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SIAIS164018

CAT: 0804-HY-147219Size: 1 EachDry Ice: NoHazardous: No
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CAT#:0804-HY-147219Size:1 Each
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
SIAIS164018 is a PROTAC-based ALK and EGFR degrader, with IC50 value of 2.5 nM and 6.6 nM for ALK and ALK G1202R, respectively. SIAIS164018 strongly inhibits cancer cells migration and invasion, causes G1 cell cycle arrest and induces apoptosis. SIAIS164018 exhibits better property than Brigatinib.
CAS Number
2353492-68-7
UNSPSC
12352005
Target
Anaplastic lymphoma kinase (ALK) ; Apoptosis; EGFR; PROTACs
Type
Reference compound
Related Pathways
Apoptosis; JAK/STAT Signaling; PROTAC; Protein Tyrosine Kinase/RTK
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/siais164018.html
Solubility
DMSO : 100 mg/mL (ultrasonic)
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
Molecular Formula
C43H48ClN10O7P
Molecular Weight
883.33
References & Citations
[1]Ren C, et al. Discovery of a Brigatinib Degrader SIAIS164018 with Destroying Metastasis-Related Oncoproteins and a Reshuffling Kinome Profile. J Med Chem. 2021 Jul 8;64 (13) :9152-9165.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported

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