476159-98-5
476159-98-5
Chemical Structure
AZM475271
Synonym(s): M475271
- CAS. Nr.: 476159-98-5
- Formula:C23H27ClN4O3
- Molecular Weight:442.94
IUPAC Name: N-(2-chloro-5-methoxyphenyl)-6-methoxy-7-((1-methylpiperidin-4-yl)methoxy)quinazolin-4-amine
InChIKey: WPOXAFXHRJYEIC-UHFFFAOYSA-N
SMILES: CN1CCC(COC2=CC3=NC=NC(NC4=CC(OC)=CC=C4Cl)=C3C=C2OC)CC1
Biological Activity: AZM475271 (M475271) is an orally active and selective Src kinase inhibitor. AZM475271 inhibits phosphorylation of c-Src kinase, Lck, c-yes (IC50s = 0.01, 0.03, 0.08 μM, respectively). AZM475271 induces apoptosis. AZM475271 reduces tumor cell proliferation and migration in vitro and in vivo, and reduces microvessel density (MVD). AZM475271 inhibits tumor growth and metastasis. AZM475271 sensitizes tumor cells to the cytotoxic effects of Gemcitabine (HY-17026)[1][2][3][4].
| Art. -Nr. | Produktname | Reinheit | Beschreibung | Pricing | |||||||||||||||||||
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AZM475271 | 99.89% | AZM475271 (M475271) is an orally active and selective Src kinase inhibitor. AZM475271 inhibits phosphorylation of c-Src kinase, Lck, c-yes (IC50s = 0.01, 0.03, 0.08 μM, respectively). AZM475271 induces apoptosis. AZM475271 reduces tumor cell proliferation and migration in vitro and in vivo, and reduces microvessel density (MVD). AZM475271 inhibits tumor growth and metastasis. AZM475271 sensitizes tumor cells to the cytotoxic effects of Gemcitabine (HY-17026). | ||||||||||||||||||||
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Vandetanib trifluoroacetate | Vandetanib trifluoroacetate (D6474 trifluoroacetate) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC50=40 nM). Vandetanib trifluoroacetate also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC50=110 nM) and EGFR/HER1 (IC50=500 nM). | |||||||||||||||||||||
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Vandetanib hydrochloride | Vandetanib hydrochloride (D6474 hydrochloride) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC50=40 nM). Vandetanib hydrochloride also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC50=110 nM) and EGFR/HER1 (IC50=500 nM). | |||||||||||||||||||||
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Vandetanib (Standard) | ≥98% | Vandetanib (Standard) is the analytical standard of Vandetanib. This product is intended for research and analytical applications. Vandetanib (D6474) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC50=40 nM). Vandetanib also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC50=110 nM) and EGFR/HER1 (IC50=500 nM). | ||||||||||||||||||||
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Vandetanib-13C6 | Vandetanib-13C6 is a 13C labeled Vandetanib (HY-10260). Vandetanib (D6474) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC50=40 nM). Vandetanib also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC50=110 nM) and EGFR/HER1 (IC50=500 nM). | |||||||||||||||||||||
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LDDN-0003499 | LDDN-0003499 is a Src family tyrosine kinase inhibitor and anti-inflammatory agent. LDDN-0003499 reduces basal and Aβ-stimulated levels of active, phosphorylated Lyn and Src kinases, and attenuates Aβ-stimulated secretion of pro-inflammatory cytokines TNFα and IL-6 in microglial cells. LDDN-0003499 can be used for the research of Alzheimer's disease. | |||||||||||||||||||||
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Tesevatinib | 99.41% | Tesevatinib (XL-647) is an orally available, blood-brain barrier-penetrant inhibitor of the epidermal growth factor receptor (EGFR). Tesevatinib significantly reduces cellular viability, with IC50 values of 11 nM and 102 nM in GBM12 and GBM6, respectively. Tesevatinib also inhibits HER2 (IC50=16.1 nM), VEGFR2 (IC50=1.5 nM), and Src (IC50=10.3 nM). Tesevatinib can inhibit tumor proliferation and exhibits antitumor activity. | ||||||||||||||||||||
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EGFR-IN-91 | EGFR-IN-91 (compound 9) is an orally available EGFR inhibitor with blood-brain barrier penetrability. EGFR-IN-91 inhibits EGFRL858R/C797S and EGFRexon 19del/C797S, inducing tumor regression in xenograft (PDX) mouse models. EGFR-IN-91 has the potential to inhibit localized and metastatic non-small cell lung cancer (NSCLC) driven by EGFR mutants. | |||||||||||||||||||||
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EGFR/C797S-IN-1 | EGFR/C797S-IN-1 is a potent EGFR-C797S inhibitor with an IC50 value of 0.128 µM. EGFR/C797S-IN-1 shows anti-proliferative activity and anti-tumor activity. EGFR/C797S-IN-1 inhibits the expression of p-EGFR in a dose-dependent manner. | |||||||||||||||||||||
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EGFR-IN-126 | EGFR-IN-126 (compound 9d) is a potent inhibitor of EGFRL858R/T790M/C797S, with the IC50 value of 0.005 μM. EGFR-IN-126 shows antitumor effects in vivo and in vitro. | |||||||||||||||||||||
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M387783 | M387783 is an oxidative metabolite of Gefitinib (HY-50895). M387783 is commonly used in pharmacokinetic and metabolic pathway studies. | |||||||||||||||||||||
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References
- [1]. Plé PA, et al. Discovery of a new class of anilinoquinazoline inhibitors with high affinity and specificity for the tyrosine kinase domain of c-Src. J Med Chem. 2004 Feb 12;47(4):871-87. [Content Brief]
- [2]. Yezhelyev MV, et al. Inhibition of SRC tyrosine kinase as treatment for human pancreatic cancer growing orthotopically in nude mice. Clin Cancer Res. 2004 Dec 1;10(23):8028-36. [Content Brief]
- [3]. Bartscht T, et al. TGF-β Signal Transduction in Pancreatic Carcinoma Cells is Sensitive to Inhibition by the Src Tyrosine Kinase Inhibitor AZM475271. Anticancer Agents Med Chem. 2017;17(7):966-972. [Content Brief]
- [4]. Wang Y, et al. Smooth muscle contraction and growth of stromal cells in the human prostate are both inhibited by the Src family kinase inhibitors, AZM475271 and PP2. Br J Pharmacol. 2016 Dec;173(23):3342-3358. [Content Brief]
