Belizatinib
Based on 1 publication(s) in Google Scholar
Belizatinib (TSR-011) is an orally active, potent inhibitor of ALK and TRKA, TRKB, and TRKC, with IC50 of 0.7 nM for wild-type recombinant ALK kinase.
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 : 99.62%
- CAS 番号: 1357920-84-3
- 分子式: C33H44FN5O3
- 分子量:577.73
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
MedChemExpress(MCE)の使用を引用している文献 Belizatinib
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生物活性
製品説明
IC50 & Target
|
TrkA |
TrkB |
TrkC |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
231 nM
Compound: 36
|
Inhibition of INSR expressed in CHO cells assessed as inhibition of receptor phosphorylation pre-incubated before insulin stimulation by Meso-Scale Discovery pY-IR assay
Inhibition of INSR expressed in CHO cells assessed as inhibition of receptor phosphorylation pre-incubated before insulin stimulation by Meso-Scale Discovery pY-IR assay
|
[PMID: 22734674] |
体外実験
Belizatinib (TSR-011) has antitumour activity.
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.
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | 2011-05 | PHASE1 |
化学情報
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CAS 番号 1357920-84-3
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性状 Solid
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分子量 577.73
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分子式 C33H44FN5O3
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Color White to off-white
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SMILES
O=C(NC1=NC2=CC=C(CN3CCC(C(C)(O)C)CC3)C=C2N1[C@H]4CC[C@@H](C(NC(C)C)=O)CC4)C5=CC=C(F)C=C5
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別名
TSR-011
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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 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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J Pharm Biomed Anal
Belizatinib: Novel reactive intermediates and bioactivation pathways characterized by LC-MS/MS. [Abstract]2019 Jul 15:171:132-147. PMID: 30999224
溶剤 & 溶解度
体外:
DMSO : ≥ 300 mg/mL (519.27 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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 (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.7309 mL | 8.6546 mL | 17.3091 mL | 43.2728 mL |
| 5 mM | 0.3462 mL | 1.7309 mL | 3.4618 mL | 8.6546 mL | |
| 10 mM | 0.1731 mL | 0.8655 mL | 1.7309 mL | 4.3273 mL | |
| 15 mM | 0.1154 mL | 0.5770 mL | 1.1539 mL | 2.8849 mL | |
| 20 mM | 0.0865 mL | 0.4327 mL | 0.8655 mL | 2.1636 mL | |
| 25 mM | 0.0692 mL | 0.3462 mL | 0.6924 mL | 1.7309 mL | |
| 30 mM | 0.0577 mL | 0.2885 mL | 0.5770 mL | 1.4424 mL | |
| 40 mM | 0.0433 mL | 0.2164 mL | 0.4327 mL | 1.0818 mL | |
| 50 mM | 0.0346 mL | 0.1731 mL | 0.3462 mL | 0.8655 mL | |
| 60 mM | 0.0288 mL | 0.1442 mL | 0.2885 mL | 0.7212 mL | |
| 80 mM | 0.0216 mL | 0.1082 mL | 0.2164 mL | 0.5409 mL | |
| 100 mM | 0.0173 mL | 0.0865 mL | 0.1731 mL | 0.4327 mL |