Erlotinib mesylate
Based on 143 publication(s) in Google Scholar
Erlotinib (CP-358774) mesylate is a selective, orally active EGFR tyrosine kinase inhibitor. Erlotinib mesylate also acts as a substrate and inhibitor of OATP2B1, with an IC50 of approximately 0.079 μM for inhibiting OATP2B1-mediated uptake of estrone 3-sulfate. Erlotinib mesylate blocks EGFR phosphorylation, downstream signal transduction, as well as the growth and proliferation of cancer cells. Erlotinib mesylate inhibits MMP-10-mediated renal injury, fibrotic lesions, the ERK1/2, GSK-3β and β-catenin signaling pathways, as well as the deposition of fibronectin, α-SMA, collagen and renal injury markers. Erlotinib mesylate is metabolized via CYP3A to produce the active metabolite OSI-420. Erlotinib mesylate can be used in research related to non-small cell lung cancer, gastric cancer, papillary renal cell carcinoma, EGFR inhibitor resistance and renal fibrosis.
For research use only. We do not sell to patients.
- CAS No.: 248594-19-6
- Formula: C23H27N3O7S
- Molecular Weight:489.54
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Publications Citing Use of MedChemExpress (MCE) Erlotinib mesylate
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- Cancer Cell. 2025 Jul 25:S1535-6108(25)00310-1. [Abstract]
- Cell Res. 2020 Oct;30(10):833-853. [Abstract]
- Nat Immunol. 2022 Feb;23(2):251-261. [Abstract]
- Bioact Mater. 2024 May 11:38:384-398. [Abstract]
- Bioact Mater. 2021 Nov 4;13:312-323. [Abstract]
- Nat Cell Biol. 2026 Mar 27. [Abstract]
- Cancer Res. 2024 Feb 1;84(3):479-492. [Abstract]
- Nat Commun. 2026 Jan 21;17(1):1902. [Abstract]
- Nat Commun. 2023 Apr 24;14(1):2342. [Abstract]
- Nat Commun. 2023 Mar 28;14(1):1726. [Abstract]
- Nat Commun. 2019 Apr 18;10(1):1812 [Abstract]
- Mol Cell. 2023 Dec 7;83(23):4334-4351.e7. [Abstract]
- Mol Cell. 2022 Jul 7;82(13):2443-2457.e7. [Abstract]
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- Acta Pharm Sin B. 2025 Dec 29.
- J Exp Clin Cancer Res. 2026 Jan 6;45(1):32. [Abstract]
- J Exp Clin Cancer Res. 2024 Nov 20;43(1):308. [Abstract]
- J Exp Clin Cancer Res. 2021 Jan 9;40(1):25. [Abstract]
- J Clin Invest. 2020 Mar 2;130(3):1417-1430. [Abstract]
- Cell Rep Med. 2026 Apr 21;7(4):102691. [Abstract]
- Cell Rep Med. 2025 Apr 2:102053. [Abstract]
- Cell Rep Med. 2023 Feb 21;4(2):100911. [Abstract]
- Cell Death Differ. 2024 Sep;31(9):1140-1156. [Abstract]
- Biomaterials. 2022 Oct:289:121800. [Abstract]
- J Control Release. 2024 Dec:376:829-841. [Abstract]
- Cell Death Dis. 2022 Dec 27;13(12):1075. [Abstract]
- Cell Death Dis. 2022 Jan 13;13(1):55. [Abstract]
- Cancer Lett. 2025 Apr 10:217715. [Abstract]
- Allergy. 2025 May;80(5):1335-1347. [Abstract]
- J Pharm Anal. 2021 Dec;11(6):799-807. [Abstract]
- Genome Med. 2021 Sep 1;13(1):142. [Abstract]
- Cell Death Discov. 2026 Jan 9;12(1):11. [Abstract]
- Cell Death Discov. 2025 May 17;11(1):241. [Abstract]
- Acta Pharmacol Sin. 2021 Jan;42(1):108-114. [Abstract]
- NPJ Precis Oncol. 2026 Apr 8;10(1):211. [Abstract]
- Proc Natl Acad Sci U S A. 2024 May 21;121(21):e2403685121. [Abstract]
- Dev Cell. 2025 Sep 29:S1534-5807(25)00539-8. [Abstract]
- Oncogene. 2023 Sep;42(39):2869-2877. [Abstract]
- Oncogene. 2022 May;41(22):3064-3078. [Abstract]
- Oncogene. 2021 Jul;40(30):4884-4893. [Abstract]
- Oncogene. 2021 Apr;40(14):2596-2609. [Abstract]
- Oncogene. 2017 May 11;36(19):2643-2654. [Abstract]
- Int J Biol Macromol. 2023 Oct 1:250:126147. [Abstract]
- Hum Reprod Open. 2025 May 14;2025(3):hoaf027. [Abstract]
- EMBO J. 2025 Mar;44(5):1464-1487. [Abstract]
- Br J Cancer. 2025 Dec 13. [Abstract]
- Br J Cancer. 2023 Feb;128(4):678-690. [Abstract]
- Stem Cell Res Ther. 2022 Jun 21;13(1):269. [Abstract]
- Cell Rep. 2024 Mar 27;43(4):114002. [Abstract]
- Cell Rep. 2023 May 29;42(6):112570. [Abstract]
- Cell Syst. 2020 Nov 18;11(5):478-494.e9. [Abstract]
- J Med Chem. 2026 Jun 25;69(12):14390-14413. [Abstract]
- J Invest Dermatol. 2019 Jan;139(1):224-234. [Abstract]
- J Ethnopharmacol. 2025 Aug 29:352:120241. [Abstract]
- Virulence. 2022 Dec;13(1):1849-1867. [Abstract]
- Biomater Adv. 2026 Feb 18:183:214782. [Abstract]
- Ecotoxicol Environ Saf. 2024 Oct 15:285:117031. [Abstract]
- Ecotoxicol Environ Saf. 2023 Jan 1:249:114386. [Abstract]
- CNS Neurosci Ther. 2022 Jan;28(1):64-76. [Abstract]
- Biochem Pharmacol. 2025 Jul 18:241:117183. [Abstract]
- Cell Insight. 2022 Jun 16;1(4):100045. [Abstract]
- Anal Chim Acta. 2018 Nov 22:1032:138-146. [Abstract]
- Neurobiol Dis. 2020 Aug;142:104961. [Abstract]
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- Commun Biol. 2021 Dec 13;4(1):1391. [Abstract]
- Mol Cancer Res. 2019 Nov;17(11):2233-2243. [Abstract]
- Respir Res. 2026 May 9. [Abstract]
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- Cell Biol Toxicol. 2021 Apr;37(2):313-330. [Abstract]
- Int J Mol Sci. 2026 Mar 28;27(7):3092. [Abstract]
- Front Pharmacol. 2022 Apr 8;13:879751. [Abstract]
- Front Pharmacol. 2018 Jun 21:9:660. [Abstract]
- J Enzyme Inhib Med Chem. 2025 Dec;40(1):2501743. [Abstract]
- Lung Cancer. 2024 May 9:15:55-67. [Abstract]
- ACS Omega. 2025 Oct 29;10(44):52562-52575. [Abstract]
- J Nutr Biochem. 2023 Sep:119:109399. [Abstract]
- Bioorg Chem. 2025 Aug 9:164:108864. [Abstract]
- Mol Med Rep. 2026 Feb;33(2):77. [Abstract]
- PLoS Pathog. 2024 Aug 5;20(8):e1012437. [Abstract]
- Mol Pharm. 2021 Jul 5;18(7):2495-2506. [Abstract]
- Cancers (Basel). 2022 Jun 5;14(11):2807. [Abstract]
- Stem Cells. 2022 May 27;40(5):508-522. [Abstract]
- Adv Ther. 2024 Jul 18.
- Oncol Rep. 2021 Mar;45(3):1306-1314. [Abstract]
- J Cell Mol Med. 2020 Jan;24(2):1969-1979. [Abstract]
- Oncol Rep. 2016 Dec;36(6):3588-3596. [Abstract]
- Mol Oncol. 2023 Dec;17(12):2618-2636. [Abstract]
- Mol Oncol. 2018 Mar;12(3):305-321. [Abstract]
- Bioengineering (Basel). 2025 Oct 19;12(10):1121. [Abstract]
- Mol Divers. 2025 Jun;29(3):2391-2405. [Abstract]
- Saudi Pharm J. 2023 Oct;31(10):101756. [Abstract]
- Proteomes. 2023 Jun 2;11(2):20. [Abstract]
- Cancer Res Treat. 2023 Oct;55(4):1077-1086. [Abstract]
- Cancer Res Treat. 2023 Jul;55(3):778-803. [Abstract]
- Viruses. 2020 Jun 10;12(6):628. [Abstract]
- Cancer Med. 2024 May;13(10):e7083. [Abstract]
- Mol Carcinog. 2022 Jul;61(7):664-676. [Abstract]
- Exp Cell Res. 2021 Feb 1;399(1):112424. [Abstract]
- Exp Cell Res. 2020 Aug 1;393(1):112054. [Abstract]
- Cancer Med. 2019 Dec;8(18):7793-7808. [Abstract]
- J Cancer. 2024 Mar 25;15(10):2891-2899. [Abstract]
- Breast Cancer Res Treat. 2025 Jun;211(2):467-478. [Abstract]
- PeerJ. 2023 Oct 16:11:e16121. [Abstract]
- Biomed Res Int. 2019 Nov 28;2019:2410845. [Abstract]
- PLoS One. 2026 Apr 24;21(4):e0347843.
- PLoS One. 2024 Nov 1;19(11):e0308647. [Abstract]
- PLoS One. 2018 Jun 14;13(6):e0199208. [Abstract]
- Transbound Emerg Dis. 2026 Apr 13:2026:1766395. [Abstract]
- Cancer Manag Res. 2024 May 28:16:507-525. [Abstract]
- Thorac Cancer. 2020 Oct;11(10):2858-2866. [Abstract]
- Biochem Biophys Res Commun. 2026 Feb 12:800:153165.
- Biochem Biophys Res Commun. 2024 Sep 19:733:150711. [Abstract]
- Biochem Biophys Res Commun. 2022 Dec 25;636(Pt 1):125-131. [Abstract]
- Biol Methods Protoc. 2025 Feb 13;10(1):bpaf012. [Abstract]
- Am J Transl Res. 2020 May 15;12(5):2295-2304. [Abstract]
- J Med Food. 2018 Jul;21(7):701-708. [Abstract]
- Biomed Chromatogr. 2024 Nov 7:e6039. [Abstract]
- Biomed Chromatogr. 2016 Jul;30(7):1150-4. [Abstract]
- Cell Investig. 2026 May 14;2(2):100076.
- bioRxiv. 2026 Apr 15.
- Res Sq. 2026 Apr 28.
- bioRxiv. 2026 Mar 25.
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- bioRxiv. 2026 Jan 17.
- bioRxiv. 2026 Jan 9.
- bioRxiv. 2025 Sep 21.
- Res Sq. 2025 Jun 24:rs.3.rs-6456987. [Abstract]
- Complutense University of Madrid. 2025.
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- bioRxiv. 2024 Dec 20:2024.12.19.629301. [Abstract]
- bioRxiv. 2023 Oct 20:2023.10.19.563158. [Abstract]
- Biomed Pharmacother. 2024 Jun:175:116644. [Abstract]
- Research Square Preprint. 2022 Jun.
- bioRxiv. October 28, 2021.
- SSRN. 31 Aug 2021.
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- bioRxiv. 2019 Sep.
- Oncotarget. 2017 Dec 2;8(68):112313-112329. [Abstract]
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All EGFR Isoforms
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Biological Activity
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EGFR |
OATP2B1 |
β-catenin |
ERK1 |
ERK2 |
GSK-3β |
Erlotinib (CP-358774) (0.01-10 μM; 5 minutes) mesylate potently inhibits human OATP2B1 in MDCKII-OATP2B1 cells, with an IC50 of 0.079 μM[3].
The uptake of Erlotinib (approximately 0.016 μM; 7.5 minutes at pH 7.4 or 5.5) mesylate in MDCKII-OATP2B1 cells is significantly higher than that in wild-type MDCKII cells, with a 2.5-fold increase at pH 7.4 and a 3.3-fold increase at pH 5.5, which confirms that Erlotinib mesylate is a substrate of human OATP2B1[3].
Erlotinib (25 μM; 15 minutes) mesylate is metabolized by recombinant rat CYP3A1 and CYP3A2 into its metabolite OSI-420, with similar formation rates of approximately 0.20 ng/pmol CYP3 per minute[3].
Erlotinib (5-10 μM) mesylate potently inhibits Ephrin A1-induced activation of EGFR and ERK in human gastric cancer cell line NCI-N87[1].
Erlotinib (5-10 μM; 2 weeks) mesylate completely inhibits Ephrin A1-induced anchorage-independent colony formation in the human gastric cancer cell line NCI-N87[1].
Erlotinib (5-10 μM) mesylate significantly inhibits ephrin A1-induced transendothelial migration of human gastric cancer cell line NCI-N87 across human umbilical vein endothelial cell (HUVEC) monolayers[1].
Erlotinib (5-10 μM) mesylate inhibits ephrin A1-induced epithelial-mesenchymal transition (EMT) and EGFR activation in human gastric cancer AGS cells[1].
Erlotinib (5-10 μM) mesylate inhibits Ephrin A1-induced invasion of human gastric cancer AGS cells, with 10 μM achieving nearly complete inhibition[1].
Erlotinib (0.1-3 μM; 5 days) mesylate acts synergistically with the KRASG12D inhibitor MRTX1133 (HY-134813; 1-300 nM) to reduce the viability of Lkb1-knockout 634T mouse lung cancer spheroids, but exerts no such effect on Lkb1-intact 634T spheroids; significant synergistic effects are observed at Erlotinib mesylate concentrations ranging from 100 nM to 3000 nM, with further enhanced efficacy at 1 μM[2].
Erlotinib (2 μM; 1 h pre-incubation followed by 48 h rhMMP-10 exposure) mesylate potently inhibits MMP-10-mediated activation of the EGFR/ERK/GSK-3β/β-catenin signaling pathway and induction of pro-fibrotic markers in HK-2 cells[4].
The IC50 of Erlotinib (0-50 μM; 72 h) mesylate in Erlotinib mesylate-resistant A549 cells is approximately 10-fold that of parental A549 cells[5].
Erlotinib (15-30 μM; 6 months) mesylate induces the formation of an EGFR-independent drug-resistant phenotype in A549 and SK-LU-1 lung cancer cells, whereas Calu-1 cells do not acquire drug resistance under the same conditions[5].
In Erlotinib mesylate-resistant A549 cells, knockdown or knockout of GRHL2, knockdown of HER3, or knockout of E-cadherin all reduce the IC50 of Erlotinib mesylate, indicating that the GRHL2-HER3 axis and E-cadherin-mediated cell adhesion contribute to EGFR bypass resistance via relatively independent pathways[5].
Erlotinib (5 μM; 24 h) mesylate does not induce apoptosis or autophagic cell death in parental or Erlotinib mesylate-resistant A549 non-small cell lung cancer cells[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Lkb1-intact 634T spheroids; Lkb1-knockout 634T spheroids
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Concentration:0.1-3 μM
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Incubation Time:5 days
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Result:Did not produce significant synergism in Lkb1-intact spheroids.
Produced significant synergistic growth inhibition in Lkb1-knockout spheroids, with Bliss scores of 18.24 and 16.24.
Erlotinib at 1 μM markedly enhanced sensitivity to MRTX1133 in Lkb1-knockout spheroids but had minimal sensitizing activity in Lkb1-intact spheroids.
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Cell Line:Parental A549 non-small cell lung cancer (NSCLC) cells, erlotinib-resistant (ER) A549 NSCLC cells
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Concentration:15-30 μM (generate ER cells); 0-50 μM (proliferation assay); 25 μM (crystal violet staining comparison)
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Incubation Time:6 months (generate ER cells); 72 h (proliferation assay, crystal violet staining comparison)
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Result:Exhibited a low half-maximal inhibitory concentration (IC50) for erlotinib-induced proliferation inhibition in parental A549 cells.
Showed dramatically increased erlotinib resistance in ER cells, with an IC50 approximately 10-fold higher than parental cells.
Reduced parental cell density when cultured with 25 μM erlotinib for 72 h.
Maintained high ER cell density when cultured with 25 μM erlotinib for 72 h.
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Cell Line:HK-2
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Concentration:2 μM Erlotinib followed by 100 ng/mL rhMMP-10
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Incubation Time:1 h pretreatment followed by 48 h rhMMP-10 treatment
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Result:Abolished rhMMP-10-induced fibronectin expression and extracellular deposition.
The systemic exposure of Erlotinib (15.5 mg/kg; p.o.; single administration) mesylate and its metabolite OSI-420 in male Wistar rats is not significantly altered by human OATP2B1, but human OATP2B1 increases the mean residence time of OSI-420 by approximately 30%[3].
Erlotinib (40-80 mg/kg/day; oral administration; daily dosing; consecutive 5 days) mesylate alleviates MMP-10-mediated renal injury and fibrotic lesions in UUO mice in a dose-dependent manner by inhibiting the EGFR/ERK/GSK-3β/β-catenin signaling cascade[4].
Erlotinib (25 mg/kg; i.p.; administered daily from Monday to Friday for 4 consecutive weeks) mesylate significantly inhibits the growth of parental A549 non-small cell lung cancer xenografts in nude mice[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (male, 6-8 weeks old, chronic kidney disease induced by unilateral ureteral obstruction surgery plus hydrodynamic-based delivery of Flag-tagged MMP-10 expression vector)[5]
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Dosage:40 mg/kg/day; 80 mg/kg/day
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Administration:p.o.; daily; 5 days
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Result:Dose-dependently reduced renal p-EGFR, p-ERK1/2, p-GSK3β and active β-catenin.
Reduced KIM-1 and MMP-7 expression.
Suppressed fibronectin and α-SMA expression and decreased collagen deposition and renal fibrotic lesions.
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Animal Model:002019 (nude, injected subcutaneously with luciferase-expressing parental A549 NSCLC cells)[6]
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Dosage:25 mg/kg
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Administration:i.p.; daily every Monday through Friday; 4 weeks
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Result:Significantly reduced bioluminescence and tumor weight in parental A549 xenografts.
Did not significantly inhibit the growth of Erlotinib-resistant A549 xenografts, demonstrating in vivo resistance to EGFR inhibition.
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Animal Model:SCID mice (female, 4-5 weeks old) were intravenously inoculated with Ephrin A1-overexpressing NCI-N87 cells (2×106 cells/mouse)[2]
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Dosage:50 mg/kg
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Administration:i.v.; three times per week; 6 weeks
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Result:Markedly reduced lung weight.
Reduced the number of metastatic nodules in lung sections.
Suppressed Ephrin A1/EGFR-dependent gastric cancer lung metastasis.
Chemical Information
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CAS No. 248594-19-6
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Molecular Weight 489.54
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Formula C23H27N3O7S
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SMILES
CS(=O)(O)=O.COCCOC1=CC2=NC=NC(NC3=CC=CC(C#C)=C3)=C2C=C1OCCOC
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Synonyms
CP-358774 mesylate; NSC 718781 mesylate; OSI-774 mesylate
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (143)
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Journal Impact Factor
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Most Recent
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Signal Transduct Target Ther
Selective depletion of tumor-associated SAMHD1 enhances chemotherapeutic efficacy and antitumor immune responses. [Abstract]2025 Dec 15;10(1):406. PMID: 41392286 -
Cancer Cell
A pan-KRAS inhibitor and its derived degrader elicit multifaceted anti-tumor efficacy in KRAS-driven cancers. [Abstract]2025 Jul 25:S1535-6108(25)00310-1. PMID: 40780213 -
Cell Res
Three-dimensional bioprinted glioblastoma microenvironments model cellular dependencies and immune interactions. [Abstract]2020 Oct;30(10):833-853. PMID: 32499560 -
Nat Immunol
Group 3 innate lymphoid cells produce the growth factor HB-EGF to protect the intestine from TNF-mediated inflammation. [Abstract]2022 Feb;23(2):251-261. PMID: 35102343 -
Bioact Mater
Biomimetic hydrogels with mesoscale collagen architecture for patient-derived tumor organoids culture. [Abstract]2024 May 11:38:384-398. PMID: 38764448 -
Bioact Mater
A multifunctional nanotheranostic agent potentiates erlotinib to EGFR wild-type non-small cell lung cancer. [Abstract]2021 Nov 4;13:312-323. PMID: 35224311 -
Nat Cell Biol
An EGFR co-amplified lncRNA HELDR promotes glioblastoma malignancy through KAT7-driven gene programs. [Abstract]2026 Mar 27. PMID: 41896311 -
Cancer Res
Osimertinib covalently binds to CD34 and eliminates myeloid leukemia stem/progenitor cells. [Abstract]2024 Feb 1;84(3):479-492. PMID: 38095536 -
Nat Commun
An alternative EGFR activation by patient-derived R252C mutation promotes cancer progression. [Abstract]2026 Jan 21;17(1):1902. PMID: 41565660 -
Nat Commun
TMEM25 inhibits monomeric EGFR-mediated STAT3 activation in basal state to suppress triple-negative breast cancer progression. [Abstract]2023 Apr 24;14(1):2342. PMID: 37095176 -
Nat Commun
Domain-specific p53 mutants activate EGFR by distinct mechanisms exposing tissue-independent therapeutic vulnerabilities. [Abstract]2023 Mar 28;14(1):1726. PMID: 36977662 -
Nat Commun
AURKB as a target in non-small cell lung cancer with acquired resistance to anti-EGFR therapy. [Abstract]2019 Apr 18;10(1):1812 PMID: 31000705 -
Mol Cell
EGFR promotes ALKBH5 nuclear retention to attenuate N6-methyladenosine and protect against ferroptosis in glioblastoma. [Abstract]2023 Dec 7;83(23):4334-4351.e7. PMID: 37979586 -
Mol Cell
2022 Jul 7;82(13):2443-2457.e7. PMID: 35613620 -
Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
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J Exp Clin Cancer Res
High-throughput drug screening identifies EGFR/MAPK pathway targeting sensitivities in organoid models of ovarian carcinosarcoma. [Abstract]2026 Jan 6;45(1):32. PMID: 41495830 -
J Exp Clin Cancer Res
Dual inhibition of HERs and PD-1 counteract resistance in KRASG12C-mutant head and neck cancer. [Abstract]2024 Nov 20;43(1):308. PMID: 39567998 -
J Exp Clin Cancer Res
2021 Jan 9;40(1):25. PMID: 33422093 -
J Clin Invest
IL-36γ drives skin toxicity induced by EGFR/MEK inhibition and commensal Cutibacterium acnes. [Abstract]2020 Mar 2;130(3):1417-1430. PMID: 31805013 -
Cell Rep Med
HE4 drives PD-L1 expression in myeloid cells via IFN-γR-JAK-STAT3 signaling to promote tumor immune evasion. [Abstract]2026 Apr 21;7(4):102691. PMID: 41861828 -
Cell Rep Med
CAN-Scan: A multi-omic phenotype-driven precision oncology platform identifies prognostic biomarkers of therapy response for colorectal cancer. [Abstract]2025 Apr 2:102053. PMID: 40187357 -
Cell Rep Med
Using patient-derived organoids to predict locally advanced or metastatic lung cancer tumor response: A real-world study. [Abstract]2023 Feb 21;4(2):100911. PMID: 36657446 -
Cell Death Differ
PD-L2 drives resistance to EGFR-TKIs: dynamic changes of the tumor immune environment and targeted therapy. [Abstract]2024 Sep;31(9):1140-1156. PMID: 38816578 -
Biomaterials
2022 Oct:289:121800. PMID: 36166893 -
J Control Release
Macropinocytosis-targeted peptide-docetaxel conjugate for bystander pancreatic cancer treatment. [Abstract]2024 Dec:376:829-841. PMID: 39491626 -
Cell Death Dis
4EBP1 senses extracellular glucose deprivation and initiates cell death signaling in lung cancer. [Abstract]2022 Dec 27;13(12):1075. PMID: 36575176 -
Cell Death Dis
2022 Jan 13;13(1):55. PMID: 35027542 -
Cancer Lett
2025 Apr 10:217715. PMID: 40220852 -
Allergy
Amphiregulin Mediates Epithelial Cell-Eosinophil Interactions and Amplifies Inflammation in Chronic Rhinosinusitis With Nasal Polyps. [Abstract]2025 May;80(5):1335-1347. PMID: 40317745 -
J Pharm Anal
Synergistic effects of methyl 2-cyano-3,11-dioxo-18beta-olean-1,-12-dien-30-oate and erlotinib on erlotinib-resistant non-small cell lung cancer cells. [Abstract]2021 Dec;11(6):799-807. PMID: 35028186 -
Genome Med
2021 Sep 1;13(1):142. PMID: 34470667 -
Cell Death Discov
MSLN-mediated activation of EGFR-ERK1/2 signaling drives liver metastasis in breast cancer. [Abstract]2026 Jan 9;12(1):11. PMID: 41513618 -
Cell Death Discov
Matrix metalloproteinase-10 promotes kidney fibrosis by transactivating β-catenin signaling. [Abstract]2025 May 17;11(1):241. PMID: 40382334 -
Acta Pharmacol Sin
Osimertinib successfully combats EGFR-negative glioblastoma cells by inhibiting the MAPK pathway. [Abstract]2021 Jan;42(1):108-114. PMID: 32398685 -
NPJ Precis Oncol
High-throughput screening identifies NT-1 that synergizes with MRTX1133 against acquired resistant KRASG12D colorectal cancer. [Abstract]2026 Apr 8;10(1):211. PMID: 41951768 -
Proc Natl Acad Sci U S A
Genome-wide CRISPR screens in spheroid culture reveal that the tumor suppressor LKB1 inhibits growth via the PIKFYVE lipid kinase. [Abstract]2024 May 21;121(21):e2403685121. PMID: 38743625 -
Dev Cell
2025 Sep 29:S1534-5807(25)00539-8. PMID: 41027427 -
Oncogene
AXL activates YAP through the EGFR-LATS1/2 axis and confers resistance to EGFR-targeted drugs in head and neck squamous cell carcinoma. [Abstract]2023 Sep;42(39):2869-2877. PMID: 37591955 -
Oncogene
2022 May;41(22):3064-3078. PMID: 35461328 -
Oncogene
2021 Jul;40(30):4884-4893. PMID: 34163029 -
Oncogene
Epiregulin confers EGFR-TKI resistance via EGFR/ErbB2 heterodimer in non-small cell lung cancer. [Abstract]2021 Apr;40(14):2596-2609. PMID: 33750895 -
Oncogene
2017 May 11;36(19):2643-2654. PMID: 27893718
Erlotinib mesylate purchased from MedChemExpress. Usage Cited in: Oncogene. 2017 May 11;36(19):2643-2654. [Abstract]
Effects of anti-cancer agents Oxaliplatin, Erlotinib (25 μM) and cAMP inducer Forskolin (25 μM) on FOXO3 expression in Panc-1 cells are assessed for 72 h (n=3).
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Int J Biol Macromol
CL4-modified exosomes deliver lncRNA DARS-AS1 siRNA to suppress triple-negative breast cancer progression and attenuate doxorubicin resistance by inhibiting autophagy. [Abstract]2023 Oct 1:250:126147. PMID: 37544559 -
Hum Reprod Open
Hypoxia exposure impairs male fertility via inhibiting Septin2-mediated spermatogonial proliferation. [Abstract]2025 May 14;2025(3):hoaf027. PMID: 40487848 -
EMBO J
2025 Mar;44(5):1464-1487. PMID: 39838173 -
Br J Cancer
Fibroblast growth factor signals drive the metastatic behavior in small cell lung cancer. [Abstract]2025 Dec 13. PMID: 41390896 -
Br J Cancer
Drug response profiles in patient-derived cancer cells across histological subtypes of ovarian cancer: real-time therapy tailoring for a patient with low-grade serous carcinoma. [Abstract]2023 Feb;128(4):678-690. PMID: 36476658 -
Stem Cell Res Ther
The metabolism of carbamazepine in humans: steric course of the enzymatic hydrolysis of the 10,11-epoxide. [Abstract]2022 Jun 21;13(1):269. PMID: 3572965 -
Cell Rep
Endocytic activation and exosomal secretion of matriptase stimulate the second wave of EGF signaling to promote skin and breast cancer invasion. [Abstract]2024 Mar 27;43(4):114002. PMID: 38547126 -
Cell Rep
Kinetics of RTK activation determine ERK reactivation and resistance to dual BRAF/MEK inhibition in melanoma. [Abstract]2023 May 29;42(6):112570. PMID: 37252843 -
Cell Syst
Receptor-Driven ERK Pulses Reconfigure MAPK Signaling and Enable Persistence of Drug-Adapted BRAF-Mutant Melanoma Cells. [Abstract]2020 Nov 18;11(5):478-494.e9. PMID: 33113355 -
J Med Chem
Structure-Based Design and Optimization of Novel PHGDH Inhibitors for Overcoming Erlotinib-Resistant Lung Cancer. [Abstract]2026 Jun 25;69(12):14390-14413. PMID: 42263187 -
J Invest Dermatol
2019 Jan;139(1):224-234. PMID: 30081003 -
J Ethnopharmacol
Integrated network pharmacology and experimental validation reveal EGFR/p53/Bcl-2-mediated anti-hepatocellular carcinoma effects of Zedoary Turmeric Oil. [Abstract]2025 Aug 29:352:120241. PMID: 40615101 -
Virulence
Adaptor complex-mediated trafficking of Newcastle disease virus fusion protein is regulated by the YLMY motif of its cytoplasmic tail. [Abstract]2022 Dec;13(1):1849-1867. PMID: 36258290 -
Biomater Adv
Development of a HER1/CP2c dual-targeting biopharmaceutical for HER1-overexpressing head and neck cancer. [Abstract]2026 Feb 18:183:214782. PMID: 41722284 -
Ecotoxicol Environ Saf
Protective role of ghrelin against 6PPD-quinone-induced neurotoxicity in zebrafish larvae (Danio rerio) via the GHSR pathway. [Abstract]2024 Oct 15:285:117031. PMID: 39341137 -
Ecotoxicol Environ Saf
Hyperphosphorylation of EGFR/ERK signaling facilitates long-term arsenite-induced hepatocytes epithelial-mesenchymal transition and liver fibrosis in sprague-dawley rats. [Abstract]2023 Jan 1:249:114386. PMID: 36508792 -
CNS Neurosci Ther
Pharmacological inhibition of epidermal growth factor receptor attenuates intracranial aneurysm formation by modulating the phenotype of vascular smooth muscle cells. [Abstract]2022 Jan;28(1):64-76. PMID: 34729926 -
Biochem Pharmacol
Pitavastatin overcomes multi-drug resistance in CRC and NSCLC by targeting the NRP1-ZFX axis. [Abstract]2025 Jul 18:241:117183. PMID: 40684995 -
Cell Insight
Phosphorylated STYK1 restrains the inhibitory role of EGFR in autophagy initiation and EGFR-TKIs sensitivity. [Abstract]2022 Jun 16;1(4):100045. PMID: 37192859 -
Anal Chim Acta
Development of novel affinity reagents for detecting protein tyrosine phosphorylation based on superbinder SH2 domain in tumor cells. [Abstract]2018 Nov 22:1032:138-146. PMID: 30143211
Erlotinib mesylate purchased from MedChemExpress. Usage Cited in: Anal Chim Acta. 2018 Nov 22:1032:138-146. [Abstract]
30 min after EGF(100 ng/mL) and EGFP-sSH2(Arg)9 (5 μM) are added into the MDA-MB-468 cell culture medium, Erlotinib is added into the cell culture medium (100 nM), and the picture was collected at 30 min after Erlotinib treatment.
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Neurobiol Dis
ErbB1-dependent signalling and vesicular trafficking in primary afferent nociceptors associated with hypersensitivity in neuropathic pain. [Abstract]2020 Aug;142:104961. PMID: 32531343 -
Cell Rep Methods
RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]2023 Oct 23;3(10):100599. PMID: 37797618 -
Cell Rep Methods
2023 Feb 21;3(2):100411. PMID: 36936075 -
Commun Biol
A small-molecule compound D6 overcomes EGFR-T790M-mediated resistance in non-small cell lung cancer. [Abstract]2021 Dec 13;4(1):1391. PMID: 34903832 -
Mol Cancer Res
TAS6417/CLN-081 Is a Pan-Mutation-Selective EGFR Tyrosine Kinase Inhibitor with a Broad Spectrum of Preclinical Activity against Clinically Relevant EGFR Mutations. [Abstract]2019 Nov;17(11):2233-2243. PMID: 31467113 -
Respir Res
TGM2-TUFM promotes acquired resistance to EGFR-TKIs in EGFR-mutated NSCLC through p62-mediated lipophagy. [Abstract]2026 May 9. PMID: 42106683 -
Pharmaceuticals (Basel)
Bufadienolides from Chansu Injection Synergistically Enhances the Antitumor Effect of Erlotinib by Inhibiting the KRAS Pathway in Pancreatic Cancer. [Abstract]2024 Dec 16;17(12):1696. PMID: 39770538 -
Mar Drugs
New Fusarochromanone Derivatives from the Marine Fungus Fusarium equiseti UBOCC-A-117302. [Abstract]2024 Sep 28;22(10):444. PMID: 39452852 -
Cell Biol Toxicol
TRPV3 enhances skin keratinocyte proliferation through EGFR-dependent signaling pathways. [Abstract]2021 Apr;37(2):313-330. PMID: 32535744 -
Int J Mol Sci
Carcinoembryonic Antigen-Related Cell Adhesion Molecule 5 as a Biomarker for Predicting Response to Erlotinib and Gefitinib in Lung Adenocarcinoma: An Integrative Analysis of Transcriptomic Data of PC-9 and Drug-Resistant PC-9 Cell Lines. [Abstract]2026 Mar 28;27(7):3092. PMID: 41977278 -
Front Pharmacol
Transcriptomics and Metabolomics Identify Drug Resistance of Dormant Cell in Colorectal Cancer. [Abstract]2022 Apr 8;13:879751. PMID: 35462906 -
Front Pharmacol
2018 Jun 21:9:660. PMID: 29977207
Erlotinib mesylate purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2018 Jun 21:9:660. [Abstract]
By Western blotting, the α-SMA and palladin proteins are determined in cells that are pretreated with NF-κB (JSH-23), Wnt/β-catenin (XAV939), EGFR (erlotinib), p38 MAPK (TAK-715), and Smad3 (SIS3) inhibitors and are followed by TWEAK stimulation.
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J Enzyme Inhib Med Chem
Natural product sennoside B disrupts liquid-liquid phase separation of SARS-CoV-2 nucleocapsid protein by inhibiting its RNA-binding activity. [Abstract]2025 Dec;40(1):2501743. PMID: 40371698 -
Lung Cancer
HMGB1 Expression Levels Correlate with Response to Immunotherapy in Non-Small Cell Lung Cancer. [Abstract]2024 May 9:15:55-67. PMID: 38741920 -
ACS Omega
Association Study of OATP1B3 Polymorphisms on Hepatic Uptake and Drug-Drug Interaction In Vitro. [Abstract]2025 Oct 29;10(44):52562-52575. PMID: 41244417 -
J Nutr Biochem
High glucose enhances the aggressiveness of lung adenocarcinoma via activating epidermal growth factor receptor/signal transducer and activator of transcription 3 pathways. [Abstract]2023 Sep:119:109399. PMID: 37271322 -
Bioorg Chem
A pomalidomide-based gefitinib PROTAC degrader effectively inhibits lung cancer progression in EGFR-TKIs-acquired resistant models by targeting EGFR degradation and ETFA-mediated ATP generation. [Abstract]2025 Aug 9:164:108864. PMID: 40815992 -
Mol Med Rep
ISX promotes tumor migration and invasion in lung cancer by upregulating COL1A1 in vitro. [Abstract]2026 Feb;33(2):77. PMID: 41480691 -
PLoS Pathog
EGFR-MEK1/2 cascade negatively regulates bactericidal function of bone marrow macrophages in mice with Staphylococcus aureus osteomyelitis. [Abstract]2024 Aug 5;20(8):e1012437. PMID: 39102432 -
Mol Pharm
Combining Gemcitabine-Loaded Macrophage-like Nanoparticles and Erlotinib for Pancreatic Cancer Therapy. [Abstract]2021 Jul 5;18(7):2495-2506. PMID: 34078087 -
Cancers (Basel)
SCAMP3 Regulates EGFR and Promotes Proliferation and Migration of Triple-Negative Breast Cancer Cells through the Modulation of AKT, ERK, and STAT3 Signaling Pathways. [Abstract]2022 Jun 5;14(11):2807. PMID: 35681787 -
Stem Cells
DAPK1 Interacts with the p38 Isoform MAPK14, Preventing Its Nuclear Translocation and Stimulation of Bone Marrow Adipogenesis. [Abstract]2022 May 27;40(5):508-522. PMID: 35403694 -
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Oncol Rep
Repurposing of a monoamine oxidase A inhibitor‑heptamethine carbocyanine dye conjugate for paclitaxel‑resistant non‑small cell lung cancer. [Abstract]2021 Mar;45(3):1306-1314. PMID: 33650669 -
J Cell Mol Med
PRMT5 promotes epithelial-mesenchymal transition via EGFR-β-catenin axis in pancreatic cancer cells. [Abstract]2020 Jan;24(2):1969-1979. PMID: 31851779 -
Oncol Rep
Upregulated CTHRC1 promotes human epithelial ovarian cancer invasion through activating EGFR signaling. [Abstract]2016 Dec;36(6):3588-3596. PMID: 27779718 -
Mol Oncol
Activation of the EGFR/PI3K/AKT pathway limits the efficacy of trametinib treatment in head and neck cancer. [Abstract]2023 Dec;17(12):2618-2636. PMID: 37501404 -
Mol Oncol
TGF-β transactivates EGFR and facilitates breast cancer migration and invasion through canonical Smad3 and ERK/Sp1 signaling pathways. [Abstract]2018 Mar;12(3):305-321. PMID: 29215776
Erlotinib mesylate purchased from MedChemExpress. Usage Cited in: Mol Oncol. 2018 Mar;12(3):305-321. [Abstract]
Western blot analysis of total and phosphorylated EGFR expression in two breast cancer cells pretreated with different concentration Erlotinib for 4h.
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Bioengineering (Basel)
Precision Oncology for High-Grade Gliomas: A Tumor Organoid Model for Adjuvant Treatment Selection. [Abstract]2025 Oct 19;12(10):1121. PMID: 41155119 -
Mol Divers
Design, synthesis and biological evaluation of thienopyridine derivatives as c-Met kinase inhibitors. [Abstract]2025 Jun;29(3):2391-2405. PMID: 39356364 -
Saudi Pharm J
Augmented antitumor effects of erlotinib and cabozantinib on A549 non-small cell lung cancer: In vitro and in vivo studies. [Abstract]2023 Oct;31(10):101756. PMID: 37705877 -
Proteomes
Mass Spectrometry and Pharmacological Approaches to Measuring Cooption and Reciprocal Activation of Receptor Tyrosine Kinases. [Abstract]2023 Jun 2;11(2):20. PMID: 37368466 -
Cancer Res Treat
Establishment of Patient-Derived Organoids Using Ascitic or Pleural Fluid from Cancer Patients. [Abstract]2023 Oct;55(4):1077-1086. PMID: 37309112 -
Cancer Res Treat
MLL4 Regulates the Progression of Non-Small-Cell Lung Cancer by Regulating the PI3K/AKT/SOX2 Axis. [Abstract]2023 Jul;55(3):778-803. PMID: 36701842 -
Viruses
Broad-Spectrum Host-Based Antivirals Targeting the Interferon and Lipogenesis Pathways as Potential Treatment Options for the Pandemic Coronavirus Disease 2019 (COVID-19). [Abstract]2020 Jun 10;12(6):628. PMID: 32532085 -
Cancer Med
Proton pump inhibitors stabilize the expression of PD-L1 on cell membrane depending on the phosphorylation of GSK3β. [Abstract]2024 May;13(10):e7083. PMID: 38752436
Erlotinib mesylate purchased from MedChemExpress. Usage Cited in: Cancer Med. 2024 May;13(10):e7083. [Abstract]
FACS analysis was used to perform the MFI of cell membrane of PD‐L1 in H441 cells with control or multiply small molecular inhibitors (Seen in the Table 1, 24 h) (n = 3). AV412 (HY‐10346; 20, 50 nM), ERK1/2 inhibitor 1 (HY‐112287; 20, 50 nM), AR‐A014418 (HY‐10512; 100, 200 nM), Erlotinib (HY‐50896; 50, 100 nM).
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Mol Carcinog
Epidermal growth factor receptor signaling in precancerous keratinocytes promotes neighboring head and neck cancer squamous cell carcinoma cancer stem cell-like properties and phosphoinositide 3-kinase inhibitor insensitivity. [Abstract]2022 Jul;61(7):664-676. PMID: 35417043 -
Exp Cell Res
HPRT promotes proliferation and metastasis in head and neck squamous cell carcinoma through direct interaction with STAT3. [Abstract]2021 Feb 1;399(1):112424. PMID: 33340493 -
Exp Cell Res
Network-based analysis with primary cells reveals drug response landscape of acute myeloid leukemia. [Abstract]2020 Aug 1;393(1):112054. PMID: 32376287 -
Cancer Med
MYST1/KAT8 contributes to tumor progression by activating EGFR signaling in glioblastoma cells. [Abstract]2019 Dec;8(18):7793-7808. PMID: 31691527
Erlotinib mesylate purchased from MedChemExpress. Usage Cited in: Cancer Med. 2019 Dec;8(18):7793-7808. [Abstract]
Western blots of proteins expression in EGFR signaling pathways in LN229 and U87 cells with MYST1/GFP overexpression after erlotinib (200 ng/mL)/DMSO treatment.
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J Cancer
2024 Mar 25;15(10):2891-2899. PMID: 38706904 -
Breast Cancer Res Treat
2025 Jun;211(2):467-478. PMID: 40055251 -
PeerJ
2023 Oct 16:11:e16121. PMID: 37868048 -
Biomed Res Int
A Pharmacokinetic Interaction Study of Sorafenib and Iced Teas in Rats Using UPLC-MS/MS: An Illustration of Beverage-Drug Interaction. [Abstract]2019 Nov 28;2019:2410845. PMID: 31871933 -
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PLoS One
A novel small molecule screening assay using normal human chondrocytes toward osteoarthritis drug discovery. [Abstract]2024 Nov 1;19(11):e0308647. PMID: 39485774 -
PLoS One
Validated UPLC-MS/MS method for the quantification of dasatinib in plasma: Application to pharmacokinetic interaction studies with nutraceuticals in Wistar rats. [Abstract]2018 Jun 14;13(6):e0199208. PMID: 29902246 -
Transbound Emerg Dis
Numb-Associated Kinases-Mediated AP2M1 Activation Facilitates Porcine Reproductive and Respiratory Syndrome Virus Entry. [Abstract]2026 Apr 13:2026:1766395. PMID: 41982333 -
Cancer Manag Res
Deguelin Restores Paclitaxel Sensitivity in Paclitaxel-Resistant Ovarian Cancer Cells via Inhibition of the EGFR Signaling Pathway. [Abstract]2024 May 28:16:507-525. PMID: 38827785 -
Thorac Cancer
Potential monoamine oxidase A inhibitor suppressing paclitaxel-resistant non-small cell lung cancer metastasis and growth. [Abstract]2020 Oct;11(10):2858-2866. PMID: 32875729 -
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Biochem Biophys Res Commun
Investigating NanoLuc-EGFR engineered cell lines for real-time monitoring of EGFR protein dynamics in live cells. [Abstract]2024 Sep 19:733:150711. PMID: 39312880 -
Biochem Biophys Res Commun
A Beclin 1-targeting stapled peptide synergizes with erlotinib to potently inhibit proliferation of non-small-cell lung cancer cells. [Abstract]2022 Dec 25;636(Pt 1):125-131. PMID: 36332474 -
Biol Methods Protoc
Optimizing drug sensitivity assays in patient-derived tumor organoids: a comparison of IC50 estimation methods and experimental parameters. [Abstract]2025 Feb 13;10(1):bpaf012. PMID: 40060949 -
Am J Transl Res
Ellagic acid inhibits cell proliferation, migration, and invasion in melanoma via EGFR pathway. [Abstract]2020 May 15;12(5):2295-2304. PMID: 32509220 -
J Med Food
Naturally Occurring Hair Growth Peptide: Water-Soluble Chicken Egg Yolk Peptides Stimulate Hair Growth Through Induction of Vascular Endothelial Growth Factor Production. [Abstract]2018 Jul;21(7):701-708. PMID: 29583066 -
Biomed Chromatogr
A novel, sensitive, and fast ultra-high-performance liquid chromatography tandem mass spectrometry method for TNG908 determination in dog plasma and pharmacokinetic study. [Abstract]2024 Nov 7:e6039. PMID: 39510096 -
Biomed Chromatogr
Simultaneous and rapid determination of gefitinib, erlotinib and afatinib plasma levels using liquid chromatography/tandem mass spectrometry in patients with non-small-cell lung cancer. [Abstract]2016 Jul;30(7):1150-4. PMID: 26525154 -
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Res Sq
An EGFR Co-Amplified and De Novo Long Noncoding RNA HELDR Promotes Glioblastoma Malignancy through KAT7-Driven Gene Programs. [Abstract]2025 Jun 24:rs.3.rs-6456987. PMID: 40678238 -
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bioRxiv
BRAFV600 and ErbB inhibitors directly activate GCN2 in an off-target manner to limit cancer cell proliferation. [Abstract]2024 Dec 20:2024.12.19.629301. PMID: 39763857 -
bioRxiv
LKB1 suppresses growth and promotes the internalization of EGFR through the PIKFYVE lipid kinase. [Abstract]2023 Oct 20:2023.10.19.563158. PMID: 37904985 -
Biomed Pharmacother
Interplay of OATP1A/1B/2B1 uptake transporters and ABCB1 and ABCG2 efflux transporters in the handling of bilirubin and drugs. [Abstract]2024 Jun:175:116644. PMID: 38692057 -
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Oncotarget
Molecular-genetic profiling and high-throughput in vitro drug screening in NUT midline carcinoma-an aggressive and fatal disease. [Abstract]2017 Dec 2;8(68):112313-112329. PMID: 29348827
Purity & Documentation
References
[1]. Li S, et al. Ephrin A1 functions as a ligand of EGFR to promote EMT and metastasis in gastric cancer. The EMBO journal. 2025 Mar;44(5):1464-1487. [Content Brief]
[2]. Ferrarone JR, et al. Genome-wide CRISPR screens in spheroid culture reveal that the tumor suppressor LKB1 inhibits growth via the PIKFYVE lipid kinase. Proceedings of the National Academy of Sciences of the United States of America. 2024 May 21;121(21):e2403685121. [Content Brief]
[3]. Rysz MA et al. Erlotinib-A substrate and inhibitor of OATP2B1: pharmacokinetics and CYP3A-mediated metabolism in rSlco2b1-/- and SLCO2B1+/+ rats. Drug Metab Dispos. 2025 May;53(5):100069. [Content Brief]
[4]. Sun X, et al. Matrix metalloproteinase-10 promotes kidney fibrosis by transactivating β-catenin signaling. Cell death discovery. 2025 May 17;11(1):241. [Content Brief]
[5]. Ito F, et al. GRHL2-HER3 and E-cadherin mediate EGFR-bypass drug resistance in lung cancer cells. Frontiers in cell and developmental biology. 2024;12:1511190. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Erlotinib mesylate Related Classifications
HY-12008A Related Classifications
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