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Inhibitors
| Cat.No. | Name | Information |
|---|---|---|
| M1743 | Ensartinib | Ensartinib (X-396) is a potent and highly specific ALK small molecule tyrosine kinase inhibitor. |
| M1873 | LDN-193189 | LDN-193189 is a highly potent small molecule inhibitor of bone morphogenetic protein (BMP) type I receptors ALK2 and ALK3. |
| M1720 | AP26113 (Brigatinib) | AP26113 (Brigatinib) is a highly potent ALK inhibitor with IC50 of 0.6 nM. |
| M2075 | LDK378 | LDK378 is a highly selective, orally bioavailable ALK inhibitor with IC50 of 0.15 nM. |
| M1794 | SB431542 | SB-431542 is a potent and selective inhibitor of the transforming growth factor-β (TGF-β) type I receptor activin receptor-like kinase ALK5 (IC50 = 94 nM). |
| M21110 | Con B-1 | ConB-1 is a strongly selective ALK inhibitor with low toxicity to normal cells. |
| M20040 | WAY-270947 | WAY-270947 is a ALK5 inhibitor. |
| M14878 | Ensartinib dihydrochloride | Ensartinib dihydrochloride (X-396 dihydrochloride) is a potent and dual ALK/MET inhibitor with IC50s of <0.4 nM and 0.74 nM, respectively. |
| M14877 | ALK inhibitor 1 | ALK inhibitor 1 (compound 17) is a potent pyrimidin ALK inhibitor. ALK inhibitor 1 is a potent inhibitor of testis-specific serine/threonine kinase 2 (TSSK2; IC50=31 nM) and focal adhesion kinase (FAK; IC50=2 nM). |
| M9397 | MS4078 | MS4078 is a PROTAC degrader of ALK which potently decreases cellular levels of oncogenic active ALK fusion proteins in SU-DHL-1 lymphoma and NCI-H2228 lung cancer cells. |
| M6186 | Repotrectinib (TPX-0005) | Repotrectinib (TPX-0005) is a potential best-in-class ALK/ROS1/TRK inhibitor against SRC, wild-type WT ALK, The IC50 values of ALK G1202R and ALK L1196M were 5.3 nM, 1.01 nM, 1.26 nM and 1.08 nM, respectively. |
| M6168 | Ceritinib (LDK378) dihydrochloride | Ceritinib dihydrochloride (LDK378 dihydrochloride) is potent inhibitor against ALK with IC50 of 0.2 nM, shows 40- and 35-fold selectivity against IGF-1R and InsR, respectively. |
| M5613 | Entrectinib (RXDX-101) | Entrectinib (RXDX-101) is an orally bioavailable pan-TrkA/B/C, ROS1 and ALK inhibitor with IC50 ranging between 0.1 and 1.7 nM. |
| M5320 | Crizotinib hydrochloride | Crizotinib is inhibitor of the c-Met kinase and the NPM-ALK. Crizotinib inhibited cell proliferation in ALK-positive ALCL cells (IC50s=30 nM). Crizotinib is useful in treatment of anaplastic large-cell lymphoma. |
| M5309 | ALK-IN-1 | ALK-IN-1 is an analog of AP26113 which is a potent and selective ALK inhibitor. It is also an inhibitor of EGFR. |
| M4984 | CEP-37440 | CEP-37440 is a novel potent and selective Dual FAK/ALK inhibitor with IC50 s of 2.3 nM (FAK) and 120 nM(ALK cellular IC50 in 75% human plasma). |
| M4811 | CH5424802 HCl | CH5424802 HCl is a potent ALK inhibitor with IC50 of 1.9 nM, sensitive to L1196M mutation. |
| M3975 | PF-06463922 | Lorlatinib (PF-06463922) is an oral active, selective, brain osmotic and ATP-competitive ROS1/ALK inhibitor. The Ki of Lorlatinib for ROS1, wild-type ALK and ALKL1196M were <0.025 nM, <0.07 nM and 0.7 nM, respectively. Lorlatinib has anticancer activity. |
| M3889 | LDN-214117 | LDN-214117 is a potent and selective ALK2 inhibitor with IC50 of 22 nM and >100 fold selectivity for ALK5. |
| M3781 | NVP-TAE684 | NVP-TAE684 is a highly potent and selective small-molecule ALK inhibitor, which blocked the growth of ALCL-derived and ALK-dependent cell lines with IC(50) values between 2 and 10 nM. |
| M2859 | ML347 | ML347 is a selective BMP receptor inhibitor with IC50 of 32 nM for ALK2, >300-fold selectivity over ALK3. Also inhibits ALK1 activity with IC50 of 46 nM. |
| M2806 | LDN-212854 | LDN-212854 is a potent and selective BMP receptor inhibitor with IC50 of 1.3 nM for ALK2, about 2-, 66-, 1641-, and 7135-fold selectivity over ALK1, ALK3, ALK4, and ALK5, respectively. |
| M2805 | LDN-193189 Tetrahydrochloride | LDN193189 Tetrahydrochloride is the hydrochloride salt of LDN193189, which is a selective BMP signaling inhibitor, and inhibits the transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 of 5 nM and 30 nM, respectively, 200-fold selectivity for BMP versus TGF-β. |
| M2789 | K02288 | K02288 is a potent, and selective type I BMP receptor inhibitor with IC50 of 1.1, 1.8, 6.4 nM for ALK2, ALK1 and ALK6, showing weaker inhibition on other ALKs (3, 4, 5) and ActRIIA. |
| M2201 | TSR-011 | TSR-011 is a potent, orally available ALK inhibitor. |
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