[CAS NO. 1370261-97-4] PRT062607 (P505-15) HCl

Name: PRT062607 (P505-15) HCl
Brand: Arctom Scientific
SKU: SLK-S8032

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PRODUCTS SPECIFICATIONS [1370261-97-4]

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Catalog

SLK-S8032

Brand

Selleck

CAS

1370261-97-4

DESCRIPTION [1370261-97-4]

Overview

MDL	MFCD25976708
Molecular Weight	429.91
Molecular Formula	C19H23N9O.HCl
SMILES	N(C=1C(C(N)=O)=CN=C(N[C@H]2[C@@H](N)CCCC2)N1)C3=CC(=CC=C3)N4N=CC=N4.Cl

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	2.3261 mL	11.6303 mL	23.2607 mL
5 mM	0.4652 mL	2.3261 mL	4.6521 mL
10 mM	0.2326 mL	1.1630 mL	2.3261 mL
50 mM	0.0465 mL	0.2326 mL	0.4652 mL

Description

PRT062607 (P505-15, BIIB057, PRT-2607) HCl is a novel, highly selective inhibitor with of 1 nM in cell-free assays, >80-fold selective for Syk than Fgr, PAK5, Lyn, FAK, Pyk2, FLT3, MLK1 and Zap70.

Targets

In vitro

PRT062607(P505-15) anti-SYK activity is at least 80-fold greater than its affinity for other kinases. at least 80-fold greater than its affinity for other kinases. PRT062607 potently inhibits B cell antigen receptor-mediated B cell signaling and activation (IC50 0.27 and 0.28 μM, respectively) and Fcε receptor 1-mediated basophil degranulation (IC50 0.15 μM). PRT062607 inhibits BCR-dependent secretion of the chemokines CCL3 and CCL4 by CLL cells, and leukemia cell migration toward the tissue homing chemokines CXCL12, CXCL13, and beneath stromal cells. PRT062607 furthermore inhibits Syk and extracellular signal-regulated kinase phosphorylation after BCR triggering.

In vivo

The pharmacokinetic/pharmacodynamic relationship predicted that 70% Syk suppression is maintained in mice over a 24h period after 30 mg/kg dosing. At 15 mg/kg, Syk inhibition ranges from 7.5% (Cmin) to 78.4% (Cmax) with an average inhibition of 67% over 24 h. Oral administration of PRT062607 produced dose-dependent anti-inflammatory activity in two rodent models of rheumatoid arthritis. Statistically significant efficacy is observed at concentrations that specifically suppressed Syk activity by 67%.

References

[1] Coffey G, et al. J Pharmacol Exp Ther, 2012, 340(2), 350-359.
[2] Hoellenriegel J, et al. Leukemia, 2012, 26(7), 1576-1583.

Synonyms

5-Pyrimidinecarboxamide, 2-[[(1R,2S)-2-aminocyclohexyl]amino]-4-[[3-(2H-1,2,3-triazol-2-yl)phenyl]amino]-, hydrochloride (1:1)