QL-X-138

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

QL-X-138 是一种选择性、有效的 BTK/MNK 双激酶抑制剂，对 BTK、MNK1 和 MNK2 的 IC50 分别为 8、107.4 和 26 nM。

QL-X-138 is a selective and potent BTK/MNK dual kinase inhibitor with IC50 of 8, 107.4, and 26 nM for BTK, MNK1, and MNK2, respectively; exhibits covalent binding to BTK and noncovalent binding to MNK; enhances the antiproliferative efficacies in vitro against a variety of B-cell cancer cell lines, as well as AML and CLL primary patient cells; arrests cell cycle progression and strongly induces apoptosis.

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.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.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.QL-X-138 (3-10000 nM; 4 h) blocks BTK- and MNK-mediated signaling in lymphoma and leukemia cell. Western Blot Analysis 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.

——

——

MAPK/ERK Signaling

MNK

MNK

——

——

1469988-63-3

421.46

C25H19N5O2

>98% (HPLC)

——

——

N-[2-Methyl-5-[2-oxo-9-(1H-pyrazol-4-yl)benzo[h]-1,6-naphthyridin-1(2H)-yl]phenyl]-2-propenamide

(-20℃)

With Ice Pack

≥ 2 years