2353492-68-7
Chemical Structure
SIAIS164018
- CAS No.: 2353492-68-7
- Formula:C43H48ClN10O7P
- Molecular Weight:883.33
IUPAC Name: benzyl (2S,4S)-2-(4-cyanophenyl)-4-ethoxypiperidine-1-carboxylate
InChIKey: AQGLXXCBEXDRNS-UHFFFAOYSA-N
SMILES: O=C1NC(C(CC1)N2C(C3=C(C2=O)C(NCC(N4CCN(C5CCN(CC5)C6=CC=C(C(OC)=C6)NC7=NC=C(C(NC8=C(P(C)(C)=O)C=CC=C8)=N7)Cl)CC4)=O)=CC=C3)=O)=O
Biological Activity: SIAIS164018 is a multi-kinase (ALK, EGFR, FAK, PYK2, PTK6) PROTAC degrader, with IC50 values of 2.5 nM and 6.6 nM against ALK and ALK (G1202R), respectively. SIAIS164018 promotes the ubiquitination and degradation of ALK, EGFR, FAK, PYK2 and PTK6. SIAIS164018 induces cell cycle arrest at the G1 phase and triggers cell Apoptosis. SIAIS164018 exhibits preferential inhibitory activity against FER kinase. SIAIS164018 can be used in research related to non-small cell lung cancer, ovarian cancer and triple-negative breast cancer[1][2][3][4].
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SIAIS164018 | SIAIS164018 is a multi-kinase (ALK, EGFR, FAK, PYK2, PTK6) PROTAC degrader, with IC50 values of 2.5 nM and 6.6 nM against ALK and ALK (G1202R), respectively. SIAIS164018 promotes the ubiquitination and degradation of ALK, EGFR, FAK, PYK2 and PTK6. SIAIS164018 induces cell cycle arrest at the G1 phase and triggers cell Apoptosis. SIAIS164018 exhibits preferential inhibitory activity against FER kinase. SIAIS164018 can be used in research related to non-small cell lung cancer, ovarian cancer and triple-negative breast cancer. | |||||||||||||||||||||
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- [1]. Kossakowski K, et al. FDA-approved kinase inhibitors in PROTAC design, development and synthesis. Journal of enzyme inhibition and medicinal chemistry. 2025 Dec;40(1):2542357. [Content Brief]
- [2]. Ren C, et al. Discovery of a Brigatinib Degrader SIAIS164018 with Destroying Metastasis-Related Oncoproteins and a Reshuffling Kinome Profile. Journal of medicinal chemistry. 2021 Jul 08;64(13):9152-9165. [Content Brief]
- [3]. Zhang Y, et al. Development of the nonreceptor tyrosine kinase FER-targeting PROTACs as a potential strategy for antagonizing ovarian cancer cell motility and invasiveness. The Journal of biological chemistry. 2023 Jun;299(6):104825. [Content Brief]
- [4]. Rallabandi NC, et al. EGFR molecular degraders: preclinical successes and the road ahead. Future Med Chem. 2025 Mar;17(6):633-636. [Content Brief]
Keywords
