Cat. No. Name Size Price Add Cart
KI2776ASP-30265 mg$148
ASP-302610 mg$234
ASP-302625 mg$470
ASP-302650 mg$752

Chemical Characteristic

Product NameASP-3026
SynonymsASP3026
CAS No.1097917-15-1
Molecular Weight 580.76
FormulaC29H40N8O3S
Chemical Name2-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
Smilesn1c(nc(nc1)Nc1c(cccc1)S(=O)(=O)C(C)C)Nc1c(cc(cc1)N1CCC(CC1)N1CCN(CC1)C)OC
Chemical Structure

Biological activities

ASP-3026 is a potent and selective inhibitor of ALK kinase. ASP-3026 inhibits ALK kinase activity with an IC50 of 3.2 nM.[1] In vitro, ASP-3026 inhibits the growth of NCI-H2228, a human NSCLC tumor cell line endogenously expressing EML4-ALK variant 3. In vivo in mice with NCI-H2228 tumor xenografts, ASP-3026(daily oral dosing for 14 days) induces dose dependent anti-tumor effects. Meanwhile, in an EML4-ALK driven tumor model with gatekeeper mutation, ASP-3026 shows potent anti-tumor effects.[2]

Protocols

In vitro, ASP-3026 is dissolved in DMSO.[2]

References

[1] Latif M, et al. Journey of the ALK-inhibitor CH5424802 to phase II clinical trial. Arch Pharm Res. 2013, 36 (9): 1051-1054.
[2] Kuromitsu S, Mori M, Shimada I, et al. Antitumor activities of ASP3026 against EML4-ALK-dependent tumor models. Mol Cancer Ther. 2011, 10: A227.

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