KW-2449 - CAS:1000669-72-6 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	KW-2449
英文名称:	KW-2449
别名:	[4-[2-(1H-吲唑-3-基)乙烯基]苯基]-1-哌嗪基甲酮 (E)-(4-(2-(1H-indazol-3-yl)vinyl)phenyl)(piperazin-1-yl)methanone;[4-[(E)-2-(1H-indazol-3-yl)ethenyl]phenyl]-piperazin-1-ylmethanone
CAS No:	1000669-72-6	分子式:	C₂₀H₂₀N₄O	分子量:	332.4
CAS No:	1000669-72-6
分子式:	C₂₀H₂₀N₄O
分子量:	332.4

安全技术说明书(PDF) MSDS(PDF) 点击下载产品说明书(PDF)

K10085 KW-2449 ≥98% (psaitong)

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包装规格：

5mg 25mg 100mg in glass bottle

溶解性：

溶于DMSO（≥50 mg/mL）

产品描述：

基本信息

产品编号：K10085
产品名称：KW-2449
CAS:	1000669-72-6	储存条件	粉末	-20℃	四年

分子式：	C20H20N4O		溶于液体	-80℃	六个月
分子量	332.40			-20℃	一个月
化学名：
Solubility (25°C)	体外	DMSO	67mg/mL (201.56mM)
		Ethanol	67mg/mL (201.56mM)
		Water	Insoluble
	体内（现配现用）	0.5%methylcellulose	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	3.0084mL	15.0421mL	30.0842mL
5mM	0.6017mL	3.0084mL	6.0168mL
10mM	0.3008mL	1.5042mL	3.0084mL
50mM	0.0602mL	0.3008mL	0.6017mL

生物活性

产品描述	一种多靶点激酶抑制剂，对FLT3，ABL，ABLT315I和 Aurora kinase 的 IC50 值分别为6.6，14，4 和 48 nM。
靶点/IC₅₀	FLT3 (D835Y) (Cell-free assay)	Abl (T315I) (Cell-free assay)	FLT3 (Cell-free assay)	Abl (Cell-free assay)	FGFR1 (Cell-free assay)
靶点/IC₅₀	1nM	4nM	6.6nM	14nM	36nM
体外研究	KW-2449 shows growth inhibitory activities against FLT3/ITD-, FLT3/D835Y-, and wt-FLT3/FL-expressing 32D cells, MOLM-13 and MV4;11 with GI50 values of 0.024,0.046, 0.014, 0.024, and 0.011μM, respectively. KW-2449 suppresses the phosphorylations of FLT3 (P-FLT3) and its downstream molecule phospho-STAT5 (P-STAT5) in MOLM-13 cells in a dosedependent manner.KW-2449 increases the percentage of cells in the G1 phase of the cell cycle and reciprocally reduced the percentage of cells in the S phase, resulting in the increase of apoptotic cell population.
体内研究	Oral administration of KW-2449 shows dose-dependent and significant tumor growth inhibition in FLT3-mutated xenograft model with minimum bone marrow suppression. In FLT3 wild-type human leukemia, it induces the reduction of phosphorylated histone H3, G2/M arrest, and apoptosis. In imatinib-resistant leukemia, KW-2449 contributes to release of the resistance by the simultaneous down-regulation of BCR/ABL and Aurora kinases. Furthermore, the antiproliferative activity of KW-2449 is confirmed in primary samples from AML and imatinib-resistant patients.The inhibitory activity of KW2449 is not affected by the presence of human plasma protein, such as α1-acid glycoprotein.

推荐实验方法(仅供参考)

细胞实验:
Cell viability is determined by the sodium 3′-[1-(phenylaminocarbonyl)-3, 4-tetrazolium]-bis (4-methoxy-6-nitro) benzene sulfonic acid hydrate assay after incubation with or without KW-2449 for 72 hours at 37℃. The number of viable cells is determined using the Cell Proliferation Kit II.

动物实验:

Mice: SCID mice are subcutaneously inoculated with MOLM-13 cells. Five days after inoculation, tumor volume is measured using the Antitumor test system II. The 25 mice with tumors ranging from 90 to 130 mm3 are selected and randomized using the Antitumor test system II. From the day of randomization, vehicle (0.5 wt/vol% MC400) or KW-2449 (2.5, 5.0, 10, and 20mg/kg) is orally administered to mice twice a day for 14 days. Tumor volume is measured twice a week during the treatment.

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