KW-2449|1000669-72-6|-陌孚医药/Medlife

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KW-2449

目录号: PL01409 纯度: ≥99%

CAS No. :1000669-72-6

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中文名称	KW-2449
中文别名	[4-[2-(1H-吲唑-3-基)乙烯基]苯基]-1-哌嗪基甲酮;KW2449 抑制剂
英文名称	KW-2449
英文别名	[4-[2-(1H-Indazol-3-yl)ethenyl]phenyl]-1-piperazinylmethanone;(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;KW2449;KW-2449;, KW 2449, KW-2449;cc-533;CHEMBL1908397;KW 2449, KW2449;S2158_Selleck;SureCN1596894;3-[(E)-2-{4-[(PIPERAZIN-1-YL)CARBONYL]PHENYL}ETHENYL]-2H-INDAZOLE;{4-[(E)-2-(1H-Indazol-3-yl)vinyl]phenyl}(1-piperazinyl)methanone;(E)-(4-(2-(1H-indazol-3-yl)vinyl)phenyl)(piperazin-1-yl)methanone;KW2449(E)-(4-(2-(1H-indazol-3-yl)vinyl)phenyl)(piperazin-1-yl)methanonehydrochloride
Cas No.	1000669-72-6
分子式	C₂₀H₂₀N₄O
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

KW-2449是多靶点激酶抑制剂，对FLT3，ABL，ABL^T315I和 Aurora kinase 的 IC₅₀ 值分别为6.6，14，4 和 48 nM。

生物活性

KW-2449 is a multi-targeted kinase inhibitor of FLT3, ABL, ABL and Aurora kinase with IC 50 s of 6.6, 14, 4 and 48 nM, respectively.

性状

Solid

IC50 & Target[1][2]

Abl 4 nM (IC50) ABL-T315I 14 nM (IC50

体外研究(In Vitro)

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 0.011 μM, respectively. KW-2449 suppresses the phosphorylations of FLT3 (P-FLT3) and its downstream molecule phospho-STAT5 (P-STAT5) in MOLM-13 cells in a dose-dependent 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. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

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 KW-2449 is not affected by the presence of human plasma protein, such as α1-acid glycoprotein. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

参考文献

[1]. Shiotsu Y, et al. KW-2449, a novel multikinase inhibitor, suppresses the growth of leukemia cells with FLT3 mutations or T315I-mutated BCR/ABL translocation. Blood. 2009 Aug 20;114(8):1607-17.

溶解度数据	In Vitro: DMSO : ≥ 50 mg/mL (150.42 mM)配制储备液

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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