2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK Membrane Transporter/Ion Channel Apoptosis
  3. EGFR P-glycoprotein Apoptosis
  4. Befotertinib

Befotertinib (D-0316) is an orally active EGFR inhibitor and ABCB1 inhibitor. Befotertinib selectively targets EGFR mutations including EGFRT790M, EGFRL858R and delE746-A750, forms covalent bonds with EGFRC797, 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.

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Befotertinib

Befotertinib 화학구조

CAS No. : 1835667-63-4

사이즈 가격 재고 수량
무료 샘플 (0.1 - 0.2 mg)   지금 신청하기  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 해외재고보유
Solution
10 mM * 1 mL in DMSO 해외재고보유
Solid
5 mg 해외재고보유
10 mg 해외재고보유
25 mg 해외재고보유
50 mg 해외재고보유
100 mg 해외재고보유
200 mg   견적 받기  
500 mg   견적 받기  

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고객리뷰

Based on 2 publication(s) in Google Scholar

Other Forms of Befotertinib:

Befotertinib Related Antibodies

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EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

  • Biological Activity

  • 순도&문서

  • References

  • 고객리뷰

제품 설명

Befotertinib (D-0316) is an orally active EGFR inhibitor and ABCB1 inhibitor. Befotertinib selectively targets EGFR mutations including EGFRT790M, EGFRL858R and delE746-A750, forms covalent bonds with EGFRC797, 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[1][2].

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.

Befotertinib Related Antibodies

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
분자량

567.61

화학식

C29H32F3N7O2
CAS No.
Appearance

Solid

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
선적

Room temperature in continental US; may vary elsewhere.
보관
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
용액&용해도
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7618 mL 8.8089 mL 17.6177 mL
5 mM 0.3524 mL 1.7618 mL 3.5235 mL
View the 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.

  • 몰농도 계산기

  • 농도 희석 계산기

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • 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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • 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

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
순도&문서

Purity: 99.86%

SDS (252 KB)

COA (255 KB) HNMR (312 KB) LCMS (267 KB)

Handling Instructions (2659 KB)
References

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 1.7618 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 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Befotertinib1835667-63-4D-0316D0316D 0316EGFRP-glycoproteinApoptosisEpidermal growth factor receptorErbB-1HER1P-gpPgpMultidrug resistance protein 1MDR1ATP-binding cassette sub-family B member 1ABCB1Cluster of differentiation 243CD243L858RKB-V1H1975NCI-ADR-RESMDR19-HEK293delE746-A750non-small cell lung cancerT790MInhibitorinhibitorinhibit

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상품명:
Befotertinib
Cat. No.:
HY-137433
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