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.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.40%
- CAS No.: 2364326-23-6
- Formule: C31H31FN8O3
- Masse moléculaire:582.63
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Stockage:
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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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 |
Chemical Information
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CAS No. 2364326-23-6
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Appearance Solid
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Masse moléculaire 582.63
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Solvant et solubilité
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
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Fiche technique (276 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
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 |
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| 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 |
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