TL 13-112 structure
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Common Name | TL 13-112 | ||
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CAS Number | 2229037-19-6 | Molecular Weight | 1002.573 | |
Density | 1.4±0.1 g/cm3 | Boiling Point | N/A | |
Molecular Formula | C49H60ClN9O10S | Melting Point | N/A | |
MSDS | N/A | Flash Point | N/A |
Use of TL 13-112TL13-112 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). |
Name | 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 |
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Synonym | More Synonyms |
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). |
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Related Catalog | |
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 |
Density | 1.4±0.1 g/cm3 |
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Molecular Formula | C49H60ClN9O10S |
Molecular Weight | 1002.573 |
Exact Mass | 1001.387207 |
LogP | 3.02 |
Index of Refraction | 1.620 |
Hazard Codes | Xi |
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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 |