KW-2449

产品编号: DC8522 Featured
KW-2449
结构式
1000669-72-6
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中国地区超过5000个高品质化合物库存
应用领域
KW-2449是多靶点激酶抑制剂,对FLT3,ABL,ABLT315I和 Aurora kinase 的 IC50 值分别为6.6,14,4 和 48 nM。
Cas No.: 1000669-72-6
名称:
别名: KW2449,KW 2449
SMILES: C1CN(CCN1)C(=O)C2=CC=C(C=C2)/C=C/C3=NNC4=CC=CC=C43
分子式: C20H20N4O
分子量: 332.4
纯度:
保存条件: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description:
In Vivo:
In Vitro:
References: KW 2449 is a multikinase inhibitor of FLT3, ABL, ABL-T315I, and Aurora kinase. KW 2449 displays potent inhibition of growth effects on leukemia cells with FLT3 mutations via inhibition of the FLT3 kinase, resulting in the down-regulation of phosphorylated-FLT3/STAT5, G1 arrest, and apoptosis. KW 2449 induces the reduction of phosphorylated histone H3, G2/M arrest, and apoptosis in FLT3 wild-type human leukemia. KW 2449 contributes to release of the resistance by the simultaneous down-regulation of BCR/ABL and Aurora kinases in imatinib-resistant leukemia. KW 2449 inhibitory activity is not affected by the presence of human plasma protein, such as α1-acid glycoprotein. KW 2449 has potent growth inhibitory activity against various types of leukemia by several mechanisms of action. KW 2449 decreases phosphorylation levels of FLT3 and STAT5 in a dose-dependent manner. KW 2449 is a potent inhibitor of ABL-T315I, which is associated with IM resistance (IC50 of 4 nM). KW-2449 has the potent growth inhibitory activities against not only FLT3/ITD-expressing leukemia cells but also FLT3/KDM-activated and wild-type FLT3-overexpressing leukemia cells. 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 can dephosphorylate constitutively active WT-FLT3 kinase but not inhibit the proliferation of leukemia cells if they are not mainly addicted to FLT3 the kinase. KW 2449 mediates cytotoxicity through inhibition of FLT3/ITD. KW 2449 is a direct inhibitor of FLT3 and induces inhibition of its downstream target STAT5. KW 2449 interacts synergistically with HDACIs to induce apoptosis in Ph+ CML cells in a time- and concentration-dependent manner. KW 2449 moderately reduces phosphorylation of histone H3, an indicator of Aurora B activity, in nocodozole-treated K562 cells.
Kinase Assay:
Cell Assay:
Animal Administration:
References:
MSDS
TITLE DOWNLOAD
MSDS_2398_DC8522_1000669-72-6
COA
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产品编号 产品名称 应用领域
DC8522 KW-2449 KW-2449是多靶点激酶抑制剂,对FLT3,ABL,ABLT315I和 Aurora kinase 的 IC50 值分别为6.6,14,4 和 48 nM。