| Chemical Properties | Back Directory | [density ]
1.402±0.06 g/cm3(Temp: 20 °C; Press: 760 Torr)(predicted) | [form ]
Solid | [pka]
10.83±0.40(predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
CPD-1224 is an orally effective ALK inhibitor, a derivative of an ALK inhibitor that connects to the cereblon ligand. CPD-1224 targets the EML4-ALK oncogenic fusion protein and degrades both ALK and the mutant forms L1196M/G1202R. CPD-1224 can slow down tumor growth[1]. | [in vivo]
CPD-1224 (10 mg/kg, oral) has a 28% oral bioavailability in mice[1].
CPD-1224 (10 mg/kg, oral, twice daily, 15 days) inhibits tumor growth in mice[1]. | Animal Model: | Ba/F3 cell xenograft model in mice[1] | | Dosage: | 10 mg/kg, twice a day, 15 days | | Administration: | Oral | | Result: | Effectively reduced the total ALK and phosphorylated ALK (p-ALK) levels in tumors and inhibited tumor growth. |
| [References]
[1] Gao Y, et al. Catalytic Degraders Effectively Address Kinase Site Mutations in EML4-ALK Oncogenic Fusions. J Med Chem. 2023 Apr 10. DOI:10.1021/acs.jmedchem.2c01864 |
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| Company Name: |
Biorbyt Ltd.
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| Tel: |
+44 (0)1223 859 353 |
| Website: |
http://www.biorbyt.com |
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