Art. -Nr.: HY-13561

AZM475271

(Synonyms: M475271)

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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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Reinheit: 99.89%
CAS. Nr.: 476159-98-5
Formel: C₂₃H₂₇ClN₄O₃
Molecular Weight:442.94

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

AZM475271 Chemical Structure

CAS. Nr.: 476159-98-5

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

Lck

0.03 μM (IC₅₀)

Alle Src Isoform-spezifische Produkte anzeigen :

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]
NIH3T3	IC₅₀	0.01 μM Compound: 35, M475271	Inhibition of human c-Src in NIH3T3 cells Inhibition of human c-Src in NIH3T3 cells	[PMID: 17064066]
NIH3T3	IC₅₀	0.53 μM Compound: 35, M475271	Antiproliferative activity against mouse NIH3T3 cell line transfected with c-SRC Antiproliferative activity against mouse NIH3T3 cell line transfected with c-SRC	[PMID: 17064066]
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 = 0.48 μM) 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 (> 20 μM).
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.

Chemical Information

CAS. Nr. 476159-98-5
Appearance Solid
Molecular Weight 442.94
Formel C₂₃H₂₇ClN₄O₃
Color White to off-white
SMILES

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

M475271
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Lösungsmittel & Löslichkeit

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2576 mL

11.2882 mL

22.5764 mL

5 mM

0.4515 mL

2.2576 mL

4.5153 mL

10 mM

0.2258 mL

1.1288 mL

2.2576 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (285 KB)
SDS (479 KB)
- English - EN (479 KB)
- Français - FR (479 KB)
- Deutsch - DE (479 KB)
- Norwegian - NO (479 KB)
- Español - ES (479 KB)
- Swedish - SV (479 KB)
- Italian - IT (479 KB)
- Korean - KR (479 KB)
- Portuguese - PT (479 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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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AZM475271

Apoptosis Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Reprogramming Compound Library

Orally Active Compound Library

Anti-Pancreatic Cancer Compound Library

Angiogenesis-Related Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Pain-Related Compound Library

Membrane Protein-targeted Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Alle Src Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

AZM475271

Apoptosis Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Reprogramming Compound Library

Orally Active Compound Library

Anti-Pancreatic Cancer Compound Library

Angiogenesis-Related Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Pain-Related Compound Library

Membrane Protein-targeted Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Alle Src Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

AZM475271 Related Classifications

HY-13561 Related Classifications