TL13-112
Based on 2 publication(s) in Google Scholar
TL13-112 is a potent and selective ALK-PROTAC degrader and inhibits ALK activity with an IC50 value of 0.14 nM. TL13-112 also prompts the degradation of additional kinases including Aurora A, FER, PTK2 and RPS6KA1 with IC50 values of 8550 nM, 42.4 nM, 25.4 nM, and 677 nM, respectively. TL13-112 is comprised of the conjugation of Ceritinib (HY-15656) and the Cereblon ligand of Pomalidomide (HY-10984).
(Pink: Anaplastic lymphoma kinase (ALK) ligand (HY-15656); Blue: Cereblon ligand (HY-41547); Black: linker).
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- 純度: 98.01%
- CAS 番号: 2229037-19-6
- 分子式: C49H60ClN9O10S
- 分子量:1002.57
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
MedChemExpress(MCE)の使用を引用している文献 TL13-112
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生物活性
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Cereblon 2.4 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| SR | IC50 |
5.9 nM
Compound: Cpd 11
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Antiproliferative activity against ALK positive human SR cells
Antiproliferative activity against ALK positive human SR cells
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[PMID: 33751979] |
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 40 nM in H3122 cell and Karpas 299, respectively. ALK degradation acts at 4 hours of treatment in H3122 cells and at 8 hours of treatment in Karpas 299 cells. The maximum degradation achieves at 16 hours in both cell lines. [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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:H3122 and Karpas 299 cells
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Concentration:0.01 μM; 0.05 μM; 0.1 μM; 0.5 μM; 1 μM
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Incubation Time:16 hours
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Result:Inhibited ALK and Aurora A expression completely at 1 μM.
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Cell Line:H3122 and Karpas 299 cells
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Concentration:0.01 μM; 0.05 μM; 0.1 μM; 0.5 μM; 1 μM
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Incubation Time:16 hours
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Result:Decreased PTK2, ALK, FER, RPS6KA1 and Aurora A expression.
化学情報
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CAS 番号 2229037-19-6
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性状 Solid
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分子量 1002.57
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分子式 C49H60ClN9O10S
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Color Light yellow to yellow
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SMILES
O=C(NCCOCCOCCN1CCC(C2=CC(OC(C)C)=C(NC3=NC=C(Cl)C(NC4=CC=CC=C4S(=O)(C(C)C)=O)=N3)C=C2C)CC1)CNC5=CC=CC(C(N6C(CC7)C(NC7=O)=O)=O)=C5C6=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
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Sci Transl Med
Targeting CCR7-PI3Kγ overcomes resistance to tyrosine kinase inhibitors in ALK-rearranged lymphoma. [Abstract]2023 Jun 28;15(702):eabo3826. PMID: 37379367 -
bioRxiv
2025 Nov 30:2025.11.26.690562. PMID: 41394586
溶剤 & 溶解度
DMSO : 100 mg/mL (99.74 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (271 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)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
参考文献
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 | 0.9974 mL | 4.9872 mL | 9.9744 mL | 24.9359 mL |
| 5 mM | 0.1995 mL | 0.9974 mL | 1.9949 mL | 4.9872 mL | |
| 10 mM | 0.0997 mL | 0.4987 mL | 0.9974 mL | 2.4936 mL | |
| 15 mM | 0.0665 mL | 0.3325 mL | 0.6650 mL | 1.6624 mL | |
| 20 mM | 0.0499 mL | 0.2494 mL | 0.4987 mL | 1.2468 mL | |
| 25 mM | 0.0399 mL | 0.1995 mL | 0.3990 mL | 0.9974 mL | |
| 30 mM | 0.0332 mL | 0.1662 mL | 0.3325 mL | 0.8312 mL | |
| 40 mM | 0.0249 mL | 0.1247 mL | 0.2494 mL | 0.6234 mL | |
| 50 mM | 0.0199 mL | 0.0997 mL | 0.1995 mL | 0.4987 mL | |
| 60 mM | 0.0166 mL | 0.0831 mL | 0.1662 mL | 0.4156 mL | |
| 80 mM | 0.0125 mL | 0.0623 mL | 0.1247 mL | 0.3117 mL |