SU 5402 - CAS:215543-92-3 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	SU 5402
英文名称:	SU 5402
别名:	SU 5402 3-[4-Methyl-2-(2-oxo-1,2-dihydro-indol-3-ylidenemethyl)-1H-pyrrol-3-yl]-propionic acid
CAS No:	215543-92-3	分子式:	C₁₇H₁₆N₂O₃	分子量:	296.32054
CAS No:	215543-92-3
分子式:	C₁₇H₁₆N₂O₃
分子量:	296.32054

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S11101 SU 5402 ≥98% (psaitong)

相关产品

包装规格：

5mg 25mg 100mg in glass bottle

溶解性：

溶于DMSO（≥30mg/mL）

产品描述：

基本信息

产品编号：S11101
产品名称：SU 5402
CAS:	215543-92-3	储存条件	粉末	-20℃	四年

分子式：	C17H16N2O3		溶于液体	-80℃	六个月
分子量	296.32			-20℃	一个月
化学名：
Solubility (25°C)	体外	DMSO	59mg/mL (199.1mM)
		Ethanol	Insoluble
		Water	Insoluble
	体内（现配现用）
＜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	3.3747mL	16.8737mL	33.7473mL
5mM	0.6749mL	3.3747mL	6.7495mL
10mM	0.3375mL	1.6874mL	3.3747mL
50mM	0.0675mL	0.3375mL	0.6749mL

生物活性

产品描述	一种有效的多靶点受体酪氨酸激酶抑制剂，作用于 VEGFR2，FGFR1 和 PDGFRβ，IC50 分别为 20nM，30nM 和 510nM。
靶点/IC₅₀	VEGFR2 (Cell-free assay)	FGFR1 (Cell-free assay)	PDGFRβ (Cell-free assay)
	20nM	30nM	510nM
体外研究	SU 5402 is cocrystallized with the catalytic domain of FGF-R1 (flg-1) and is found to inhibit yrosine phosphorylation of VEGFR2 (Flk-1/KDR) and PDGF-R in NIH 3T3 cells with IC50 values of 0.4 and 60.9μM, respectively[1]. In order to investigate whether phosphorylation of PKM2 and LDHA is mediated in FGFR1-specific manner, FTC-133 are treated with receptor tyrosine kinase inhibitors Dovitinib and SU 5402 (SU-5402). Dovitinib treatment results in significant decrease of phosphorylation status at a concentration of 100nM after four hours of incubation for both PKM2 and LDHA. No significant changes are seen when administered at concentrations of 1nM and 10nM. SU 5402 administration leads to a sigificant decrease of PKM2 and LDHA phosphorylation at a concentration of 20μM.
体内研究	Inhibition of FGFR1 with SU 5402 (SU5402) administered to ΔF508-CFTR homozygous mice results in partial ΔF508-CFTR.rescue, as shown by an increase in saliva secretion, a surrogate "sweat test" assay in mice. As salivary secretion is often sex dependent, only male mice are chosen for these experiments. Our results indicate that treatment of the ΔF508-CFTR mice with SU 5402 restores the saliva secretion level to ~10% of that observed for the wild-type CFTR mice, which suggests that SU 5402 can have therapeutic benefits to Cystic Fibrosis (CF). The selective FGFR1 inhibitor SU 5402 (SU5402) prevents and/or reverses PH induced by MCT (monocrotaline) in rats. In rats treated with SU 5402 on days 21 to 42 after the MCT injection, evaluations on day 42 show marked decreases in pulmonary artery pressure (PAP), RV/(LV+S), and distal artery muscularization compare with rats treated with the vehicle (saline).

推荐实验方法(仅供参考)

细胞实验:

8505C and FTC133 cells are grown in DMEM/F12 suppplemented with 10% FCS and 1% PenStrep and incubated at 37℃, 5% CO2. For B-CPAP RPMI 1640 medium is used. FGFR1 inhibition experiments are performed on FTC133 cells by employment of Receptor Tyrosine Kinase Inhibitors TKI-258 (Dovitinib) and SU 5402 (20μM). Inhibition is conducted over 4h with the indicated inhibitor concentrations. Control cells receive corresponding concentrations of DMSO.

动物实验:

Rats

To assess the potential effects of the FGFR1 inhibitor SU 5402 on established PH, adult male Wistar rats (200-250g) are given MCT (60mg/kg s.c.), left untreated for 21 days, then randomly divided into 2 groups (10 animals in each group), of which one is treated with SU 5402 (25mg/kg/day) and the other given the vehicle, from day 21 to day 42. All treatments are given once a day by s.c. injection.

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