QL-X-138 is a potent and selective BTK/MNK dual kinase inhibitor, exhibits covalent binding to BTK and non-covalent binding to MNK. QL-X-138 shows IC 50 s of 9.4 nM, 107.4 nM and 26 nM for BTK, MNK1 and MNK2 kinases respectively. QL-X-138 also shows anti- dengue virus 2 activity, with an IC 50 of 3.5 μM. QL-X-138 can be used for the research of B-cell malignancies.

QL-X-138 (72 h) exhibits anti-proliferation activity against lymphoma and leukemia cell lines, with an GI 50 s 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 (EC 50 =11 nM). Strongly blocked phosphorylation of the BTK downstream target PLCγ2 Y1217 (EC 50 =57 nM). Suppressed the phosphorylation of the MNK downstream target eIF4E S209 at a concentration of 1 μM.

1469988-63-3

C25H19N5O2

421.46

QL-X-138

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years