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

Befotertinib mesylate  (Synonyms: D-0316 mesylate)

Cat. No.: HY-137433A
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Befotertinib (D-0316) mesylate is an orally active EGFR inhibitor and ABCB1 inhibitor. Befotertinib mesylate selectively targets EGFR mutations including EGFRT790M, EGFRL858R and delE746-A750, forms covalent bonds with EGFRC797, inhibits oncogenic signaling pathways, and exerts antiproliferative effects. Befotertinib mesylate 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 mesylate 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.

Befotertinib mesylate

Befotertinib mesylate Chemical Structure

CAS No. : 2226167-02-6

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Befotertinib mesylate Related Antibodies

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Description

Befotertinib (D-0316) mesylate is an orally active EGFR inhibitor and ABCB1 inhibitor. Befotertinib mesylate selectively targets EGFR mutations including EGFRT790M, EGFRL858R and delE746-A750, forms covalent bonds with EGFRC797, inhibits oncogenic signaling pathways, and exerts antiproliferative effects. Befotertinib mesylate 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 mesylate 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) mesylate 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) mesylate 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) mesylate 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) mesylate 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 mesylate 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.
Molecular Weight

663.71

Formula

C30H36F3N7O5S
CAS No.
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.O=S(O)(C)=O
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Room temperature in continental US; may vary elsewhere.
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Please store the product under the recommended conditions in the Certificate of Analysis.
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Befotertinib mesylate Related Classifications

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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:

Befotertinib2226167-02-6D-0316D0316D 0316EGFRP-glycoproteinApoptosisEpidermal growth factor receptorErbB-1HER1P-gpPgpMultidrug resistance protein 1MDR1ATP-binding cassette sub-family B member 1ABCB1Cluster of differentiation 243CD243NSCLClung cancerInhibitorinhibitorinhibit

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