|4-((3-(2H-1,2,3-三唑-2-基)苯基)氨基)-2-((1R,2S)-2-氨基环己基)氨基)嘧啶-5-甲酰胺盐酸盐|CsnPharm

CAS No.: 1370261-97-4

PRT062607 HCl Catalog No. CSN16941

Synonyms: P505-15 Hydrochloride;P505-15 HCl;BIIB-057 HCl

PRT062607 HCl is an inhibitor of SYK with IC50 of 1 nM.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 Syk

IC50:1nM
描述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.
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
C57BL/6 mouse bone marrow cells	-	Cytotoxic assay	5 h	Cytotoxicity against C57BL/6 mouse bone marrow cells assessed as growth inhibition preincubated for 4 days followed by [3H]-thymidine addition measured after 5 hrs by betaplate counting analysis, IC50=5.853 μM	25633741
CHO cells	-	Function assay	-	Inhibition of human ERG expressed in CHO cells by automated Qpatch clamp assay, IC50=8.6 μM	25633741
human Ramos cells	-	Function assay	-	Inhibition of SYK in human Ramos cells, IC50=0.223 μM	23350847

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.3261 mL
- 11.6304 mL
- 23.2609 mL
- 5 mM
- 0.4652 mL
- 2.3261 mL
- 4.6522 mL
- 10 mM
- 0.2326 mL
- 1.1630 mL
- 2.3261 mL

技术信息

CAS号

1370261-97-4

储存条件

粉末: Keep in dark place,Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H24ClN9O

运输

蓝冰

分子量

429.91

别名

P505-15 Hydrochloride;P505-15 HCl;BIIB-057 HCl;PRT-2607;PRT-062607;BIIB-057;P-505-15

溶解度

DMSO	300.0 mg/mL (697.8 mM) warming
Water	120.0 mg/mL (279.1 mM) warming

动物实验配方

0.5% CMC-Na

30 mg/mL

suspension

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