2229037-04-9

2229037-04-9 structure

Name: TL 13-12
Chemical Name: N-(2-{2-[2-(4-{4-[(5-Chloro-4-{[2-(isopropylsulfonyl)phenyl]amino}-2-pyrimidinyl)amino]-3-methoxyphenyl}-1-piperazinyl)ethoxy]ethoxy}ethyl)-N2-[2-(2,6-dioxo-3-piperidinyl)-1,3-dioxo-2,3-dihydro-1H-isoindol-4-yl]glycinamide
CAS Number: 2229037-04-9
Molecular Formula: C₄₅H₅₃ClN₁₀O₁₀S
Molecular Weight: 961.481
Catalog: Signaling Pathways Protein Tyrosine Kinase/RTK ALK
Create Date: 2020-01-12 12:19:50
Modify Date: 2024-04-02 00:11:44
TL13-12 is a novel Anaplastic Lymphoma Kinase (ALK)-PROTAC developed through conjugation of TAE684 and the cereblon ligand pomalidomide; also promotes the degradation of additional kinases including PTK2 (FAK), Aurora A, FER, and RPS6KA1 (RSK1).

Name	N-(2-{2-[2-(4-{4-[(5-Chloro-4-{[2-(isopropylsulfonyl)phenyl]amino}-2-pyrimidinyl)amino]-3-methoxyphenyl}-1-piperazinyl)ethoxy]ethoxy}ethyl)-N2-[2-(2,6-dioxo-3-piperidinyl)-1,3-dioxo-2,3-dihydro-1H-isoindol-4-yl]glycinamide
Synonyms	Acetamide, N-[2-[2-[2-[4-[4-[[5-chloro-4-[[2-[(1-methylethyl)sulfonyl]phenyl]amino]-2-pyrimidinyl]amino]-3-methoxyphenyl]-1-piperazinyl]ethoxy]ethoxy]ethyl]-2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]amino]- N-(2-{2-[2-(4-{4-[(5-Chloro-4-{[2-(isopropylsulfonyl)phenyl]amino}-2-pyrimidinyl)amino]-3-methoxyphenyl}-1-piperazinyl)ethoxy]ethoxy}ethyl)-N2-[2-(2,6-dioxo-3-piperidinyl)-1,3-dioxo-2,3-dihydro-1H-i soindol-4-yl]glycinamide

Description	TL13-12 is a novel Anaplastic Lymphoma Kinase (ALK)-PROTAC developed through conjugation of TAE684 and the cereblon ligand pomalidomide; also promotes the degradation of additional kinases including PTK2 (FAK), Aurora A, FER, and RPS6KA1 (RSK1).
Related Catalog	Research Areas >> Cancer Signaling Pathways >> Protein Tyrosine Kinase/RTK >> ALK
Target	IC50: 0.69 nM (ALK)[1]
In Vitro	TL13-12 (0-200 nM; 16 hours) is selective for degradation of ALK with the DC50s of 10 nM and 180 nM in H3122 cell and Karpas 299, respectively[1]. TL13-12 (0-160 nM; 16 hours) degrades ALK and aurora A protein expression as a dose-dependent manner in Kelly and CHLA20 cells[1]. TL13-12 (100 nM; 16 hours) significantly inhibits Tariqudan-induced ALK and Aurora A protein expression in CHLA20 cells[1]. Western Blot Analysis[1] Cell Line: Kelly and CHLA20 cells Concentration: 0 nM; 20 nM; 40 nM; 60 nM; 80 nM; 100 nM; 140 nM; 160 nM Incubation Time: 16 hours Result: Exhibited degrader behavior in cells. Western Blot Analysis[1] Cell Line: CHLA20 cells Concentration: 100 nM Incubation Time: 16 hours Result: Decreased ALK and Aurora A protein expression.
References	[1]. Powell CE, et al. Chemically Induced Degradation of Anaplastic Lymphoma Kinase (ALK).J Med Chem. 2018 May 10;61(9):4249-4255.