Gozanertinib
Based on 1 Customer Validation
Gozanertinib is an orally active furanopyrimidine-based EGFR inhibitor with IC50s of 15 nM and 48 nM for EGFRWT and EGFRL858R/T790M, respectively. Gozanertinib can occupy the ATP-binding site. Gozanertinib has significant antitumor efficacy.
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- Pureza: 98.37%
- No. CAS: 1226549-49-0
- Fòrmula: C32H31N5O3
- Peso molecular:533.62
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
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EGFRWT 15 nM (IC50) |
EGFRL858R/T790M 48 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A-431 | CC50 |
1020 nM
Compound: 78
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Cytotoxicity in human A431 cells assessed as reduction in cell viability incubated for 96 hrs by MTS method
Cytotoxicity in human A431 cells assessed as reduction in cell viability incubated for 96 hrs by MTS method
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[PMID: 31560541] |
| A-431 | CC50 |
1020 nM
Compound: DBPR112; 11
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Antiproliferative activity against human A-431 cells overexpressing wild-type EGFR assessed as cell growth inhibition measured after 96 hrs by MTS assay
Antiproliferative activity against human A-431 cells overexpressing wild-type EGFR assessed as cell growth inhibition measured after 96 hrs by MTS assay
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[PMID: 36749735] |
| HCC827 | CC50 |
25 nM
Compound: 78
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Cytotoxicity in human HCC827 cells assessed as reduction in cell viability incubated for 96 hrs by MTS method
Cytotoxicity in human HCC827 cells assessed as reduction in cell viability incubated for 96 hrs by MTS method
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[PMID: 31560541] |
| NCI-H1975 | CC50 |
620 nM
Compound: 78
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Cytotoxicity in human NCI-H1975 cells assessed as reduction in cell viability incubated for 96 hrs by MTS method
Cytotoxicity in human NCI-H1975 cells assessed as reduction in cell viability incubated for 96 hrs by MTS method
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[PMID: 31560541] |
| NCI-H1975 | CC50 |
620 nM
Compound: DBPR112; 11
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Antiproliferative activity against human NCI-H1975 cells overexpressing EGFR T790M/L858R assessed as cell growth inhibition measured after 96 hrs by MTS assay
Antiproliferative activity against human NCI-H1975 cells overexpressing EGFR T790M/L858R assessed as cell growth inhibition measured after 96 hrs by MTS assay
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[PMID: 36749735] |
Gozanertinib (compound 78; 0.32-1000 nM; 16 hours) induces reduction of phosphorylated EGFR in a dose-dependent manner[1].
Gozanertinib shows the inhibitory activity against HCC827 (CC50=25 nM), H1975 (CC50=620 nM) and A431 Cell (CC50=1.02 μM) cell lines[1].
Gozanertinib occupies the ATP-binding site and interacts with surrounding residues by covalent bonding, hydrogen bonds, and hydrophobic interactions, which give it a potent inhibitory activity against WT EGFR[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:H1975 cells
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Concentration:0.32, 1.6, 8.0, 40, 200, 1000 nM
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Incubation Time:16 hours
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Result:Induced reduction of phosphorylated EGFR in a dose-dependent manner in H1975 cells.
Gozanertinib (IV; 5 mg/kg) has a T1/2 of 2.3 hours, a CL of 55.6 mL/min kg, and a Vss of 8.6 L/kg for rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:HCC827 tumor model (6- to 8-week-old athymic NU-Fox1nu nude mice)[1]
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Dosage:20, 50 mg/kg
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Administration:Orally; 5 days/week for 2 consecutive weeks (days 1-5 and 8-12)
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Result:Significantly reduced tumor growth.
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Animal Model:Rats[1]
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Dosage:5 mg/kg for IV and 20 mg/kg for PO (Pharmacokinetic Analysis)
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Administration:IV or PO
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Result:Had a T1/2 of 2.3 hours, a CL of 55.6 mL/min•kg, and a Vss of 8.6 L/kg by IV.
Had a T1/2 of 3.4 hours, a Cmax of 508 ng/mL and an AUC of 2978 ng/mL•h by PO.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1226549-49-0
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Appearance Solid
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Peso molecular 533.62
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Fòrmula C32H31N5O3
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Color Off-white to light yellow
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SMILES
O=C(NC1=CC=CC(C2=C(C3=CC=CC=C3)OC4=NC=NC(N[C@@H](C5=CC=CC=C5)CO)=C42)=C1)/C=C/CN(C)C
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Synonyms
DBPR112
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 250 mg/mL (468.50 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (3.90 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.08 mg/mL (3.90 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (279 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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 | 1.8740 mL | 9.3700 mL | 18.7399 mL | 46.8498 mL |
| 5 mM | 0.3748 mL | 1.8740 mL | 3.7480 mL | 9.3700 mL | |
| 10 mM | 0.1874 mL | 0.9370 mL | 1.8740 mL | 4.6850 mL | |
| 15 mM | 0.1249 mL | 0.6247 mL | 1.2493 mL | 3.1233 mL | |
| 20 mM | 0.0937 mL | 0.4685 mL | 0.9370 mL | 2.3425 mL | |
| 25 mM | 0.0750 mL | 0.3748 mL | 0.7496 mL | 1.8740 mL | |
| 30 mM | 0.0625 mL | 0.3123 mL | 0.6247 mL | 1.5617 mL | |
| 40 mM | 0.0468 mL | 0.2342 mL | 0.4685 mL | 1.1712 mL | |
| 50 mM | 0.0375 mL | 0.1874 mL | 0.3748 mL | 0.9370 mL | |
| 60 mM | 0.0312 mL | 0.1562 mL | 0.3123 mL | 0.7808 mL | |
| 80 mM | 0.0234 mL | 0.1171 mL | 0.2342 mL | 0.5856 mL | |
| 100 mM | 0.0187 mL | 0.0937 mL | 0.1874 mL | 0.4685 mL |
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