ALK-IN-12 is a potent and orally active ALK inhibitor with an IC 50 of 0.18 nM. ALK-IN-12 also inhibits IGF1R and InsR (IC 50 =20.3 and 90.6 nM). Antitumor activities.

ALK-IN-12 (compound 11e) effectively inhibits viability of the Karpas-299 ALCL cell line with an IC 50 of 28.3 nM[1].

ALK-IN-12 (10-50 mg/kg; orally; once daily for 13 consecutive days) shows dose-dependent antitumor activity[1]. ALK-IN-12 (3 mg/kg; i.v.; 6-8 week old female CD rats ) treatment shows AUC 0-∞ , CL, t 1/2 and V ss are 3039 ng?h/mL, 0.91 h?kg, 6.6 hours and 6.12 L/kg, respectively[1]. ALK-IN-12 (10 mg/kg; p.o.; 6-8 week old female CD rats) treatment shows C max , AUC 0-∞ , t max , t 1/2 and F are 3254 ng/mL, 4056 ng?h/mL, 6.0 hours, 12.5 hours and 39%, respectively[1]. Animal Model: Eight- to 10-week old female SCID/beige mice (Karpas-299 xenograft mouse model expressing the NPM-ALK fusion)[1]Dosage: 10-50 mg/kg Administration: Orally; once daily for 13 consecutive days Result: Dose-dependent antitumor activity. Led to tumor stasis (50 mg/kg dose).

1197958-53-4

C24H30ClN6O2P

500.96

ALK-IN-12

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years