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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.
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Application | Cell viability and proliferation assays |
| 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. |
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Application | Kinase binding of small molecule inhibitors |
| Results | Notably, the photosensitizing effect of small molecule inhibitors can also be used for photodynamic therapy of cancer. |
| 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 |
| Best-selling ALK Products |
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| 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). |
| LDN-193189
LDN-193189 is a highly potent small molecule inhibitor of bone morphogenetic protein (BMP) type I receptors ALK2 and ALK3. |
| ASP3026
ASP3026 is a selective and oral active anaplastic lymphoma kinase (ALK) inhibitor with a IC50 value of 3.5 nM. ASP3026 can inhibit the phosphorylation of IGF-1R, STAT3, AKT and JNK proteins, and induce the cleavage of caspase 3 and PARP. It also inhibited ROS and ACK. |
| LDK378
Ceritinib (LDK378) is a highly selective, orally bioavailable ALK inhibitor with IC50 of 0.15 nM. |
| LDN-193189 dihydrochloride
LDN-193189 dihydrochloride 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. |
| Other ALK Products |
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| RepSox
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). |
| 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. |
| Alectinib
Alectinib (CH5424802) is a highly selective, orally active and potent ALK inhibitor with IC50 of 1.9 nM. Alectinib (CH5424802) also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively. Alectinib demonstrates effective central nervous system (CNS) penetration. |
| CEP-28122
CEP-28122 is a highly potent and selective orally active ALK inhibitor. |
| AZD3463
AZD3463 is a novel ALK/IGF1R inhibitor with IC50 value of 22 nM. |
| UK 383367
UK 383367 is a potent and selective BMP-1 (procollagen C-proteinase; PCP) inhibitor with IC50 of 44 nM. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
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