Cat. No.: HY-137433

Befotertinib

(Synonyms: D-0316)

2 Cited Publications

Customer Review

Based on 2 publication(s) in Google Scholar

Befotertinib (D-0316) is an orally active EGFR inhibitor and ABCB1 inhibitor. Befotertinib selectively targets EGFR mutations including EGFR^T790M, EGFR^L858R and delE746-A750, forms covalent bonds with EGFR^C797, inhibits oncogenic signaling pathways, and exerts antiproliferative effects. Befotertinib inhibits ABCB1-mediated drug efflux, activates the ATPase activity of ABCB1, acts as a chemosensitizer and apoptosis enhancer, and restores the sensitivity of multidrug-resistant cancer cells. Befotertinib can be used in research related to multidrug-resistant cancers and non-small cell lung cancer.

For research use only. We do not sell to patients.

Purity: 99.86%
CAS No.: 1835667-63-4
Formula: C₂₉H₃₂F₃N₇O₂
Molecular Weight:567.61

Storage:

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

Befotertinib Chemical Structure

CAS No.: 1835667-63-4

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Antibody-Drug Conjugates

One-stop solution for XDC (ADC/PDC/RDC/ApDC/FDC/ISAC/VDC/SMDC)

Biological Activity
- Description
- In Vitro
- Clinical Trial
Chemical Information
Publications (2)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

All EGFR Isoforms :

In Vitro

Befotertinib (0.1-100 μM; 72 h) exhibits comparable cytotoxic activity in ABCB1-overexpressing KB-V1, NCI-ADR-RES, MDR19-HEK293 cells and their parental cell lines KB-3-1, OVCAR-8, pcDNA3.1-HEK293^[1].
Befotertinib (2 μM; 48 h) enhances Paclitaxel (HY-B0015)-induced apoptosis. After 48 h of combined treatment, the proportion of apoptotic cells increases to 85% in KB-V1 cells and to 95% in NCI-ADR-RES cells^[1].
Befotertinib (10 μM; 10 min) inhibits ABCB1-mediated drug efflux and significantly enhances calcein accumulation in KB-V1, NCI-ADR-RES and MDR19-HEK293 cells after 10 minutes of incubation^[1].
Befotertinib (0.001-10000 nM; 72 h) potently inhibits the proliferation of EGFR-mutant non-small cell lung cancer (NSCLC) cell lines H1975, HCC-827 and H3255, with EC₅₀ values of 1.2 nM, 3.0 nM and 4.3 nM, respectively; whereas it exerts minimal effects on A431 cells overexpressing wild-type (WT) EGFR, with an EC₅₀ value of 1200 nM^[2].

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

Apoptosis Analysis^[1]

Cell Line:

KB-V1, NCI-ADR-RES
Concentration:

2 μM (befotertinib); 1 μM (paclitaxel)
Incubation Time:

48 h
Result:

Induced minimal apoptosis (apoptotic cell populations below 10%) when treated alone in KB-V1 and NCI-ADR-RES cells.
Increased apoptosis to 85% in KB-V1 cells and almost 95% in NCI-ADR-RES cells when co-treated with paclitaxel, comparable to the positive control combination of tariquidar and paclitaxel.

Cell Proliferation Assay^[2]

Cell Line:

HCC-827 (delE746-A750), H3255 (L858R), H1975 (L858R/T790M), A431 (WT EGFR overexpressing)
Concentration:

0.001-10000 nM
Incubation Time:

72 h
Result:

Exhibited an antiproliferative EC₅₀ of 1200 nM against A431 WT EGFR-overexpressing cells.
Exhibited an antiproliferative EC₅₀ of 1.2 nM against H1975 L858R/T790M EGFR cells.
Exhibited an antiproliferative EC₅₀ of 3.0 nM against HCC-827 delE746-A750 EGFR cells.
Exhibited an antiproliferative EC₅₀ of 4.3 nM against H3255 L858R EGFR cells.

Clinical Trial

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

Chemical Information

CAS No. 1835667-63-4
Appearance Solid
Molecular Weight 567.61
Formula C₂₉H₃₂F₃N₇O₂
Color Light yellow to yellow
SMILES

O=C(NC1=CC(NC2=NC(C3=CN(CC(F)(F)F)C4=C3C=CC=C4)=CC=N2)=C(C=C1N(CCN(C)C)C)OC)C=C
Synonyms

D-0316
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Publications (2)

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Journal Impact Factor

J Med Chem

Profiling and Optimizing Targeted Covalent Inhibitors through EGFR-Guided Studies. [Abstract]

2025 Aug 28;68(16):17917-17932. PMID: 40801664
Preprints

2024 Jun 04.

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (88.09 mM; ultrasonic and warming and heat to 60°C; 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

1.7618 mL

8.8089 mL

17.6177 mL

5 mM

0.3524 mL

1.7618 mL

3.5235 mL

10 mM

0.1762 mL

0.8809 mL

1.7618 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.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

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Volume _(start) Volume _(start)

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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 (3.66 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% Corn Oil

Solubility: ≥ 2.08 mg/mL (3.66 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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
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)
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)
Handling Instructions (2659 KB)

References

[1]. Li YC, et al. Befotertinib restored chemosensitivity to multidrug-resistant cancer cells by inhibiting the drug efflux activity of ABCB1. J Pharm Pharmacol. 2026;78(3):rgag020. [Content Brief]

[2]. Damghani T, et al. Profiling and Optimizing Targeted Covalent Inhibitors through EGFR-Guided Studies. J Med Chem. 2025;68(16):17917-17932. [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	1.7618 mL	8.8089 mL	17.6177 mL	44.0443 mL
	5 mM	0.3524 mL	1.7618 mL	3.5235 mL	8.8089 mL
	10 mM	0.1762 mL	0.8809 mL	1.7618 mL	4.4044 mL
	15 mM	0.1175 mL	0.5873 mL	1.1745 mL	2.9363 mL
	20 mM	0.0881 mL	0.4404 mL	0.8809 mL	2.2022 mL
	25 mM	0.0705 mL	0.3524 mL	0.7047 mL	1.7618 mL
	30 mM	0.0587 mL	0.2936 mL	0.5873 mL	1.4681 mL
	40 mM	0.0440 mL	0.2202 mL	0.4404 mL	1.1011 mL
	50 mM	0.0352 mL	0.1762 mL	0.3524 mL	0.8809 mL
	60 mM	0.0294 mL	0.1468 mL	0.2936 mL	0.7341 mL
	80 mM	0.0220 mL	0.1101 mL	0.2202 mL	0.5506 mL

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Befotertinib

Apoptosis Compound Library

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

Membrane Transporter/Ion Channel Compound Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Covalent Screening Library

Differentiation Inducing Compound Library

Orally Active Compound Library

Anti-Hepatitis C Virus Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cytokine Inhibitors Library

Cell Death Library

Anti-Drug-Resistant Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) Befotertinib

All EGFR Isoforms

Biological Activity

Chemical Information

Publications (2)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Befotertinib Related Classifications

HY-137433 Related Classifications