YN14
Based on 1 Customer Validation
YN14 is a KRASG12C proteolysis targeting chimera (PROTAC). YN14 is highly potent and selective KRASG12C degrader and induces a stable KRASG12C: YN14: VHL ternary complex with low binding free energy (ΔG). YN14 has antiproliferative effects and significantly inhibits KRASG12C-mutant cancer cell growth. YN14 leads to tumor regression with tumor growth inhibition (TGI%) rates more than 100 % in the MIA PaCa-2 xenograft model.
(Pink: KRAS(G12C) ligand (HY-114277); Blue: VHL ligand (HY-125845); Black: linker (HY-W588704)).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.08%
- 分子式: C62H75F2N11O7S
- 分子量:1156.39
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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
PROTACs アイソフォーム固有の製品をすべて表示
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生物活性
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| ASPC1 | IC50 |
>10 μM
Compound: YN14
|
Antiproliferative activity against human ASPC1 cells expressing KRAS G12D mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human ASPC1 cells expressing KRAS G12D mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
|
[PMID: 37852032] |
| HEK-293T | IC50 |
>10 μM
Compound: YN14
|
Cytotoxicity against HEK293T cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
Cytotoxicity against HEK293T cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
|
[PMID: 37852032] |
| HepG2 | IC50 |
>10 μM
Compound: YN14
|
Antiproliferative activity against human HepG2 cells expressing KRAS assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human HepG2 cells expressing KRAS assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
|
[PMID: 37852032] |
| MIA PaCa-2 | IC50 |
0.045 μM
Compound: YN14
|
Antiproliferative activity against human MIA PaCa-2 cells expressing KRAS G12C mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human MIA PaCa-2 cells expressing KRAS G12C mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
|
[PMID: 37852032] |
| NCI-H358 | IC50 |
0.091 μM
Compound: YN14
|
Antiproliferative activity against human NCI-H358 cells expressing KRAS G12C mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human NCI-H358 cells expressing KRAS G12C mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
|
[PMID: 37852032] |
化学情報
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性状 Solid
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分子量 1156.39
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分子式 C62H75F2N11O7S
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Color White to off-white
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SMILES
O=C(C=C)N1C[C@H](C)N(C2=NC(N(C3=C(C)C=CN=C3C(C)C)C4=NC(C5=C(OCC6CCN(CCCC(N[C@@H](C(C)(C)C)C(N7[C@H](C(NCC8=CC=C(C9=C(C)N=CS9)C=C8)=O)C[C@@H](O)C7)=O)=O)CC6)C=CC=C5F)=C(F)C=C42)=O)CC1
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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
溶剤 & 溶解度
DMSO : 100 mg/mL (86.48 mM; Need ultrasonic; 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 (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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 | 0.8648 mL | 4.3238 mL | 8.6476 mL | 21.6190 mL |
| 5 mM | 0.1730 mL | 0.8648 mL | 1.7295 mL | 4.3238 mL | |
| 10 mM | 0.0865 mL | 0.4324 mL | 0.8648 mL | 2.1619 mL | |
| 15 mM | 0.0577 mL | 0.2883 mL | 0.5765 mL | 1.4413 mL | |
| 20 mM | 0.0432 mL | 0.2162 mL | 0.4324 mL | 1.0810 mL | |
| 25 mM | 0.0346 mL | 0.1730 mL | 0.3459 mL | 0.8648 mL | |
| 30 mM | 0.0288 mL | 0.1441 mL | 0.2883 mL | 0.7206 mL | |
| 40 mM | 0.0216 mL | 0.1081 mL | 0.2162 mL | 0.5405 mL | |
| 50 mM | 0.0173 mL | 0.0865 mL | 0.1730 mL | 0.4324 mL | |
| 60 mM | 0.0144 mL | 0.0721 mL | 0.1441 mL | 0.3603 mL | |
| 80 mM | 0.0108 mL | 0.0540 mL | 0.1081 mL | 0.2702 mL |