YN14
Based on 1 Customer Validation
YN14 is a KRASG12C PROTAC degrader that recruits E3 ubiquitin ligase to induce the polyubiquitination and proteasomal degradation of KRASG12C. YN14 induces tumor cell apoptosis, cell cycle arrest, and cell migration inhibition. YN14 exhibits in vivo antitumor proliferative activity in tumor cell xenograft nude mice. YN14 can be used in cancer-related research.
(Pink: KRAS(G12C) ligand (HY-114277); Blue: VHL ligand (HY-125845); Black: linker (HY-W588704)).
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 99.08%
- Formel: C62H75F2N11O7S
- Molecular Weight:1156.39
-
Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biologische Aktivität
-
Chemical Information
-
Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
-
Help & FAQs
Alle PROTACs Isoform-spezifische Produkte anzeigen
MoreAlle Caspase Isoform-spezifische Produkte anzeigen
More
Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
KRas G12C |
Caspase 3 |
Akt |
Cellular Effect
|
Cell Line
|
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] |
In Vitro
YN14 (0-10000 nM; 72 h) effectively induces potent, concentration-dependent degradation of the KRASG12C protein in NCI-H358 non-small cell lung cancer cells and Miapaca-2 pancreatic cancer cells; its DC50 is 0.067 μM in NCI-H358 and 0.028 μM in Miapaca-2[1].
YN14 (30-300 nM; 24-48 h) induces apoptosis in NCI-H358 non-small cell lung cancer cells and Miapaca-2 pancreatic cancer cells, and arrests the cell cycle of NCI-H358 and Miapaca-2 cells at the G2/M phase in a dose-dependent manner[1].
YN14 (30-300 nM; 12 h) inhibits the migration capacity of NCI‑H358 cells in a dose-dependent manner, exhibiting a dose-dependent effect[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:NCI-H358 non-small cell lung cancer cells, Miapaca-2 pancreatic cancer cells
-
Concentration:0 nM, 1 nM, 3.3 nM, 10 nM, 33 nM, 100 nM, 300 nM, 1000 nM, 3000 nM, 10000 nM
-
Incubation Time:72 h
-
Result:Induced concentration-dependent degradation of KRASG12C protein in NCI-H358 cells, with KRASG12C protein signal beginning to decrease markedly at 33 nM, partial residual KRASG12C signal remaining at 1000 nM, and full restoration of the KRASG12C signal at 10000 nM.
Induced gradual concentration-dependent reduction of KRASG12C protein levels in Miapaca-2 cells, with distinct KRASG12C protein degradation starting from 10 nM, and near-maximal KRASG12C degradation achieved at 100 nM and 300 nM.
Showed no alteration in β-actin signal intensity across all tested concentrations, confirming equal protein loading across all samples.
-
Cell Line:NCI-H358 non-small cell lung cancer cells
-
Concentration:30, 100, 300 nM
-
Incubation Time:12 h
-
Result:Inhibited the migration capacity of NCI‑H358 cells in a dose-dependent manner, exhibiting a dose-dependent effect.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:BALB/c nude mice (female, 4~6 weeks) were subcutaneously inoculated with 5×106 Miapaca‑2 human pancreatic cancer cells.[1]
-
Dosage:10, 30 mg/kg
-
Administration:Intraperitoneal (IP) injection; once daily; for 2, 4, 6, 8, 10, 12, 14, 16 days
-
Result:Markedly suppressed tumour growth with TGI of 93.42 % measured on day 8 in the 10 mg/kg group, and no obvious body‑weight loss or toxic responses were observed in experimental animals.
Achieved TGI > 100 % measured on day 8 in the 30 mg/kg group, indicating tumour regression.
Revealed downregulation of KRASG12C, CD31, p‑ERK and p‑AKT, and upregulation of pro‑apoptotic marker cleaved‑caspase 3 in tumour tissues via immunohistochemistry and western‑blot assays.
- Scratch/Wound-Healing Migration Assay
- Annexin V plus membrane-impermeant dye apoptosis staining
- BrdU Incorporation Assay
- Cell migration
- Neural Crest/Neuronal Cell Migration Explant Assay
- Protocol for Cell Cycle
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Flow cytometric DNA-content cell-cycle staining
- Chemotaxis Gradient Chamber Assay 1
- Under-Agarose Cell Migration Assay
- Transwell/Boyden Chamber Migration Assay
- Patient-Derived Xenograft (PDX)
- Apoptosis Solutions
- 3D Collagen/Hydrogel Matrix Migration Assay
- Splenic/Portal-Vein Liver Metastasis Xenograft
- Subcutaneous Cell-Line-Derived Xenograft
- Cell-Exclusion Zone Migration Assay
- Chemotaxis Gradient Chamber Assay 2
- Orthotopic Cell-Line Xenograft
- Intraperitoneal/Peritoneal Dissemination Xenograft
Chemical Information
-
Appearance Solid
-
Molecular Weight 1156.39
-
Formel C62H75F2N11O7S
-
Color White to off-white
-
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
-
Versand
Room temperature in continental US; may vary elsewhere.
-
Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
In Vitro:
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
-
Data Sheet (286 KB)
-
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)
-
Handling Instructions (2659 KB)
Verweise
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 |
YN14 Related Classifications
HY-155356 Related Classifications
Powered by Bioz