SMD-3040 TFA
SMD-3040 TFA is a potent and selective SMARCA2 PROTAC degrader (DC50: 12 nM; Dmax: 91%). SMD-3040 TFA can inhibit tumor cell proliferation and exhibits antitumor activity. SMD-3040 TFA can be used in the study of tumors such as melanoma. (SMARCA2/4-ligand (HY-171765); HY-112078 VHL ligand (HY-112078))
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: 99.90%
- 分子式: C54H67F3N10O7S
- 分子量:1057.23
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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
SMD-3040 (0-1 μM; 1-48 h) TFA can effectively degrade SMARCA2 in cells such as Hela, SK-Mel-5 and SK-Mel-28[1].
SMD-3040 (7 days) TFA significantly inhibits cell growth in SMARCA4-deficient cancer cell lines (such as SK-Mel-5, H838, A549, etc.) with GI50 of 8.8-119 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SK-Mel-5 and SK-Mel-28 cells
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Concentration:0.01, 0.03, 0.1, 0.3, 1, 3, 10, 30, 100, 300 and 1000 nM
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Incubation Time:24 h
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Result:Inhibited the level of SMARCA2.
Had DC50 values of 20 and 35 nM in K-Mel-5 and SK-Mel-28 cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Xenograft mouse models treated SK-Mel-5 melanoma cell line carrying SMARCA4 gene deletion[1]
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Dosage:25 and 50 mg/kg
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Administration:Intravenous injection; twice weekly; two weeks
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Result:Effectively inhibited tumor growth in two different smarca4-deficient xenograft models.
Was well-tolerated in mice.
化学情報
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性状 Solid
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分子量 1057.23
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分子式 C54H67F3N10O7S
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Color Off-white to light yellow
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SMILES
O=C(N[C@H](C(N1[C@H](C(N[C@H](C2=CC=C(C3=C(C)N=CS3)C=C2)C)=O)C[C@@H](O)C1)=O)C(C)(C)C)[C@H]4CC[C@H](CN5CC6(CCC(N7N=CC(C8=C(N)N=NC(C9=C(O)C=CC=C9)=C8)=C7)CC6)C5)CC4.O=C(O)C(F)(F)F
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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 (94.59 mM; Need ultrasonic and warming; 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 (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 | 0.9459 mL | 4.7293 mL | 9.4587 mL | 23.6467 mL |
| 5 mM | 0.1892 mL | 0.9459 mL | 1.8917 mL | 4.7293 mL | |
| 10 mM | 0.0946 mL | 0.4729 mL | 0.9459 mL | 2.3647 mL | |
| 15 mM | 0.0631 mL | 0.3153 mL | 0.6306 mL | 1.5764 mL | |
| 20 mM | 0.0473 mL | 0.2365 mL | 0.4729 mL | 1.1823 mL | |
| 25 mM | 0.0378 mL | 0.1892 mL | 0.3783 mL | 0.9459 mL | |
| 30 mM | 0.0315 mL | 0.1576 mL | 0.3153 mL | 0.7882 mL | |
| 40 mM | 0.0236 mL | 0.1182 mL | 0.2365 mL | 0.5912 mL | |
| 50 mM | 0.0189 mL | 0.0946 mL | 0.1892 mL | 0.4729 mL | |
| 60 mM | 0.0158 mL | 0.0788 mL | 0.1576 mL | 0.3941 mL | |
| 80 mM | 0.0118 mL | 0.0591 mL | 0.1182 mL | 0.2956 mL |