AZM475271

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].

Product Specifications

CAS Number

[476159-98-5]

Product Name Alternative

M475271

UNSPSC

12352005

Hazard Statement

H301

Target

Apoptosis; Src

Type

Reference compound

Related Pathways

Apoptosis; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/AZM475271.html

Purity

99.89

Solubility

DMSO : ≥ 42 mg/mL

Smiles

CN1CCC(COC2=CC3=NC=NC(NC4=CC(OC)=CC=C4Cl)=C3C=C2OC)CC1

Molecular Formula

C23H27ClN4O3

Molecular Weight

442.94

Precautions

H301

References & Citations

[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.|[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.|[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.