Neladalkib
Based on 1 Customer Validation
Neladalkib (NVL-655) is an oral ALK inhibitor, the IC50 for Neladalkib in inhibiting ALK is 2.8 nM. Neladalkib promotes cell apoptosis and has anti-tumor activity.
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 : 99.87%
- CAS 番号: 2739866-40-9
- 分子式: C23H22ClFN6O
- 分子量:452.91
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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
製品説明
体外実験
Neladalkib has an IC50 of 2.7 nM in Ba/F3 CLIP1-LTK cells[1].
Neladalkib has a strong inhibitory effect on ALKT1151insT, ALKT1151M, ALKL1152R, ALKC1156Y, ALKI1171N, ALKI1171S, ALKI1171T, ALKF1174L, ALKF1174S, ALKV1180L, ALKL1198F, ALKG1202R, ALKD1203N, ALKS1206R, and ALKR1275Q (IC50 = 0.9-6.8 nmol/L), while it has a weaker inhibitory effect on ALKG1196M, ALKG1269A, and ALKG1269S (IC50 = 11-79 nmol/L)[2].
Neladalkib (1-100 nM, 24 h) increases the activation of caspase 3/7 and reduces the S-phase cells in NCI-H3122[2].
Neladalkib (1-100 nM, 24 h) promotes apoptosis in NCI-H3122 cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:ALK-driven tumor xenografts in mice[2]
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Dosage:0.06, 0.2, 0.5, 1.5 mg/kg
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Administration:Oral
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Result:Inhibited tumor proliferation.
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 2739866-40-9
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性状 Solid
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分子量 452.91
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分子式 C23H22ClFN6O
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Color White to off-white
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SMILES
CCN1C2=C(C(Cl)=N1)CC3=CN(C)N=C3C4=CC=C(F)C=C4[C@H](OC5=C(N)N=CC2=C5)C
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別名
NVL-655
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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
体外:
DMSO : 100 mg/mL (220.79 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 (280 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)
- Korean - KR (251 KB)
- Portuguese - PT (251 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 | 2.2079 mL | 11.0397 mL | 22.0794 mL | 55.1986 mL |
| 5 mM | 0.4416 mL | 2.2079 mL | 4.4159 mL | 11.0397 mL | |
| 10 mM | 0.2208 mL | 1.1040 mL | 2.2079 mL | 5.5199 mL | |
| 15 mM | 0.1472 mL | 0.7360 mL | 1.4720 mL | 3.6799 mL | |
| 20 mM | 0.1104 mL | 0.5520 mL | 1.1040 mL | 2.7599 mL | |
| 25 mM | 0.0883 mL | 0.4416 mL | 0.8832 mL | 2.2079 mL | |
| 30 mM | 0.0736 mL | 0.3680 mL | 0.7360 mL | 1.8400 mL | |
| 40 mM | 0.0552 mL | 0.2760 mL | 0.5520 mL | 1.3800 mL | |
| 50 mM | 0.0442 mL | 0.2208 mL | 0.4416 mL | 1.1040 mL | |
| 60 mM | 0.0368 mL | 0.1840 mL | 0.3680 mL | 0.9200 mL | |
| 80 mM | 0.0276 mL | 0.1380 mL | 0.2760 mL | 0.6900 mL | |
| 100 mM | 0.0221 mL | 0.1104 mL | 0.2208 mL | 0.5520 mL |