1. PROTAC
    Protein Tyrosine Kinase/RTK
  2. PROTAC
    ALK
  3. TL13-12

TL13-12 

Cat. No.: HY-122582
Handling Instructions

TL13-12 is a potent and selective ALK-PROTAC degrader and inhibits ALK activity with an IC50 value of 0.69 nM. TL13-12 also prompts the degradation of additional kinases including Aurora A, FER, PTK2, and RPS6KA1 with IC50 values of 13.5 nM, 5.74 nM, 18.4 nM, and 65 nM, respectively. TL13-12 is comprised of the conjugation of TAE684 (HY-10192) and the cereblon ligand of Pomalidomide (HY-10984).

For research use only. We do not sell to patients.

TL13-12 Chemical Structure

TL13-12 Chemical Structure

CAS No. : 2229037-04-9

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Description

TL13-12 is a potent and selective ALK-PROTAC degrader and inhibits ALK activity with an IC50 value of 0.69 nM. TL13-12 also prompts the degradation of additional kinases including Aurora A, FER, PTK2, and RPS6KA1 with IC50 values of 13.5 nM, 5.74 nM, 18.4 nM, and 65 nM, respectively. TL13-12 is comprised of the conjugation of TAE684 (HY-10192) and the cereblon ligand of Pomalidomide (HY-10984)[1].

IC50 & Target

Cereblon

1.2 μM (IC50)

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.
Molecular Weight

961.48

Formula

C₄₅H₅₃ClN₁₀O₁₀S

CAS No.

2229037-04-9

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

TL13-12PROTACALKProteolysis-targeting chimeraAnaplastic lymphoma kinaseALK tyrosine kinase receptorCD246Cluster of differentiation 246KellyCHLA20 H3122Karpas 299Inhibitorinhibitorinhibit

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