AZM475271

Modify Date: 2025-08-26 11:39:36

AZM475271 Structure
AZM475271 structure
Common Name AZM475271
CAS Number 476159-98-5 Molecular Weight 442.93800
Density N/A Boiling Point N/A
Molecular Formula C23H27ClN4O3 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of AZM475271


AZM475271 is a potent and selective Src kinase inhibitor with IC50 of 5 nM; no inhibitory activity on Flt3, KDR, Tie-2.IC50 value: 5 nM [1]Target: Src inhibitorin vitro: AZM475271 demonstrated strong dose-dependent inhibition of Src tyrosine kinase activity in the L3.6pl human pancreatic carcinoma cell line. Maximum reduction of Src kinase activity was observed after incubation for 4 hours with ≥5 μmol/L. The IC50 concentration of AZM475271 to inhibit the phosphorylation of c-src, lck, and c-yes was 0.01, 0.03, and 0.08 μmol/L, respectively, in comparison with an IC50 of 0.7 μmol/L AZM475271 to inhibit KDR [2].in vivo: Tumors appeared to be palpable at day 14 after tumor cell injection in all animals except mice treated with both AZM475271 and gemcitabine, in which the earliest possible palpation of the tumors was at day 17 after tumor cell injection. Treatment with gemcitabine or AZM475271 alone did not significantly change animal weight [2].

 Names

Name N-(2-chloro-5-methoxyphenyl)-6-methoxy-7-[(1-methylpiperidin-4-yl)methoxy]quinazolin-4-amine
Synonym More Synonyms

 AZM475271 Biological Activity

Description AZM475271 is a potent and selective Src kinase inhibitor with IC50 of 5 nM; no inhibitory activity on Flt3, KDR, Tie-2.IC50 value: 5 nM [1]Target: Src inhibitorin vitro: AZM475271 demonstrated strong dose-dependent inhibition of Src tyrosine kinase activity in the L3.6pl human pancreatic carcinoma cell line. Maximum reduction of Src kinase activity was observed after incubation for 4 hours with ≥5 μmol/L. The IC50 concentration of AZM475271 to inhibit the phosphorylation of c-src, lck, and c-yes was 0.01, 0.03, and 0.08 μmol/L, respectively, in comparison with an IC50 of 0.7 μmol/L AZM475271 to inhibit KDR [2].in vivo: Tumors appeared to be palpable at day 14 after tumor cell injection in all animals except mice treated with both AZM475271 and gemcitabine, in which the earliest possible palpation of the tumors was at day 17 after tumor cell injection. Treatment with gemcitabine or AZM475271 alone did not significantly change animal weight [2].
Related Catalog
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.

[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.

 Chemical & Physical Properties

Molecular Formula C23H27ClN4O3
Molecular Weight 442.93800
Exact Mass 442.17700
PSA 68.74000
LogP 4.77550
InChIKey WPOXAFXHRJYEIC-UHFFFAOYSA-N
SMILES COc1ccc(Cl)c(Nc2ncnc3cc(OCC4CCN(C)CC4)c(OC)cc23)c1
Storage condition 2-8℃

 AZM475271Bioassay

View more

Name: Bioavailability in male dog
Source: ChEMBL
Target: Canis lupus familiaris
External Id: CHEMBL856631
Name: Antiproliferative activity against p53+/+ human HCT116 cells after 72 hrs by CellTite...
Source: ChEMBL
Target: HCT-116
External Id: CHEMBL4412239
Name: Antiproliferative activity against p53-/- human HCT116 cells after 72 hrs by CellTite...
Source: ChEMBL
Target: HCT-116
External Id: CHEMBL4412240
Name: Antiproliferative activity against human MCF7 cells after 72 hrs by CellTiter 96 aque...
Source: ChEMBL
Target: MCF7
External Id: CHEMBL4412241
Name: Clearance in male dog
Source: ChEMBL
Target: Canis lupus familiaris
External Id: CHEMBL856627
Name: Antiproliferative activity against human A549 cells after 72 hrs by CellTiter 96 aque...
Source: ChEMBL
Target: A549
External Id: CHEMBL4412242
Name: Antiproliferative activity against human NHDF cells after 72 hrs by CellTiter 96 aque...
Source: ChEMBL
Target: NHDF
External Id: CHEMBL4412243
Name: Inhibition of Lyn B (unknown origin) at 0.5 uM preincubated for 10 mins followed by s...
Source: ChEMBL
Target: Tyrosine-protein kinase Lyn
External Id: CHEMBL4412229
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 Synonyms

Methoxy Aniline 7
AZM475271
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