TRK-IN-21 (5n) 是一种具有口服活性的TRK抑制剂。TRK-IN-21 抑制 TRKAWT，TRKAG667C，TRKAF589L和 TRKAG595， 其IC50值分别为 0.3，2.3，0.4 和 0.5 nM。TRK-IN-21 可以用于癌症的研究。
| 生物活性 | TRK-IN-21 (5n) is an orally activityTRKinhibitor. TRK-IN-21 inhibitsTRKAWT,TRKAG667C,TRKAF589L, andTRKAG595withIC50s of 0.3, 2.3, 0.4 and 0.5 nM, respectively. TRK-IN-21 can be used for the research ofcancer[1]. |
| IC50& Target | IC50: 0.3 nM (TRKAWT), 2.3 nM (TRKAG667C), 0.4 nM (TRKAF589L), 0.5 nM (TRKAG595)[1] |
体内研究
(In Vivo) | TRK-IN-21 (30-100 mg/kg; p.o. twice daily for 11-14 days) inhibits tumor growth in Ba/F3-TRKA xenograft models[1]. 1.19Pharmacokinetic Properties of TRK-IN-21 in Rats and Dogs[1]. | Rats
IV 1 mg/kg | Rats
IV 5 mg/kg | Dogs
IV 2 mg/kg | Dogs
PO 10 mg/kg | | Cmax(ng/mL) | 231.2 | 93.5 | 1063.8 | 2070.1 | | Tmax(h) | 0.1 | 1.7 | | 0.3 | | AUClast(ng·h/mL) | 456.1 | 588.6 | 6923.0 | 24305.2 | | CL (L/h/kg) | 2.1 | 8.0 | 0.2 | 0.3 | | T1/2(h) | 2.2 | 2.2 | 15.2 | 15.3 | | Vz (L/kg) | 6.7 | 25.7 | 4.2 | 6.2 | | MRT (h) | 2.5 | 4.0 | 8.2 | 8.8 | | F (%) | | 26 | 30.2 | 71 |
| Animal Model: | 6-week-old BALB/cA nude mice with Ba/F3-TRKA xenografts[1] | | Dosage: | 30 and 100 mg/kg | | Administration: | Oral gavage; 30 and 100 mg/kg twice daily; for 11-14 days | | Result: | Dose-dependently inhibited BaF3-TMP3-TRKAWT-transfected tumor progression with a tumor growth inhibition value of 97%, showed a better potency to larotrectinib at the same dosage. Inhibited BaF3-LMNA-TrkAG667C-transfected tumor progression with a tumor growth inhibition value of 73%, showed a better potency to selitrectinib at the same dosage. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
