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AZM475271

CAT: 0804-HY-13561-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-13561-01Size:5 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
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[2][3][4].
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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
Lck