Belizatinib, formerly known as TSR-011, is a potent, orally bioavailable dual inhibitor of ALK (anaplastic lymphoma kinase) with IC50 of 0.7 nM and an inhibitor of tropomyosin receptor kinase (TRK) with IC50 values less than 3 nM for TRK A, B, and C. Belizatinib has high affinity for wild-type recombinant ALK kinase which is overexpressed in some tumors, therefore, belizatinib has potential anticancer activity by disrupting the ALK- and TRK-mediated signaling transduction and suppressing tumor cell growth in ALK/TRK-overexpressing tumor cells.
理化性质和储存条件
| Molecular Weight (MW) | 577.73 |
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| Formula | C33H44FN5O3 |
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| CAS No. | 1357920-84-3 |
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| Storage | -20℃ for 3 years in powder form |
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| -80℃ for 2 years in solvent |
| Solubility (In vitro) | DMSO: 100 mg/mL (173.1 mM) |
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| Water: <1 mg/mL |
| Ethanol: 100 mg/mL (173.1 mM) |
| SMILES | O=C(NC1=NC2=CC=C(CN3CCC(C(C)(O)C)CC3)C=C2N1[C@H]4CC[C@@H](C(NC(C)C)=O)CC4)C5=C C=C(F)C=C5 |
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| Synonyms | TSR-011; TSR011; TSR 011; Belizatinib |
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实验参考方法
| In Vitro | In vitro activity: Belizatinib, formerly known as TSR-011, is a potent, orally bioavailable dual inhibitor of ALK (anaplastic lymphoma kinase) with IC50 of 0.7 nM and an inhibitor of tropomyosin receptor kinase (TRK) with IC50 values less than 3 nM for TRK A, B, and C. Belizatinib has high affinity for wild-type recombinant ALK kinase which is overexpressed in some tumors, therefore, belizatinib has potential anticancer activity by disrupting the ALK- and TRK-mediated signaling transduction and suppressing tumor cell growth in ALK/TRK-overexpressing tumor cells. TSR-011 has high affinity for wild-type recombinant ALK kinase activity, with an IC50 value of 0.7 nM and inhibits tropomyosin receptor kinase (TRK) A, B, and C (IC50 < 3nM).
Kinase Assay: belizatinib is a potent inhibitor of ALK with IC50 of 0.7 nM and an inhibitor of tropomyosin receptor kinase (TRK) with IC50 values less than 3 nM for TRK A, B, and C.
Cell Assay: |
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| In Vivo | TSR-011 displayed potent inhibition of ALK-dependent tumor growth in mouse models and is well-tolerated. |
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| References | Ther Adv Med Oncol, 2016 Jan;8(1):32-47; GJ Weiss, et al. Journal of clinical oncology. 2014. |
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