SPH5030
Based on 1 Customer Validation
SPH5030 is a selective and irreversible HER2 inhibitor. SPH5030 inhibits HER2WT and EGFRWT with IC50s of 3.51 and 8.13 nM, respectively. SPH5030 shows excellent activities against HER2 mutants. SPH5030 can be used for the research of cancer.
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: 99.40%
- CAS 番号: 2364326-23-6
- 分子式: C31H31FN8O3
- 分子量:582.63
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保管条件:
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
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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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
EGFR アイソフォーム固有の製品をすべて表示
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生物活性
IC50: 3.51 nM (HER2WT), 0.42 nM (HER2D769H), 0.43 nM (HER2D769Y), 0.16 nM (HER2V777L), 0.56 nM (HER2R896C), 8.13 nM (EGFRWT)[1]
SPH5030 (0-10 μM; 72 h) shows anti-proliferation activities against tumor cell lines[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:NCI-N87, BT-474, SK-BR-3 with HER2 overexpression, MDA-MB-468 with EGFR overexpression, NCI-H441, Es-2, MFE-280, NUGC-4, COLO678, KM12-luc and BaF3 cell lines
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Concentration:0-10 μM
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Incubation Time:72 hours
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Result:Effectively inhibited NCI-N87, BT-474, SK-BR-3 with HER2 overexpression and BaF3 cells with IC50s of 1.09, 2.01, 20.09 and 6.3 nM, respectively. Poorly inhibited MDA-MB-468 with EGFR overexpression, NCI-H441, Es-2, MFE-280, NUGC-4, COLO678 and KM12-luc cells with IC50s of 2980, 4257, 2716, 3967, 1218, 6065 and 3597 nM, respectively.
| Mice IV 3 mg/kg |
Mice PO 10 mg/kg |
Rats IV 3 mg/kg |
Rats PO 6 mg/kg |
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| CL (L/kg·h) | 0.70±0.20 | 0.78±0.13 | ||
| t1/2 (h) | 3.76±0.15 | 3.60±0.59 | 4.56±0.20 | 4.38±0.35 |
| Vss (L/kg) | 2.96±0.96 | 3.55±0.64 | ||
| Cmax (μg/mL) | 1.90±0.14 | 0.76±0.33 | ||
| tmax (h) | 2.67±1.15 | 3.33±1.15 | ||
| AUC0-t (h·μg/mL) | 13.07±0.48 | 5.47±2.82 | ||
| F (%) | 87.66 | 71.35 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude mouse with NCI-N87 and BT474 xenografts, and NPSG mouse with BAF3 HER2 A775_G776insYVMA xenografts[1]
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Dosage:5, 10, 20 and 40 mg/kg
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Administration:Oral gavage; 5-40 mg/kg once per day; for 13 or 21 days
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Result:Dose-dependently inhibited tumor growth in NCI-N87, BT474 and BAF3 HER2 A775_G776insYVMA xenograft mouse models, and showed an equivalent or better activity of tumor inhibition compared with neratinib and pyrotinib at a dose of 20 mg/kg. Showed no mortality or significant loss of body weight in xenograft mouse models.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 2364326-23-6
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性状 Solid
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分子量 582.63
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分子式 C31H31FN8O3
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Color Off-white to light yellow
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SMILES
CCOC1=C(C=C2C(N=CN=C2NC3=CC(C)=C(C=C3)OC4=CC5=NC=NN5C=C4)=C1)NC(/C(F)=C/[C@H]6CCCN6C)=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
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
溶剤 & 溶解度
DMSO : ≥ 100 mg/mL (171.64 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, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). 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 (protect from light, stored under nitrogen). 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 (276 KB)
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SDS (252 KB)
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- Deutsch - DE (252 KB)
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- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (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 (protect from light, stored under nitrogen). 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 | 1.7164 mL | 8.5818 mL | 17.1636 mL | 42.9089 mL |
| 5 mM | 0.3433 mL | 1.7164 mL | 3.4327 mL | 8.5818 mL | |
| 10 mM | 0.1716 mL | 0.8582 mL | 1.7164 mL | 4.2909 mL | |
| 15 mM | 0.1144 mL | 0.5721 mL | 1.1442 mL | 2.8606 mL | |
| 20 mM | 0.0858 mL | 0.4291 mL | 0.8582 mL | 2.1454 mL | |
| 25 mM | 0.0687 mL | 0.3433 mL | 0.6865 mL | 1.7164 mL | |
| 30 mM | 0.0572 mL | 0.2861 mL | 0.5721 mL | 1.4303 mL | |
| 40 mM | 0.0429 mL | 0.2145 mL | 0.4291 mL | 1.0727 mL | |
| 50 mM | 0.0343 mL | 0.1716 mL | 0.3433 mL | 0.8582 mL | |
| 60 mM | 0.0286 mL | 0.1430 mL | 0.2861 mL | 0.7151 mL | |
| 80 mM | 0.0215 mL | 0.1073 mL | 0.2145 mL | 0.5364 mL | |
| 100 mM | 0.0172 mL | 0.0858 mL | 0.1716 mL | 0.4291 mL |
SPH5030 関連分類
HY-143319 関連分類
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