AZM475271 (Synonyms: M475271)

Cat. No.: HY-13561 Purity: 99.85%: FAQs
Data Sheet SDS COA Handling Instructions

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AZM475271 is a potent and selective Src kinase inhibitor with IC50 of 5 nM; no inhibitory activity on Flt3, KDR, Tie-2.

For research use only. We do not sell to patients.

AZM475271 Chemical Structure

CAS No. : 476159-98-5

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 99	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 99	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 90	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 140	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 490	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 790	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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Biological Activity
Purity & Documentation
References
Customer Review

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 inhibitor in 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].

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]

Molecular Weight

442.94

Formula

C₂₃H₂₇ClN₄O₃

CAS No.

476159-98-5

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
10 mM	0.2258 mL	1.1288 mL	2.2576 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.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.85%

Select Batch:

Data Sheet (276 KB) SDS (252 KB)

COA (254 KB) LCMS (93 KB)

Handling Instructions (2659 KB)

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. [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]

Complete Stock Solution Preparation Table

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

AZM475271 Related Classifications

Help & FAQs

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.

Keywords:

AZM475271476159-98-5M475271AZM 475271AZM-475271M 475271M-475271SrcInhibitorinhibitorinhibit

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AZM475271 (Synonyms: M475271)

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AZM475271 Related Antibodies

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Biological Activity

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Customer Review

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Complete Stock Solution Preparation Table

AZM475271 Related Classifications

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