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QL-X-138
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
QL-X-138图片
CAS NO:1469988-63-3
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
QL-X-138 是一种有效和选择性的BTK/MNK双激酶抑制剂,表现出与 BTK 的共价结合和与 MNK 的非共价结合。QL-X-138 对 BTK、MNK1 和 MNK2 激酶的IC50值分别为 9.4 nM、107.4 nM 和 26 nM。QL-X-138 还显示出抗登革热病毒 2 活性,IC50值为 3.5 μM。QL-X-138 可用于 B 细胞恶性肿瘤的研究。
生物活性

QL-X-138 is a potent and selectiveBTK/MNK dual kinaseinhibitor, exhibits covalent binding toBTKand non-covalent binding toMNK. QL-X-138 showsIC50s of 9.4 nM, 107.4 nM and 26 nM forBTK,MNK1andMNK2kinases respectively. QL-X-138 also shows anti-dengue virus 2activity, with anIC50of 3.5 μM. QL-X-138 can be used for the research of B-cell malignancies[1][2].

体外研究
(In Vitro)

QL-X-138 (72 h) exhibits anti-proliferation activity against lymphoma and leukemia cell lines, with an GI50s of 0.31, 1.2, 0.49,1.4, 0.4, 0.23, 0.95, 1.2, 1.4, 0.23, 1.3, 0.93, 1, and 2.4 μM for TMD8, U2932, Ramos, OCI-AML3, SKM-1, NOMO-1, NB4, HEL, U937, NALM6, MEC-1, MEC-2, Hs 505.T and REC-1 cells, respectively[1].
QL-X-138 (0.5-5 μM; 24-72 h) arrests the progression of Ramos, OCI-AML-3, U937 and U2932 cells cycle in a dose dependent manner[1].
QL-X-138 (0.5-5 μM; 8-72 h) induces apoptosis of Ramos, OCI-AML-3, U937 and U2932 cells in a time- and dose-dependent manner[1].
QL-X-138 (3-10000 nM; 4 h) blocks BTK- and MNK-mediated signaling in lymphoma and leukemia cell[1].

Western Blot Analysis[1]

Cell Line:Ramos, OCI-AML3, U2932, TMD8 and U937 cells
Concentration:3, 10, 30, 100, 300, 1000, 3000, 10000 nM
Incubation Time:4 hours
Result:Significantly suppressed BTK auto-phosphorylation of Y223 (EC50=11 nM).
Strongly blocked phosphorylation of the BTK downstream target PLCγ2 Y1217 (EC50=57 nM).
Suppressed the phosphorylation of the MNK downstream target eIF4E S209 at a concentration of 1 μM.
分子量

421.45

Formula

C25H19N5O2

CAS 号

1469988-63-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.