AP26113
- CAS No.
- 1197958-53-4
- Chemical Name:
- AP26113
- Synonyms
- ALK-IN-12;5-Chloro-N4-[2-(dimethylphosphinyl)phenyl]-N2-[2-methoxy-4-(4-methyl-1-piperazinyl)phenyl]-2,4-pyrimidinediamine;2,4-Pyrimidinediamine, 5-chloro-N4-[2-(dimethylphosphinyl)phenyl]-N2-[2-methoxy-4-(4-methyl-1-piperazinyl)phenyl]-
- CBNumber:
- CB13339849
- Molecular Formula:
- C24H30ClN6O2P
- Molecular Weight:
- 500.96
- MDL Number:
- MOL File:
- 1197958-53-4.mol
- MSDS File:
- SDS
AP26113 Chemical Properties, Uses, Production
Uses
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].
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. DOI:10.1021/acs.jmedchem.6b00306
AP26113 Preparation Products And Raw materials
Raw materials
Preparation Products
AP26113 Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Shanghai Beckham Medical Technology Co., Ltd | 13816613772 | huahero21@sina.com | China | 2994 | 55 |
| BOC Sciences | 16314854226; +8616314854226 | inquiry@bocsci.com | United States | 19852 | 58 |
| Shanghai Merlot Chemical Co., LTD | 15821661757 | 226174156@qq.com | China | 476 | 58 |
| Shanghai jerryxing Biomedical Technology Co., Ltd | 17521512546 17721492509 | 460170712@qq.com | China | 4995 | 58 |
| TargetMol Chemicals Inc. | 15002134094 | marketing@targetmol.cn | China | 29874 | 58 |
