QL-X-138

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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。

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.