For research use only, not for therapeutic use.
ASP-3026（Cat No.:I000408）is a selective inhibitor of the anaplastic lymphoma kinase (ALK) and c-Met, key drivers of tumor growth and survival in various cancers, particularly non-small cell lung cancer (NSCLC) with ALK rearrangements. By targeting these kinases, ASP-3026 inhibits abnormal signaling pathways involved in cancer cell proliferation and metastasis. Its specificity for ALK, along with its ability to cross the blood-brain barrier, makes it a valuable compound for treating ALK-positive cancers, including those with brain metastases. ASP-3026 holds potential for advancing targeted cancer therapies and overcoming drug resistance.
| Catalog Number | I000408 |
| CAS Number | 1097917-15-1 |
| Synonyms | 2-N-[2-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl]-4-N-(2-propan-2-ylsulfonylphenyl)-1,3,5-triazine-2,4-diamine |
| Molecular Formula | C₂₉H₄₀N₈O₃S |
| Purity | ≥95% |
| Target | ALK |
| Solubility | in DMSO > 10 mM |
| Storage | Store at -20°C |
| IC50 | 3.5 nM |
| IUPAC Name | 2-N-[2-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl]-4-N-(2-propan-2-ylsulfonylphenyl)-1,3,5-triazine-2,4-diamine |
| InChI | InChI=1S/C29H40N8O3S/c1-21(2)41(38,39)27-8-6-5-7-25(27)33-29-31-20-30-28(34-29)32-24-10-9-23(19-26(24)40-4)36-13-11-22(12-14-36)37-17-15-35(3)16-18-37/h5-10,19-22H,11-18H2,1-4H3,(H2,30,31,32,33,34) |
| InChIKey | MGGBYMDAPCCKCT-UHFFFAOYSA-N |
| SMILES | CC(C)S(=O)(=O)C1=CC=CC=C1NC2=NC(=NC=N2)NC3=C(C=C(C=C3)N4CCC(CC4)N5CCN(CC5)C)OC |
| Reference | </br>1:First-in-human, open-label dose-escalation and dose-expansion study of the safety, pharmacokinetics, and antitumor effects of an oral ALK inhibitor ASP3026 in patients with advanced solid tumors. Li T, LoRusso P, Maitland ML, Ou SH, Bahceci E, Ball HA, Park JW, Yuen G, Tolcher A.J Hematol Oncol. 2016 Mar 10;9:23. doi: 10.1186/s13045-016-0254-5. PMID: 26966027 Free PMC Article</br>2:Characterization and Thermodynamic Stability of Polymorphs of Di(arylamino) Aryl Compound ASP3026. Takeguchi K, Hirakura Y, Yamazaki K, Shimada I, Ieda S, Okada M, Takiyama H.Chem Pharm Bull (Tokyo). 2015;63(6):418-22. doi: 10.1248/cpb.c14-00774. PMID: 26027465 Free Article</br>3:NPM/ALK mutants resistant to ASP3026 display variable sensitivity to alternative ALK inhibitors but succumb to the novel compound PF-06463922. Mologni L, Ceccon M, Pirola A, Chiriano G, Piazza R, Scapozza L, Gambacorti-Passerini C.Oncotarget. 2015 Mar 20;6(8):5720-34. PMID: 25749034 Free PMC Article</br>4:The ALK inhibitor ASP3026 eradicates NPM-ALK⁺ T-cell anaplastic large-cell lymphoma in vitro and in a systemic xenograft lymphoma model. George SK, Vishwamitra D, Manshouri R, Shi P, Amin HM.Oncotarget. 2014 Jul 30;5(14):5750-63. PMID: 25026277 Free PMC Article</br>5:The selective anaplastic lymphoma receptor tyrosine kinase inhibitor ASP3026 induces tumor regression and prolongs survival in non-small cell lung cancer model mice. Mori M, Ueno Y, Konagai S, Fushiki H, Shimada I, Kondoh Y, Saito R, Mori K, Shindou N, Soga T, Sakagami H, Furutani T, Doihara H, Kudoh M, Kuromitsu S.Mol Cancer Ther. 2014 Feb;13(2):329-40. doi: 10.1158/1535-7163.MCT-13-0395. Epub 2014 Jan 13. PMID: 24419060 Free Article |
