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X-376 is a potent and highly specific ALK small molecule tyrosine kinase inhibitors (TKIs) with IC50 of 0.61 nM. In Ambit kinome screens, cell growth inhibition studies, and surrogate kinase assays, X-376 was more potent inhibitors of ALK but less potent inhibitors of MET compared to PF-02341066. X-376 displayed potent antitumor activity in vivo with favorable pharmacokinetic and toxicity profiles.
Science. 2017 Dec 1;358(6367).
The target landscape of clinical kinase drugs
X-376 purchased from AbMole
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Source | Munich Industrial University (2018). Figure 36. X-376 (AbMole BioScience) |
| Method | Kinase binding of small molecule inhibitors | |
| Cell Lines | BT-474 cells, Caki-1 cells, KM-12 and HEK-293 cells | |
| Concentrations | 1 μM | |
| Incubation Time | 24 h | |
| Results | Notably, the photosensitizing effect of small molecule inhibitors can also be used for photodynamic therapy of cancer. |
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Source | Science (2017). Figure 4. X-376 (Abmole Bioscience) |
| Method | Cell viability and proliferation assays | |
| Cell Lines | A-431 and ACHN cells | |
| Concentrations | 50 nM | |
| Incubation Time | 72 h | |
| Results | Regardless of whether or not EGFR carried an activating mutation, the combination was always more effective in inhibiting cell viability and proliferation than any one drug alone. |
| Molecular Weight | 547.41 |
| Formula | C25H25Cl2FN6O3 |
| CAS Number | 1365267-27-1 |
| Solubility (25°C) | DMSO 90 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related ALK Products |
|---|
| AP26113 (Brigatinib)
AP26113 (Brigatinib) is a highly potent ALK inhibitor with IC50 of 0.6 nM. |
| 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). |
| RepSox (ALK5 Inhibitor II)
RepSox (ALK5 Inhibitor II) is a potent and ATP-competitive inhibitor of the TGF-β type I receptor ALK5 (IC50 values are 0.004 and 0.023 μM for ALK5 autophosphorylation and ALK5 binding respectively). |
| LDN-193189
LDN-193189 is a highly potent small molecule inhibitor of bone morphogenetic protein (BMP) type I receptors ALK2 and ALK3. |
| GSK1838705A
GSK1838705A is a small-molecule kinase inhibitor that inhibits IGF-IR and the insulin receptor with IC50s of 2.0 and 1.6 nmol/L, respectively. |
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