SIAIS164018


Catalog No. Size PriceQuantity
M12454-2 2mg solid $80
M12454-10 10mg solid $240

Description

SIAIS164018 is an enlightening degrader for us to excavate the charm of protein degradation.First, SIAIS164018 could degrade not only ALK fusion proteins in activating or G1202R-mutated form but also mutant EGFR with L858R + T790M, which are two most important targets in non-small-cell lung cancer. Second, SIAIS164018 strongly inhibited cell migration and invasion of Calu-1 and MDA-MB-231. Third and surprisingly, SIAIS164018 degrades several important oncoproteins involved in metastasis such as FAK, PYK2, and PTK6. Interestingly, SIAIS164018 reshuffled the kinome ranking profile when compared to Brigatinib. Finally, SIAIS164018 is orally bioavailable and well tolerated in vivo.

Product information

Molecular Weight: 883.33

Formula: C43H48ClN10O7P

Chemical Name: 4-(2-(4-(1-(4-(5-chloro-4-(2-(dimethylphosphoryl)phenylamino)pyrimidin-2-ylamino)-3-methoxyphenyl)piperidin-4-yl)piperazin-1-yl)-2-oxoethylamino)-2-(2, 6-dioxopiperidin-3-yl)isoindoline-1, 3-dione

Smiles: COC1=CC(=CC=C1NC1=NC(NC2=CC=CC=C2P(C)(C)=O)=C(Cl)C=N1)N1CCC(CC1)N1CCN(CC1)C(=O)CNC1=CC=CC2=C1C(=O)N(C1CCC(=O)NC1=O)C2=O

InChiKey: AQGLXXCBEXDRNS-UHFFFAOYSA-N

InChi: InChI=1S/C43H48ClN10O7P/c1-61-34-23-27(11-12-30(34)48-43-46-24-29(44)39(50-43)47-31-8-4-5-10-35(31)62(2,3)60)51-17-15-26(16-18-51)52-19-21-53(22-20-52)37(56)25-45-32-9-6-7-28-38(32)42(59)54(41(28)58)33-13-14-36(55)49-40(33)57/h4-12,23-24,26,33,45H,13-22,25H2,1-3H3,(H,49,55,57)(H2,46,47,48,50)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

Products are for research use only. Not for human use.

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