PF-4708671 - CAS:1255517-76-0 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	PF-4708671
英文名称:	PF-4708671
别名:	2-[[4-(5-乙基-4-嘧啶基)-1-哌嗪基]甲基]-6-(三氟甲基)-1H-苯并咪唑;PF-4708671 抑制剂;PF-4708671 国华试剂 2-((4-(5-Ethylpyrimidin-4-yl)piperazin-1-yl)methyl)-5-(trifluoromethyl)-1H-benzo[d]imidazole
CAS No:	1255517-76-0	分子式:	C₁₉H₂₁F₃N₆	分子量:	390.41
CAS No:	1255517-76-0
分子式:	C₁₉H₂₁F₃N₆
分子量:	390.41

安全技术说明书(PDF) MSDS(PDF) 点击下载产品说明书(PDF)

P10866 PF-4708671 ≥98% (psaitong)

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包装规格：

10mg 50mg in glass bottle

溶解性：

溶于DMSO（33.33 mg/mL 超声）

产品描述：

基本信息

产品编号：P10866
产品名称：PF-4708671
CAS:	1255517-76-0	储存条件	粉末	-20℃	四年

分子式：	C19H21F3N6		溶于液体	-80℃	两年
分子量	390.41			-20℃	一个月
化学名：	2-((4-(5-Ethylpyrimidin-4-yl)piperazin-1-yl)methyl)-5-(trifluoromethyl)-1H-benzo[d]imidazole
Solubility (25°C)	体外	DMSO	30mg/mL (76.84mM)
		Ethanol	40mg/mL (102.45mM)
		Water	Insoluble
	体内（现配现用）	30% PEG400+0.5% Tween80+5% propylene glycol	30mg/mL
＜1mg/ml表示微溶或不溶。
普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。

制备储备液

浓度溶液体积质量	1mg	5mg	10mg
1mM	2.5614mL	12.8070mL	25.6141mL
5mM	0.5123mL	2.5614mL	5.1228mL
10mM	0.2561mL	1.2807mL	2.5614mL
50mM	0.0512mL	0.2561mL	0.5123mL

生物活性

产品描述	一种有效的细胞渗透性 S6K1 抑制剂，Ki为 20nM，IC50 为 160nM。
靶点/IC₅₀	p70 S6K1 (Cell-free assay) 160nM
体外研究	PF-4708671 inhibits the activity of full-length S6K1 in vitro with a Ki of 20nM, and S6K1 isolated from IGF1-stimulated HEK293 cells with an IC50 of 0.16μM, and only inhibits very weakly the closely related S6K2 isoform (IC50 of 65μM). PF4708671 inhibits RSK1 (IC50 of 4.7μM) and RSK2 (IC50 of 9.2μM) over 20-fold less potently than S6K1. PF4708671 inhibits MSK1 (IC50 of 0.95μM) 4-fold more weakly than S6K1[1]. HCT116 cells are treated with (i) vehicle (DMSO), (ii) OSI-906 (5μM), (iii) PF-4708671 (10μM), and (iv) OSI-906 (5μM)+PF-4708671 (10μM) for various amounts of time. HCT116 cells treated with OSI-906 alone (closed square) or PF4708671 alone (open circle) slightly inhibit cell growth. In contrast, proliferation in HCT116 cells is significantly inhibited after a 2-day treatment with the combination of OSI-906 and PF-4708671 (closed circle). A similar result is also observed when SW480 cells are treated with the combination of OSI-906 and PF-4708671.Colony formation also significantly reduces in OSI-906+PF-4708671-treated cells comparing with vehicle, OSI-906 alone, or PF-4708671 alone treated HCT116 or SW480 cells.
体内研究	The tumor growth rate in mice treated with the combination of OSI-906+PF-4708671 is significantly slower than that of OSI906 alone (P=0.0189) or PF4708671 alone (P=0.0165) treated mice. The average tumor volume in the OSI-906+PF-4708671- treated mice is approximately 50% of that in mice treated with OSI-906 (P=0.0056) or PF-4708671 alone (P<0.001) at the end of a 15-day treatment.

推荐实验方法(仅供参考)

细胞实验：

Cell Assay

GEO, HT29, SW480, and HCT116 cells are used. The effects of OSI-906 or the combination of OSI-906 and PF-4708671 on cell proliferation is determined with XTT and clonogenic assays. XTT assays are performed using the Cell Proliferation Kit II (XTT). For clonogenic assays, cells (1×103 cells/well) are seeded on a 6-well plate and subsequently treated with drugs (OSI906 5μM, PF-4708671 10μM). After 1 week of incubation, cells are stained with 1% crystal violet, and the number of colonies is counted and recorded.

动物实验:

Animal Administration

Mice

Five- to 6-week-old female athymic nude mice (Hsd:Athymic Nude-Foxn1nu) are randomly assigned to the following groups(5 mice/group). For injection of HT29-L and HT29-P cells, mice are treated with vehicle (25mM tartaric acid) or OSI-906 (30mg/kg) for 12 days. For injection of HCT116 cells, mice are treated with (i) vehicle (25mM tartaric acid); (ii) OSI-906 alone (30mg/kg); (iii) PF-4708671 alone (60mg/kg); and (iv) OSI-906 (30mg/kg)+PF-4708671 (60mg/kg) and treated with drugs orally for 14 days. Vehicle and OSI-906 are given once per day and PF-4708671 is given once every other day. Twenty-four hours after the last treatment, the mice are sacrificed and the tumor weights were measured.

保存条件：

-20℃

UN码：

HazardClass：

危害声明：

安全说明：

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参考文献 & 客户发表文献

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

质量 =

浓度 *

体积 *

分子量

*选择对应的单位 *空出希望得到的变量，填写另外两个变量

用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入输出 )

* = *

连续稀释计算器方程

连续稀释
初始浓度:
稀释倍数:

计算结果

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

摩尔浓度计算公式

稀释公式

连续稀释计算器方程

连续稀释

计算结果