Cat. No.: HY-128778

Gozanertinib

(Synonyms: DBPR112)

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Gozanertinib is an orally active furanopyrimidine-based EGFR inhibitor with IC₅₀s of 15 nM and 48 nM for EGFR^WT and EGFR^L858R/T790M, respectively. Gozanertinib can occupy the ATP-binding site. Gozanertinib has significant antitumor efficacy.

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Pureté: 98.37%
CAS No.: 1226549-49-0
Formule: C₃₂H₃₁N₅O₃
Masse moléculaire:533.62

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Gozanertinib Chemical Structure

CAS No.: 1226549-49-0

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target^[1]

EGFR^WT

15 nM (IC₅₀)

EGFR^L858R/T790M

48 nM (IC₅₀)

Voir tous les produits spécifiques à Isoform EGFR :

Cellular Effect

Cell Line	Type	Value	Description	References
A-431	CC₅₀	1020 nM Compound: 78	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	[PMID: 31560541]
A-431	CC₅₀	1020 nM Compound: DBPR112; 11	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	[PMID: 36749735]
HCC827	CC₅₀	25 nM Compound: 78	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	[PMID: 31560541]
NCI-H1975	CC₅₀	620 nM Compound: 78	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	[PMID: 31560541]
NCI-H1975	CC₅₀	620 nM Compound: DBPR112; 11	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	[PMID: 36749735]

In Vitro

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.

Western Blot Analysis^[1]

Cell Line:

H1975 cells
Concentration:

0.32, 1.6, 8.0, 40, 200, 1000 nM
Incubation Time:

16 hours
Result:

Induced reduction of phosphorylated EGFR in a dose-dependent manner in H1975 cells.

In Vivo

Gozanertinib (orally; 20-50 mg/kg; 5 days/week for 2 consecutive weeks) significantly reduces tumor growth in HCC827 tumor model. Gozanertinib (orally; 50 mg/kg; once a day for 15 days) has a significant antitumor effect (mean tumor growth inhibition of 34%) in H1975 tumor model^[1].
Gozanertinib (IV; 5 mg/kg) has a T_1/2 of 2.3 hours, a CL of 55.6 mL/min kg, and a V_ss of 8.6 L/kg for rats^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

HCC827 tumor model (6- to 8-week-old athymic NU-Fox1nu nude mice)^[1]
Dosage:

20, 50 mg/kg
Administration:

Orally; 5 days/week for 2 consecutive weeks (days 1-5 and 8-12)
Result:

Significantly reduced tumor growth.

Animal Model:

Rats^[1]
Dosage:

5 mg/kg for IV and 20 mg/kg for PO (Pharmacokinetic Analysis)
Administration:

IV or PO
Result:

Had a T_1/2 of 2.3 hours, a CL of 55.6 mL/min•kg, and a V_ss of 8.6 L/kg by IV.
Had a T_1/2 of 3.4 hours, a C_max of 508 ng/mL and an AUC of 2978 ng/mL•h by PO.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1226549-49-0
Appearance Solid
Masse moléculaire 533.62
Formule C₃₂H₃₁N₅O₃
Color Off-white to light yellow
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
Synonyms

DBPR112
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvant et solubilité

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.8740 mL

9.3700 mL

18.7399 mL

5 mM

0.3748 mL

1.8740 mL

3.7480 mL

10 mM

0.1874 mL

0.9370 mL

1.8740 mL

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.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (3.90 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (279 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Lin SY, et al. Discovery of a Furanopyrimidine-Based Epidermal Growth Factor Receptor Inhibitor (DBPR112) as a Clinical Candidate for the Treatment of Non-Small Cell Lung Cancer. J Med Chem. 2019 Nov 27;62(22):10108-10123. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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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Gozanertinib

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Voir tous les produits spécifiques à Isoform EGFR

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Gozanertinib Related Classifications

HY-128778 Related Classifications