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)).
For research use only. We do not sell to patients.
- Purity: 99.08%
- Formula: C62H75F2N11O7S
- Molecular Weight:1156.39
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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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
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[PMID: 37852032] |
| HEK-293T | IC50 |
>10 μM
Compound: YN14
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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
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[PMID: 37852032] |
| HepG2 | IC50 |
>10 μM
Compound: YN14
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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
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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
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[PMID: 37852032] |
| NCI-H358 | IC50 |
0.091 μM
Compound: YN14
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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
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[PMID: 37852032] |
Chemical Information
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Appearance Solid
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Molecular Weight 1156.39
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Formula 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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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 (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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (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)
- 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 | 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 |
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