1. Protein Tyrosine Kinase/RTK
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  3. QL-X-138

QL-X-138 

Cat. No.: HY-124645
Handling Instructions

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 IC50s 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 IC50 of 3.5 μM. QL-X-138 can be used for the research of B-cell malignancies.

For research use only. We do not sell to patients.

QL-X-138 Chemical Structure

QL-X-138 Chemical Structure

CAS No. : 1469988-63-3

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Description

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 IC50s 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 IC50 of 3.5 μM. QL-X-138 can be used for the research of B-cell malignancies[1][2].

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

421.45

Formula

C₂₅H₁₉N₅O₂

CAS No.
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QL-X-138
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HY-124645
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