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).
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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: 98.80%
- CAS 番号: 2951015-29-3
- 分子式: C38H39FN8O7
- 分子量:738.76
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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
生物活性
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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.
化学情報
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CAS 番号 2951015-29-3
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性状 Solid
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分子量 738.76
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分子式 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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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 (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.
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 (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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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 | 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 |