLLPXCNDZJMJ-IDVLALEDSA-N

InChi Code: InChI=1S/C19H23N9O.ClH/c20-15-6-1-2-7-16(15)26-19-22-11-14(17(21)29)18(27-19)25-12-4-3-5-13(10-12)28-23-8-9-24-28;/h4-5,8-11,15-16H,1-2,6-7,20H2,(H2,21,29)(H2,22,25,26,27);1H/t15-,16+;/m0./s1

SMILES Code: O=C(C1=CN=C(N[C@H]2[C@@H](N)CCCC2)N=C1NC3=CC=CC(N4N=CC=N4)=C3)N.[H]Cl

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, not in water

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).

Harmonized System Code:

293490

Additional Information

References

1: Spurgeon SE, Coffey G, Fletcher LB, Burke R, Tyner JW, Druker BJ, Betz A, DeGuzman F, Pak Y, Baker D, Pandey A, Hollenbach SJ, Sinha U, Loriaux MM. The selective SYK inhibitor P505-15 (PRT062607) inhibits B cell signaling and function in vitro and in vivo and augments the activity of fludarabine in chronic lymphocytic leukemia. J Pharmacol Exp Ther. 2013 Feb;344(2):378-87. doi: 10.1124/jpet.112.200832. Epub 2012 Dec 7. PubMed PMID: 23220742; PubMed Central PMCID: PMC3558816.

2: Hoellenriegel J, Coffey GP, Sinha U, Pandey A, Sivina M, Ferrajoli A, Ravandi F, Wierda WG, O'Brien S, Keating MJ, Burger JA. Selective, novel spleen tyrosine kinase (Syk) inhibitors suppress chronic lymphocytic leukemia B-cell activation and migration. Leukemia. 2012 Jul;26(7):1576-83. doi: 10.1038/leu.2012.24. Epub 2012 Feb 7. PubMed PMID: 22362000.

3: Coffey G, DeGuzman F, Inagaki M, Pak Y, Delaney SM, Ives D, Betz A, Jia ZJ, Pandey A, Baker D, Hollenbach SJ, Phillips DR, Sinha U. Specific inhibition of spleen tyrosine kinase suppresses leukocyte immune function and inflammation in animal models of rheumatoid arthritis. J Pharmacol Exp Ther. 2012 Feb;340(2):350-9. doi: 10.1124/jpet.111.188441. Epub 2011 Oct 31. PubMed PMID: 22040680.

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MedKoo Biosciences/P505-15 hydrochloride/406272/1g

Technical Data

Additional Information

References