1197958-53-4

1197958-53-4 structure

Name: ALK-IN-12
Chemical Name: AP26113
CAS Number: 1197958-53-4
Molecular Formula: C₂₄H₃₀ClN₆O₂P
Molecular Weight: 501.0
Catalog: Signaling Pathways Protein Tyrosine Kinase/RTK ALK
Create Date: 2018-06-28 17:43:02
Modify Date: 2026-07-17 06:14:00
ALK-IN-12 is a potent and orally active ALK inhibitor with an IC50 of 0.18 nM. ALK-IN-12 also inhibits IGF1R and InsR (IC50=20.3 and 90.6 nM). Antitumor activities[1].

Name	AP26113

Description	ALK-IN-12 is a potent and orally active ALK inhibitor with an IC50 of 0.18 nM. ALK-IN-12 also inhibits IGF1R and InsR (IC50=20.3 and 90.6 nM). Antitumor activities[1].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> Protein Tyrosine Kinase/RTK >> ALK
In Vitro	ALK-IN-12 (compound 11e) effectively inhibits viability of the Karpas-299 ALCL cell line with an IC50 of 28.3 nM[1].
In Vivo	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 AUC0-∞, CL, t1/2 and Vss 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 Cmax, AUC0-∞, tmax, t1/2 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).
References	[1]. Huang WS, et al. Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase. J Med Chem. 2016;59(10):4948-4964.