Erlotinib-d8
Erlotinib-d8 (CP-358774-d8) is the deuterated-labeled Erlotinib (HY-50896). Erlotinib (CP-358774) is a selective, orally active EGFR tyrosine kinase inhibitor. Erlotinib 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 blocks EGFR phosphorylation, downstream signal transduction, as well as the growth and proliferation of cancer cells. Erlotinib 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 is metabolized via CYP3A to produce the active metabolite OSI-420. Erlotinib 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.: 1266656-97-6
- Formula: C22H15D8N3O4
- Molecular Weight:401.49
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
All EGFR Isoforms
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Biological Activity
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EGFR |
OATP2B1 |
β-catenin |
ERK1 |
ERK2 |
GSK-3β |
1. This compound can be used as a tracer
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.
Chemical Information
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CAS No. 1266656-97-6
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Unlabeled Cas 183321-74-6
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Molecular Weight 401.49
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Formula C22H15D8N3O4
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SMILES
COC([2H])([2H])C([2H])([2H])OC(C(OC([2H])([2H])C([2H])([2H])OC)=C1)=CC2=C1C(NC3=CC(C#C)=CC=C3)=NC=N2
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Synonyms
CP-358774-d8; NSC 718781-d8; OSI-774-d8
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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.
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)
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