ASP-3026

• CAT Number: I000408
• CAS Number: 1097917-15-1
• Molecular Formula: C₂₉H₄₀N₈O₃S
• Molecular Weight: 580.74
• 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

ASP3026（Cat No.:I000408） is a potent and selective inhibitor of anaplastic lymphoma kinase (ALK), a receptor tyrosine kinase that plays a role in the development of certain cancers. It exhibits strong inhibitory activity against ALK with an IC50 value of 3.5 nM, indicating its high potency in blocking the activity of this target. By specifically targeting ALK, ASP3026 shows potential for the treatment of ALK-positive cancers, including non-small cell lung cancer (NSCLC) and anaplastic large-cell lymphoma (ALCL).

Reference

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 Article2: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 Article3: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 Article4: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 Article5: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