2229037-04-9
Chemical Structure
TL13-12
- CAS No.: 2229037-04-9
- Formula:C45H53ClN10O10S
- Molecular Weight:961.48
IUPAC Name: N-(2-(2-(2-(4-(4-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-3-methoxyphenyl)piperazin-1-yl)ethoxy)ethoxy)ethyl)-2-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)acetamide
InChIKey: WXNUIPVZMJMPNM-UHFFFAOYSA-N
SMILES: O=C(NCCOCCOCCN1CCN(C2=CC=C(NC3=NC=C(Cl)C(NC4=CC=CC=C4S(=O)(C(C)C)=O)=N3)C(OC)=C2)CC1)CNC5=CC=CC(C(N6C(CC7)C(NC7=O)=O)=O)=C5C6=O
Biological Activity: TL13-12 is a CRBN-recruiting ALK PROTAC degrader, with a DC50 of 10 nM in H3122 cells. TL13-12 induces dimerization of CRBN and truncated ALK, which brings the DNA-binding domain and transactivation domain into close proximity, thereby activating the expression of downstream reporter genes, while exhibiting extremely low leaky expression under non-inducing conditions. TL13-12 serves as a tool molecule for the orthogonal PROTAC-CID system, and is applied in research on non-small cell lung cancer, anaplastic large cell lymphoma, and neuroblastoma[1][2].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
|
|
TL13-12 | 98.16% | TL13-12 is a CRBN-recruiting ALK PROTAC degrader, with a DC50 of 10 nM in H3122 cells. TL13-12 induces dimerization of CRBN and truncated ALK, which brings the DNA-binding domain and transactivation domain into close proximity, thereby activating the expression of downstream reporter genes, while exhibiting extremely low leaky expression under non-inducing conditions. TL13-12 serves as a tool molecule for the orthogonal PROTAC-CID system, and is applied in research on non-small cell lung cancer, anaplastic large cell lymphoma, and neuroblastoma. | ||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
References
- [1]. Powell CE, et al. Chemically Induced Degradation of Anaplastic Lymphoma Kinase (ALK). Journal of medicinal chemistry. 2018 May 10;61(9):4249-4255. [Content Brief]
- [2]. Ma D, et al. Engineered PROTAC-CID Systems for Mammalian Inducible Gene Regulation. Journal of the American Chemical Society. 2023 Jan 25;145(3):1593-1606.
