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TL 13-112

Names

[ CAS No. ]:
2229037-19-6

[ Name ]:
TL 13-112

[Synonym ]:
Acetamide, N-[2-[2-[2-[4-[4-[[5-chloro-4-[[2-[(1-methylethyl)sulfonyl]phenyl]amino]-2-pyrimidinyl]amino]-2-methyl-5-(1-methylethoxy)phenyl]-1-piperidinyl]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]-5-isopropoxy-2-methylphenyl}-1-piperidinyl)ethoxy]ethoxy}ethyl)-N2-[2-(2,6-dioxo-3-piperidinyl)-1,3-dioxo-2,3- dihydro-1H-isoindol-4-yl]glycinamide

Biological Activity

[Description]:

TL13-112 is a novel Anaplastic Lymphoma Kinase (ALK)-PROTAC developed through conjugation of LDK378 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
Signaling Pathways >> PROTAC >> PROTAC

[Target]

IC50: 0.14 nM (ALK)[1]


[In Vitro]

TL13-112 binds to cereblon with an IC50 value of 2.4 uM[1]. TL13-112 (0.01 μM-1 μM; 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]. TL13-112 (0.01 μM-1 μM; 16 hours) inhibits PTK2, ALK, FER, RPS6KA1 and Aurora A expression as a dose-dependent manner in H3122, Karpas 299, and Kelly cells[1]. Western Blot Analysis[1] Cell Line: H3122 and Karpas 299 cells Concentration: 0.01 μM; 0.05 μM; 0.1 μM; 0.5 μM; 1 μM Incubation Time: 16 hours Result: Inhibited ALK and Aurora A expression completely at 1 μM. Western Blot Analysis[1] Cell Line: H3122 and Karpas 299 cells Concentration: 0.01 μM; 0.05 μM; 0.1 μM; 0.5 μM; 1 μM Incubation Time: 16 hours Result: Decreased PTK2, ALK, FER, RPS6KA1 and Aurora A 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.

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Molecular Formula ]:
C49H60ClN9O10S

[ Molecular Weight ]:
1002.573

[ Exact Mass ]:
1001.387207

[ LogP ]:
3.02

[ Index of Refraction ]:
1.620

Safety Information

[ Hazard Codes ]:
Xi

Related Compounds