AG-1478 hydrochloride
Based on 51 publication(s) in Google Scholar
AG-1478 hydrochloride (Tyrphostin AG-1478 hydrochloride) is a selective EGFR tyrosine kinase inhibitor with IC50 of 3 nM. AG-1478 hydrochloride has antiviral effects against HCV and encephalomyocarditis virus (EMCV).
For research use only. We do not sell to patients.
- CAS No.: 170449-18-0
- Formula: C16H15Cl2N3O2
- Molecular Weight:352.22
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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
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Publications Citing Use of MedChemExpress (MCE) AG-1478 hydrochloride
More- Nat Commun. 2025 May 27;16(1):4887. [Abstract]
- Nat Commun. 2024 Jul 12;15(1):5874. [Abstract]
- Adv Sci (Weinh). 2023 Jun;10(16):e2204824. [Abstract]
- Cell Death Dis. 2024 Jun 12;15(6):411. [Abstract]
- Cell Death Dis. 2021 May 18;12(6):509. [Abstract]
- Cell Death Dis. 2020 Jun 15;11(6):459. [Abstract]
- Cell Death Dis. 2019 Sep 9;10(9):649. [Abstract]
- Cell Death Discov. 2024 Jul 19;10(1):329. [Abstract]
- Nat Struct Mol Biol. 2025 May;32(5):853-863. [Abstract]
- Proc Natl Acad Sci U S A. 2026 Jul 7;123(27):e2523789123.
- Oncogene. 2021 Jul;40(30):4884-4893. [Abstract]
- Int J Biol Macromol. 2024 Jun;269(Pt 2):132025. [Abstract]
- Int J Mol Med. 2026 May;57(5):122. [Abstract]
- EMBO J. 2024 Apr;43(8):1388-1419. [Abstract]
- Br J Pharmacol. 2026 May 31. [Abstract]
- J Invest Dermatol. 2023 May;143(5):832-841.e4. [Abstract]
- Cancer Cell Int. 2021 Jun 5;21(1):291. [Abstract]
- Cancer Cell Int. 2019 Sep 23:19:241. [Abstract]
- Virulence. 2026 Dec;17(1):2602261. [Abstract]
- J Agric Food Chem. 2020 Jan 15;68(2):512-522. [Abstract]
- Ecotoxicol Environ Saf. 2024 Jan 1:269:115756. [Abstract]
- Life Sci. 2025 Feb 1:362:123358. [Abstract]
- Precis Clin Med. 2021 Aug 28;4(4):215-230. [Abstract]
- Neurobiol Dis. 2020 Aug:142:104961. [Abstract]
- Front Microbiol. 2022 Jun 30;13:894356. [Abstract]
- ACS Omega. 2022 Oct 26;7(44):39760-39771. [Abstract]
- Sci Rep. 2017 Jan 19:7:40802. [Abstract]
- Neoplasia. 2021 Jun;23(6):607-623. [Abstract]
- Neuropharmacology. 2021 Sep 15:196:108703. [Abstract]
- J Cell Mol Med. 2020 Nov;24(22):12994-13009. [Abstract]
- Oncol Rep. 2016 Dec;36(6):3588-3596. [Abstract]
- J Inflamm Res. 2026 Jun 19:19:596461. [Abstract]
- J Nutr. 2020 Apr 1;150(4):756-762. [Abstract]
- J Virol. 2021 Feb 24;95(10):e02436-20. [Abstract]
- Development. 2025 Apr 1;152(7):dev204618. [Abstract]
- Food Sci Biotechnol. 2025 Feb 24;34(10):2281-2294. [Abstract]
- J Steroid Biochem Mol Biol. 2021 Nov:214:106001. [Abstract]
- J Cell Biochem. 2018 Mar;119(3):2911-2922. [Abstract]
- Vet Microbiol. 2026 Jun 12:320:111114. [Abstract]
- J Anim Physiol Anim Nutr. 2025 Mar;109(2):610-622. [Abstract]
- PLoS One. 2021 Sep 14;16(9):e0256870. [Abstract]
- Biochem Biophys Res Commun. 2021 Oct 8:573:86-92. [Abstract]
- Sex Med. 2025 Aug 6;13(4):qfaf059. [Abstract]
- ChemistrySelect. 2023 Jan 12.
- ORL J Otorhinolaryngol Relat Spec. 2021;83(5):310-318. [Abstract]
- bioRxiv. 2023 Oct 2.
- Research Square Preprint. 2023 Jul 10.
- Environ Toxicol. 2023 May;38(5):1133-1142. [Abstract]
- bioRxiv. 2023 Feb 13, 528249.
- Biomed Pharmacother. 2022 Apr:148:112665. [Abstract]
- Research Square Preprint. 2020 Dec.
Customer Validation & Images
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WB
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Cell Imaging/Staining
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IF
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In Vivo Efficacy Study
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IF
All EGFR Isoforms
More
Biological Activity
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EGFR 3 nM (IC50) |
HCV |
EMCV |
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Cell Line
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Type | Value | Description | References |
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| A-431 | IC50 |
1.26 nM
Compound: 11b
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Displacement of [125I]4-(3-iodoanilino)-6,7-dimethoxyquinazoline from EGFR tyrosine kinase in human A431 cell membranes
Displacement of [125I]4-(3-iodoanilino)-6,7-dimethoxyquinazoline from EGFR tyrosine kinase in human A431 cell membranes
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[PMID: 16279804] |
| BaF3 | IC50 |
0.8 nM
Compound: 11b
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Inhibition of human EGFR tyrosine kinase phosphorylation expressed in mouse BaF3 cells
Inhibition of human EGFR tyrosine kinase phosphorylation expressed in mouse BaF3 cells
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[PMID: 16279804] |
| Jurkat | IC50 |
5 μM
Compound: 4
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Inhibition of p56lck kinase autophosphorylation in Jurkat cells
Inhibition of p56lck kinase autophosphorylation in Jurkat cells
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10.1016/S0960-894X(97)00034-6 |
| MCF-10A | IC50 |
173 nM
Compound: 11b
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Inhibition of DNA synthesis in EGF-dependent human MCF10A cells assessed as [3H]thymidine incorporation
Inhibition of DNA synthesis in EGF-dependent human MCF10A cells assessed as [3H]thymidine incorporation
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[PMID: 16279804] |
| MCF7 | IC50 |
1982 nM
Compound: 11b
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Inhibition of DNA synthesis in EGF-independent human MCF7 cells assessed as 3H]thymidine incorporation
Inhibition of DNA synthesis in EGF-independent human MCF7 cells assessed as 3H]thymidine incorporation
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[PMID: 16279804] |
AG-1478 (AG1478) is irreversible for growth regulation of human lung (A549) and prostate (DU145) cancer cell lines, cultured in chemically defined DMEM/F12 medium. AG-1478 seems to be more effective at lower concentrations, but is unable to completely inhibit growth of A549 cells[1]. Inhibition of EGFR by specific tyrosine kinase inhibitor AG-1478 (AG1478) significantly decreases the angiotensin II-mediated synthesis of TGF-β and fibronectin by cardiac fibroblasts. EGFR is pharmacologically inhibited by small-molecule inhibitor AG-1478 with IC50 of 4 nM[2]. Both Polyfect (PF) and Superfect (SF) treatment lead to increased apoptosis in HEK 293 cells to a similar extent as assessed by flow cytometry. The antioxidant, tempol, significantly reduced dendrimer-mediated apoptosis for both PF and SF. AG-1478 (AG1478), at a 10-fold higher dose (100 μM) than used in signaling studies, is used as a positive control and significantly induced apoptosis in HEK 293 cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 170449-18-0
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Molecular Weight 352.22
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Formula C16H15Cl2N3O2
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SMILES
COC1=CC2=NC=NC(NC3=CC=CC(Cl)=C3)=C2C=C1OC.[H]Cl
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Synonyms
Tyrphostin AG-1478 hydrochloride; NSC 693255 hydrochloride
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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 (51)
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Journal Impact Factor
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Most Recent
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Nat Commun
Clustering of NLRP3 induced by membrane or protein scaffolds promotes inflammasome assembly. [Abstract]2025 May 27;16(1):4887. PMID: 40425567 -
Nat Commun
Therapeutic potential of the secreted Kazal-type serine protease inhibitor SPINK4 in colitis. [Abstract]2024 Jul 12;15(1):5874. PMID: 38997284
AG-1478 hydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Jul 12;15(1):5874. [Abstract]
AG-1478 (10 μM; 48 h) influenced the direct downstream target of the EGFR pathway in NCM460 cells.
AG-1478 hydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Jul 12;15(1):5874. [Abstract]
Morphological images and expression of proliferative cells (yellow: Ki67), Paneth cells (red: Lyz), and enteroendocrine cells (green: CgA) in organoids derived from WT and cKO mice with or without the stimulation of AG-1478 (10 μM; 48 h).
AG-1478 hydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Jul 12;15(1):5874. [Abstract]
Typical fluorescent images of intestinal organoids from WT and KO mice including MUC2 (green), E-cadherin (red), and DAPI (blue), with AG-1478 (10 μM; 48 h) stimulation under inflammatory conditions (50 ng/mL TNF-α treatment).
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Adv Sci (Weinh)
Neuregulin4 Acts on Hypothalamic ErBb4 to Excite Oxytocin Neurons and Preserve Metabolic Homeostasis. [Abstract]2023 Jun;10(16):e2204824. PMID: 37060105
AG-1478 hydrochloride purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2023 Jun;10(16):e2204824. [Abstract]
ErbB4 antagonist AG‐1478 (20 nM; i.c.v.) markedly attenuated the effects of rNrg4 on food intake and body weight of HFD‐fed ErbB4 CreER mice.
AG-1478 hydrochloride purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2023 Jun;10(16):e2204824. [Abstract]
AG-1478 (20 nM; i.c.v.) inhibited the increased number of c-Fos+ cells in the PVN of ErbB4 CreER mice induced by rNrg4.
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Cell Death Dis
MAL2 reprograms lipid metabolism in intrahepatic cholangiocarcinoma via EGFR/SREBP-1 pathway based on single-cell RNA sequencing. [Abstract]2024 Jun 12;15(6):411. PMID: 38866777 -
Cell Death Dis
Sodium/glucose cotransporter 1-dependent metabolic alterations induce tamoxifen resistance in breast cancer by promoting macrophage M2 polarization. [Abstract]2021 May 18;12(6):509. PMID: 34006822 -
Cell Death Dis
Brd4 inhibition ameliorates Pyocyanin-mediated macrophage dysfunction via transcriptional repression of reactive oxygen and nitrogen free radical pathways. [Abstract]2020 Jun 15;11(6):459. PMID: 32541671 -
Cell Death Dis
Protease Nexin I is a feedback regulator of EGF/PKC/MAPK/EGR1 signaling in breast cancer cells metastasis and stemness. [Abstract]2019 Sep 9;10(9):649. PMID: 31501409 -
Cell Death Discov
2024 Jul 19;10(1):329. PMID: 39030174 -
Nat Struct Mol Biol
ERK-USP9X-coupled regulation of thymidine kinase 1 promotes both its enzyme activity-dependent and its enzyme activity-independent functions for tumor growth. [Abstract]2025 May;32(5):853-863. PMID: 39824978 -
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Oncogene
2021 Jul;40(30):4884-4893. PMID: 34163029 -
Int J Biol Macromol
2024 Jun;269(Pt 2):132025. PMID: 38704076 -
Int J Mol Med
2026 May;57(5):122. PMID: 41823548 -
EMBO J
The growth factor EPIREGULIN promotes basal progenitor cell proliferation in the developing neocortex. [Abstract]2024 Apr;43(8):1388-1419. PMID: 38514807 -
Br J Pharmacol
CKLF-like MARVEL transmembrane domain-containing superfamily 8 (CMTM8) promotes Notch signalling to maintain CD8+ T cell- and NK cell-dependent tumour immune escape. [Abstract]2026 May 31. PMID: 42219547 -
J Invest Dermatol
Cathelicidin Antimicrobial Peptide LL37 Induces TLR8 and Amplifies IL-36γ and IL-17C in Human Keratinocytes. [Abstract]2023 May;143(5):832-841.e4. PMID: 36496195 -
Cancer Cell Int
Construction of a prognostic model with histone modification-related genes and identification of potential drugs in pancreatic cancer. [Abstract]2021 Jun 5;21(1):291. PMID: 34090418 -
Cancer Cell Int
Phenyllactic acid promotes cell migration and invasion in cervical cancer via IKK/NF-κB-mediated MMP-9 activation. [Abstract]2019 Sep 23:19:241. PMID: 31572058 -
Virulence
Streptococcus mutans-derived extracellular vesicles promote herpes simplex virus infection in oral epithelia. [Abstract]2026 Dec;17(1):2602261. PMID: 41379645 -
J Agric Food Chem
TLR2/EGFR Are Two Sensors for pBD3 and pEP2C Induction by Sodium Butyrate Independent of HDAC Inhibition. [Abstract]2020 Jan 15;68(2):512-522. PMID: 31870150 -
Ecotoxicol Environ Saf
Perinatal triphenyl phosphate exposure induces metabolic dysfunctions through the EGFR/ERK/AKT signaling pathway: Mechanistic in vitro and in vivo studies. [Abstract]2024 Jan 1:269:115756. PMID: 38056125 -
Life Sci
MCP-enhanced SOD3 activity inhibits gastric cancer and potentiate chemotherapy via modulating EGFR signaling. [Abstract]2025 Feb 1:362:123358. PMID: 39746602 -
Precis Clin Med
Repurposable drugs for SARS-CoV-2 and influenza sepsis with scRNA-seq data targeting post-transcription modifications. [Abstract]2021 Aug 28;4(4):215-230. PMID: 34993416 -
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 -
Front Microbiol
EGFR Activation Impairs Antiviral Activity of Interferon Signaling in Brain Microvascular Endothelial Cells During Japanese Encephalitis Virus Infection. [Abstract]2022 Jun 30;13:894356. PMID: 35847084 -
ACS Omega
ATP Promotes Oral Squamous Cell Carcinoma Cell Invasion and Migration by Activating the PI3K/AKT Pathway via the P2Y2-Src-EGFR Axis. [Abstract]2022 Oct 26;7(44):39760-39771. PMID: 36385800 -
Sci Rep
Acetylcholine acts through M3 muscarinic receptor to activate the EGFR signaling and promotes gastric cancer cell proliferation. [Abstract]2017 Jan 19:7:40802. PMID: 28102288
AG-1478 hydrochloride purchased from MedChemExpress. Usage Cited in: Sci Rep. 2017 Jan 19:7:40802. [Abstract]
EGFR participates the process of ACh induced cell proliferation and signaling transduction. After adding 10 μM EGFR specific inhibitor AG1478 2 h prior to ACh addition, protein changes are analyzed by western blot.
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Neoplasia
STAMBP promotes lung adenocarcinoma metastasis by regulating the EGFR/MAPK signaling pathway. [Abstract]2021 Jun;23(6):607-623. PMID: 34102455 -
Neuropharmacology
Activation of the spinal EGFR signaling pathway in a rat model of cancer-induced bone pain with morphine tolerance. [Abstract]2021 Sep 15:196:108703. PMID: 34260958 -
J Cell Mol Med
LncRNA ARAP1-AS2 promotes high glucose-induced human proximal tubular cell injury via persistent transactivation of the EGFR by interacting with ARAP1. [Abstract]2020 Nov;24(22):12994-13009. PMID: 32969198 -
Oncol Rep
Upregulated CTHRC1 promotes human epithelial ovarian cancer invasion through activating EGFR signaling. [Abstract]2016 Dec;36(6):3588-3596. PMID: 27779718 -
J Inflamm Res
Salvianic Acid A Regulates Ferroptosis by Activating the Nrf2-GPX4 Pathway Through EGFR to Protect Myocardial Ischemia-Reperfusion Injury. [Abstract]2026 Jun 19:19:596461. PMID: 42345001 -
J Nutr
Human Milk Oligosaccharides Activate Epidermal Growth Factor Receptor and Protect Against Hypoxia-Induced Injuries in the Mouse Intestinal Epithelium and Caco2 Cells. [Abstract]2020 Apr 1;150(4):756-762. PMID: 31915826 -
J Virol
Microfilaments and microtubules alternately coordinate the multi-step endosomal trafficking of Classical Swine Fever Virus. [Abstract]2021 Feb 24;95(10):e02436-20. PMID: 33627389 -
Development
Inhibition of HDAC4 in granulosa cells improved co-cultured oocyte maturation in vitro independent of LH in porcine. [Abstract]2025 Apr 1;152(7):dev204618. PMID: 40066659 -
Food Sci Biotechnol
Thymol promotes cell proliferation and protects against LPS-induced intestinal inflammation via activation of the EGFR/PI3K pathway. [Abstract]2025 Feb 24;34(10):2281-2294. PMID: 40351714 -
J Steroid Biochem Mol Biol
Dihydrotestosterone regulation of cyclooxygenase-2 expression in bovine endometrial epithelium cells by androgen receptor mediated EGFR/PI3K/Akt pathway. [Abstract]2021 Nov:214:106001. PMID: 34547381 -
J Cell Biochem
Epiregulin (EREG) is upregulated through an IL-1β autocrine loop in Caco-2 epithelial cells with reduced CFTR function. [Abstract]2018 Mar;119(3):2911-2922. PMID: 29091309 -
Vet Microbiol
Curcumin maintains pseudorabies virus latent infection by inhibiting the phosphorylation level of EGFR protein. [Abstract]2026 Jun 12:320:111114. PMID: 42296914 -
J Anim Physiol Anim Nutr
Dihydromyricetin Suppresses Lipopolysaccharide-Induced Intestinal Injury Through Reducing Reactive Oxygen Species Generation and NOD-Like Receptor Pyrin Domain Containing 3 Inflammasome Activation. [Abstract]2025 Mar;109(2):610-622. PMID: 39618421 -
PLoS One
2021 Sep 14;16(9):e0256870. PMID: 34520454 -
Biochem Biophys Res Commun
Extracellular AGR2 activates neighboring fibroblasts through endocytosis and direct binding to β-catenin that requires AGR2 dimerization and adhesion domains. [Abstract]2021 Oct 8:573:86-92. PMID: 34399098 -
Sex Med
Hinokiflavone alleviates high-fat diet-induced erectile dysfunction via the EGFR/PI3K/Akt/eNOS signaling pathway. [Abstract]2025 Aug 6;13(4):qfaf059. PMID: 40808867 -
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ORL J Otorhinolaryngol Relat Spec
Human Neutrophil Elastase Mediates MUC5AC Hypersecretion via the Tumour Necrosis Factor-α Converting Enzyme-Epidermal Growth Factor Receptor Signalling Pathway in vivo. [Abstract]2021;83(5):310-318. PMID: 34130299 -
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Environ Toxicol
Comparative study of cigarette smoke, Klebsiella pneumoniae, and their combination on airway epithelial barrier function in mice. [Abstract]2023 May;38(5):1133-1142. PMID: 36757011
AG-1478 hydrochloride purchased from MedChemExpress. Usage Cited in: Environ Toxicol. 2023 May;38(5):1133-1142. [Abstract]
AG1478 (2 μM) suppresses the phosphorylation of EGFR and ERK1/2 and subsequently upregulates the expression of ZO-1 and occludin in BEAS-2B cells.
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Biomed Pharmacother
PI3K inhibitor 3-MA promotes the antiproliferative activity of esomeprazole in gastric cancer cells by downregulating EGFR via the PI3K/FOXO3a pathway. [Abstract]2022 Apr:148:112665. PMID: 35228068 -
Purity & Documentation
References
[1]. Bojko A, et al. The effect of tyrphostins AG494 and AG1478 on the autocrine growth regulation of A549 and DU145 cells. Folia Histochem Cytobiol. 2012 Jul 5;50(2):186-95. [Content Brief]
[2]. Li W, et al. EGFR Inhibition Blocks Palmitic Acid-induced inflammation in cardiomyocytes and Prevents Hyperlipidemia-induced Cardiac Injury in Mice. Sci Rep. 2016 Apr 18;6:24580. [Content Brief]
[3]. Akhtar S, et al. Cationic Polyamidoamine Dendrimers as Modulators of EGFR Signaling In Vitro and In Vivo. PLoS One. 2015 Jul 13;10(7):e0132215. [Content Brief]
[4]. Dorobantu CM, et al. Tyrphostin AG1478 Inhibits Encephalomyocarditis Virus and Hepatitis C Virus by Targeting Phosphatidylinositol 4-Kinase IIIα. Antimicrob Agents Chemother. 2016 Sep 23;60(10):6402-6. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
AG-1478 hydrochloride Related Classifications
HY-13524A Related Classifications
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