TL13-12
Based on 1 Customer Validation
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).
(Pink: Anaplastic lymphoma kinase (ALK) ligand (HY-184540); Blue: Cereblon ligand (HY-131717); Black: linker (HY-130485)).
For research use only. We do not sell to patients.
- Purity: 98.16%
- CAS No.: 2229037-04-9
- Formula: C45H53ClN10O10S
- Molecular Weight:961.48
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
All PROTACs Isoforms
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Biological Activity
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Cereblon 1.2 μM (IC50) |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Kelly and CHLA20 cells
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Concentration:0 nM; 20 nM; 40 nM; 60 nM; 80 nM; 100 nM; 140 nM; 160 nM
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Incubation Time:16 hours
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Result:Exhibited degrader behavior in cells.
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Cell Line:CHLA20 cells
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Concentration:100 nM
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Incubation Time:16 hours
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Result:Decreased ALK and Aurora A protein expression.
Chemical Information
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CAS No. 2229037-04-9
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Appearance Solid
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Molecular Weight 961.48
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Formula C45H53ClN10O10S
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Color Yellow to brown
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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
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : ≥ 100 mg/mL (104.01 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (270 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.0401 mL | 5.2003 mL | 10.4006 mL | 26.0016 mL |
| 5 mM | 0.2080 mL | 1.0401 mL | 2.0801 mL | 5.2003 mL | |
| 10 mM | 0.1040 mL | 0.5200 mL | 1.0401 mL | 2.6002 mL | |
| 15 mM | 0.0693 mL | 0.3467 mL | 0.6934 mL | 1.7334 mL | |
| 20 mM | 0.0520 mL | 0.2600 mL | 0.5200 mL | 1.3001 mL | |
| 25 mM | 0.0416 mL | 0.2080 mL | 0.4160 mL | 1.0401 mL | |
| 30 mM | 0.0347 mL | 0.1733 mL | 0.3467 mL | 0.8667 mL | |
| 40 mM | 0.0260 mL | 0.1300 mL | 0.2600 mL | 0.6500 mL | |
| 50 mM | 0.0208 mL | 0.1040 mL | 0.2080 mL | 0.5200 mL | |
| 60 mM | 0.0173 mL | 0.0867 mL | 0.1733 mL | 0.4334 mL | |
| 80 mM | 0.0130 mL | 0.0650 mL | 0.1300 mL | 0.3250 mL | |
| 100 mM | 0.0104 mL | 0.0520 mL | 0.1040 mL | 0.2600 mL |