| Identification | Back Directory | [Name]
1H-Indole-3-carboxamide, 6-[[5-chloro-4-[[2-[(methylamino)carbonyl]phenyl]amino]-2-pyrimidinyl]amino]-N,N,2-trimethyl- | [CAS]
2468219-09-0 | [Synonyms]
ALK-IN-22
1H-Indole-3-carboxamide, 6-[[5-chloro-4-[[2-[(methylamino)carbonyl]phenyl]amino]-2-pyrimidinyl]amino]-N,N,2-trimethyl- | [Molecular Formula]
C24H24ClN7O2 | [MOL File]
2468219-09-0.mol | [Molecular Weight]
477.95 |
| Hazard Information | Back Directory | [Uses]
ALK-IN-22 (compound I-24) is a potent ALK inhibitor with IC50 values of 2.3, 3.7 and 2.9 nM for ALK, ALKL1196M and ALKG1202R, respectively. ALK-IN-22 down-regulated the phosphorylation of ALK and its downstream proteins. ALK-IN-22 induces apoptosis. ALK-IN-22 can be used for tumor research[1]. | [in vivo]
ALK-IN-22 (compound I-24) (25-50 mg/kg; i.g.; Twice daily, for 14 days) has antitumor efficacy in vivo[1].
ALK-IN-22 (compound I-24) (10 mg/kg; p.o.) shows the Cmax and t1/2 values of 345.7 ng/mL and 4.1 hours, respectively[1].
ALK-IN-22 (compound I-24) (2 mg/kg; i.v.) shows the CL and t1/2 values of 36.2 mL/min/kg and 2.5 hours, respectively[1]. | Animal Model: | Female BALB / c nude mice[1] | | Dosage: | 25 and 50 mg/kg | | Administration: | Intragastric; Twice daily, for 14 days. | | Result: | The tumor growth inhibition (TGI) value of 50 mg/kg reached 93.5%. |
| Animal Model: | SD rats[1] | | Dosage: | 2 and 10 mg/kg (Pharmacokinetic Analysis) | | Administration: | Oral administration and intravenous injection | | Result: | 1.19| Parameter | F16 | VP-16 | | Dose (i.v.) mg/kg | 10 | 10 | | Cmax (ng/mL) | 26952 | 17712 | | Tmax (min) | 5 | 5 | | AUCplasma (min*ng/mL) | 2878363 | 409528 | | T1/2 (min) | 151 | 45 | | Vd (L/Kg) | 0.2341 | 0.432 | | CL (L/min/kg) | 0.001 | 0.007 |
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| [References]
[1] Thacker PS, et al. Synthesis and biological evaluation of some coumarin hybrids as selective carbonic anhydrase IX and XII inhibitors. Bioorg Chem. 2020 Nov;104:104272. DOI:10.1016/j.bioorg.2020.104272 |
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