CAS No. : 1097917-15-1

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For research use only. Not Intended for Therapeutic Use!
Cat No:I000408
Molecular Formula:C₂₉H₄₀N₈O₃S
Molecular Weight:580.74
IC50:3.5 nM
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Appearance:Solid powder
Purity: > 98%
Cat No:I000408
Cas No:1097917-15-1

ASP3026 is a novel and selective inhibitor for ALK with IC50 of 3.5 nM.
IC50 value: 3.5 nM
Target: ALK
in vitro: ASP3026 shows more selective ALK inhibition in a Tyr-kinase panel than PF02341066. ASP3026 inhibits the growth of NCI-H2228, a human NSCLC tumor cell line endogenously expressing EML4-ALK variant 3, with an IC50 value of 64.8 nM [1].
in vivo: ASP3026, administered to mice bearing subcutaneous NCI-H2228 tumor xenografts as twice daily oral dosing for 14 days, induces dose dependent anti-tumor effects starting at 1 mg/kg with strong regression at 10, 30 and 100 mg/kg [1].

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
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
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
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
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
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