YD23
Based on 1 Customer Validation
YD23 is a selective SMARCA2 PROTAC degrader with DC50 values of 64 nM and 297 nM in H1792 cells and H1975 cells. YD23 induces degradation of SMARCA2, which is synthetic lethal to SMARCA4. YD23 reduces chromatin accessibility only in SMARCA4 deficient cells, including cell cycle and cell growth regulatory genes. YD23 selectively inhibits growth of SMARCA4 mutant lung cancer cells. YD23 has potent tumor growth inhibitory activity in SMARCA4-mutant xenografts. YD23 can be used for the study of non-small cell lung cancer (NSCLC).
(Pink: SMARCA2 ligand (HY-44012); Blue: Cereblon ligand (HY-41547); Black: linker).
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 98.80%
- CAS No.: 2951015-29-3
- Formule: C38H39FN8O7
- Masse moléculaire:738.76
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Stockage: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]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Epigenetics Compound Library
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Immunology/Inflammation Compound Library
HY-L007
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Histone Modification Research Compound Library
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Anti-Cancer Compound Library
HY-L025
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Anti-Lung Cancer Compound Library
HY-L075
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Anti-Blood Cancer Compound Library
HY-L079
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PROTAC Library
HY-L151
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Anti-Hematopathy Compound Library
HY-L171
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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High-Throughput Bioactive Compound Library
HY-L205
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Activité biologique
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Cereblon |
YD23 (0.0001-10 μM, 12 days) selectively inhibits growth of SMARCA4-mutant ung cancer cell lines compared to SMARCA4-WT cells (median IC50 of 0.11 μM and 6.0 μM, for each group, respectively)[2].
YD23 (1 μM, 96 h)-downregulated genes are significantly enriched in cell cycle-related pathways such as E2F target genes, G2/M checkpoint, and mitotic spindle[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Human tumor xenografts of three SMARCA4-mutated lung cancers (H1568, H322, H2126) established in NU/J nude female mice[1]
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Dosage:12.5 mg/kg
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Administration:Intraperitoneal injection (i.p.), once daily for 25-26 days
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Result:Showed significant tumor growth inhibition (TGI) of 72% (H1568), 49% (H322), and 44% (H2126).
Effectively degraded SMARCA2 in vivo.
Showed a slight weight loss (<10%), indicating good tolerance.
Chemical Information
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CAS No. 2951015-29-3
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Appearance Solid
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Masse moléculaire 738.76
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Formule C38H39FN8O7
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Color Light yellow to yellow
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SMILES
O=C1N(C2CCC(NC2=O)=O)C(C3=C1C=CC=C3NCCOCCOC4=C(F)C=C(CN5CCN(C6=C(N)N=NC(C7=C(O)C=CC=C7)=C6)CC5)C=C4)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 100 mg/mL (135.36 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)
Pureté et documentation
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Fiche technique (272 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Instruction de manipulation (2659 KB)
Références
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 | 1.3536 mL | 6.7681 mL | 13.5362 mL | 33.8405 mL |
| 5 mM | 0.2707 mL | 1.3536 mL | 2.7072 mL | 6.7681 mL | |
| 10 mM | 0.1354 mL | 0.6768 mL | 1.3536 mL | 3.3840 mL | |
| 15 mM | 0.0902 mL | 0.4512 mL | 0.9024 mL | 2.2560 mL | |
| 20 mM | 0.0677 mL | 0.3384 mL | 0.6768 mL | 1.6920 mL | |
| 25 mM | 0.0541 mL | 0.2707 mL | 0.5414 mL | 1.3536 mL | |
| 30 mM | 0.0451 mL | 0.2256 mL | 0.4512 mL | 1.1280 mL | |
| 40 mM | 0.0338 mL | 0.1692 mL | 0.3384 mL | 0.8460 mL | |
| 50 mM | 0.0271 mL | 0.1354 mL | 0.2707 mL | 0.6768 mL | |
| 60 mM | 0.0226 mL | 0.1128 mL | 0.2256 mL | 0.5640 mL | |
| 80 mM | 0.0169 mL | 0.0846 mL | 0.1692 mL | 0.4230 mL | |
| 100 mM | 0.0135 mL | 0.0677 mL | 0.1354 mL | 0.3384 mL |
YD23 Related Classifications
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