1. Protein Tyrosine Kinase/RTK
  2. Src
  3. AZM475271

AZM475271 is an orally active and selective Src kinase inhibitor. AZM475271 inhibits phosphorylation of c-Src kinase, Lck, c-yes (IC50s = 0.01, 0.03, 0.08μM, respectively). AZM475271 induces apoptosis. AZM475271 reduces tumor cell proliferation and migration in vitro an 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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AZM475271 Chemical Structure

AZM475271 Chemical Structure

CAS No. : 476159-98-5

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Description

AZM475271 is an orally active and selective Src kinase inhibitor. AZM475271 inhibits phosphorylation of c-Src kinase, Lck, c-yes (IC50s = 0.01, 0.03, 0.08μM, respectively). AZM475271 induces apoptosis. AZM475271 reduces tumor cell proliferation and migration in vitro an 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].

IC50 & Target

Lck

0.03 μM (IC50)

Cellular Effect
Cell Line Type Value Description References
A549 IC50
> 25 μM
Compound: AZM475271
Antiproliferative activity against human A549 cells after 72 hrs by CellTiter 96 aqueous one solution assay
Antiproliferative activity against human A549 cells after 72 hrs by CellTiter 96 aqueous one solution assay
[PMID: 30562697]
A549 IC50
0.48 μM
Compound: 35, M475271
Inhibition of A549 cell migration by microdroplet migration assay
Inhibition of A549 cell migration by microdroplet migration assay
[PMID: 17064066]
HCT-116 IC50
> 25 μM
Compound: AZM475271
Antiproliferative activity against p53+/+ human HCT116 cells after 72 hrs by CellTiter 96 aqueous one solution assay
Antiproliferative activity against p53+/+ human HCT116 cells after 72 hrs by CellTiter 96 aqueous one solution assay
[PMID: 30562697]
HCT-116 IC50
> 25 μM
Compound: AZM475271
Antiproliferative activity against p53-/- human HCT116 cells after 72 hrs by CellTiter 96 aqueous one solution assay
Antiproliferative activity against p53-/- human HCT116 cells after 72 hrs by CellTiter 96 aqueous one solution assay
[PMID: 30562697]
MCF7 IC50
> 25 μM
Compound: AZM475271
Antiproliferative activity against human MCF7 cells after 72 hrs by CellTiter 96 aqueous one solution assay
Antiproliferative activity against human MCF7 cells after 72 hrs by CellTiter 96 aqueous one solution assay
[PMID: 30562697]
NHDF IC50
> 25 μM
Compound: AZM475271
Antiproliferative activity against human NHDF cells after 72 hrs by CellTiter 96 aqueous one solution assay
Antiproliferative activity against human NHDF cells after 72 hrs by CellTiter 96 aqueous one solution assay
[PMID: 30562697]
Sf9 IC50
5 nM
Compound: 56; AZM475271
Inhibition of human recombinant Src expressed in baculovirus infected Sf9 insect cells assessed as reduction in phosphorylation of polyglutamic acid/tyrosine incubated for 15 mins by ELISA
Inhibition of human recombinant Src expressed in baculovirus infected Sf9 insect cells assessed as reduction in phosphorylation of polyglutamic acid/tyrosine incubated for 15 mins by ELISA
[PMID: 30878832]
In Vitro

AZM475271 inhibits the proliferation of c-Src3T3 (transfected in fibroblast cells, 24 h, IC50 = 0.53 μM) and A549 (72 h, IC50 = 0.48μM) cells[1][2].
AZM475271 (1-20 μM, 48 h) shows no anti-proliferative effect on L3.6pl human pancreatic carcinoma cells in vitro below 15 μM, but induces cell death at 20 μM[2].
AZM475271 (5 μM, 12 h) induces apoptosis and the effect can be enhanced by combination with Gemcitabine in L3.6pl cells[2].
AZM475271 (0.1-5 μM, 4 h) inhibits L3.6pl cell migration[2].
AZM475271 (1-10 μM, 4 h) demonstrates strong dose-dependent inhibition of Src tyrosine kinase activity in the L3.6pl cell line[2].
AZM475271 effectively blocks TGF-β1-induced chemokinesis of Panc-1 cells and inhibits the high chemokinetic activity of Panc-1 cells with ectopic expression of a constitutively active ALK5T204D mutant. [3].
AZM475271 (10-100 µM, 24-72 h) inhibits SFK in prostate tissues and WPMY-1 cells, reduces α1-adrenergic and neurogenic contraction of prostate strips[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[2]

Cell Line: L3.6pl human pancreatic cancer cells
Concentration: 1, 5, 10, 15, 20 μM
Incubation Time: 48 h
Result: Showed no anti-proliferative effect on L3.6pl cells in vitro, although a rapid decrease in cell proliferation was detected at high concentrations (>20μM).
Microscopic investigation indicated the rapid inhibition of cell proliferation was caused by reduced cell numbers due to therapy-induced cell death.

Apoptosis Analysis[2]

Cell Line: L3.6pl human pancreatic cancer cells
Concentration: 5 μM
Incubation Time: 12 h
Result: Resulting in apoptosis in 12.6%, 11.0%, and 52.2% of the tumor cells in used alone group, Gemcitabine group and combination group, respectively.

Cell Migration Assay [2]

Cell Line: L3.6pl human pancreatic cancer cells
Concentration: 0.1, 1, 5 μM
Incubation Time: 4 h
Result: Produced significant inhibition of L3.6pl tumor cell migration at 1 and 5μM.

Western Blot Analysis[2]

Cell Line: L3.6pl human pancreatic cancer cells
Concentration: 1, 2.5, 5, 10 μM
Incubation Time: 4 h
Result: Demonstrated strong dose-dependent inhibition of Src tyrosine kinase activity.
Maximum reduction of Src kinase activity was observed with ≥ 5 μM (4.76-fold reduction).
In Vivo

AZM475271(50 mg/kg; p.o.; once daily for 32 days) reduces tumor volume and the effect can be enhanced by combination with Gemcitabine (100 mg/kg; i.p.; twice weekly for 32 days) in athymic nude mice injected with L3.6pl cells[2].
AZM475271 (50 mg/kg; p.o.; once) has biological effective plasma concentration with 24 hours in healthy nude mice [2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Healthy nude mice[2]
Dosage: 50 mg/kg
Administration: Oral gavage (p.o.); once
Result: The plasma concentration was 32.1 μM (14.206 ng/mL), 20 μM (8879 ng/mL), and 11.7 μM (5187 ng/mL) at 2, 6, and 24 hours after p.o..
Animal Model: Athymic nude mice (injected with 1 X 106 viable L3.6pl cells[2]
Dosage: 50 mg/kg
Administration: Oral gavage (p.o.); once daily for 32 days
Result: The median tumor volume was significantly less than that in control mice.
After combination therapy, primary pancreatic tumor volume was significantly less than that seen with Gemcitabine alone.
The incidence of liver metastasis was markedly reduced.
Did not significantly change animal weight when used alone, but reduced animal weight combined with Gemcitabine.
Has antiproliferative effect alone and in combination with Gemcitabine.
induce apoptosis in pancreatic carcinoma cells in vivo, maximum apoptotic effect was observed in the combination with Gemcitabine.
Reduced microvessel density (MVD) alone and no significant difference in combination with Gemcitabine.
Molecular Weight

442.94

Formula

C23H27ClN4O3

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 42 mg/mL (94.82 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2576 mL 11.2882 mL 22.5764 mL
5 mM 0.4515 mL 2.2576 mL 4.5153 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2576 mL 11.2882 mL 22.5764 mL 56.4411 mL
5 mM 0.4515 mL 2.2576 mL 4.5153 mL 11.2882 mL
10 mM 0.2258 mL 1.1288 mL 2.2576 mL 5.6441 mL
15 mM 0.1505 mL 0.7525 mL 1.5051 mL 3.7627 mL
20 mM 0.1129 mL 0.5644 mL 1.1288 mL 2.8221 mL
25 mM 0.0903 mL 0.4515 mL 0.9031 mL 2.2576 mL
30 mM 0.0753 mL 0.3763 mL 0.7525 mL 1.8814 mL
40 mM 0.0564 mL 0.2822 mL 0.5644 mL 1.4110 mL
50 mM 0.0452 mL 0.2258 mL 0.4515 mL 1.1288 mL
60 mM 0.0376 mL 0.1881 mL 0.3763 mL 0.9407 mL
80 mM 0.0282 mL 0.1411 mL 0.2822 mL 0.7055 mL
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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AZM475271
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