TL 13-12 structure
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Common Name | TL 13-12 | ||
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CAS Number | 2229037-04-9 | Molecular Weight | 961.481 | |
Density | 1.4±0.1 g/cm3 | Boiling Point | N/A | |
Molecular Formula | C45H53ClN10O10S | Melting Point | N/A | |
MSDS | N/A | Flash Point | N/A |
Use of TL 13-12TL13-12 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 |
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Synonym | More Synonyms |
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). |
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Related Catalog | |
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 |
Density | 1.4±0.1 g/cm3 |
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Molecular Formula | C45H53ClN10O10S |
Molecular Weight | 961.481 |
Exact Mass | 960.335510 |
LogP | 1.06 |
Index of Refraction | 1.639 |
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 |