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

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

AZM475271 Chemical Structure

CAS No. : 476159-98-5

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
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10 mM * 1 mL in DMSO USD 99 In-stock
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10 mg USD 140 In-stock
50 mg USD 490 In-stock
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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].

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

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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
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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HY-13561
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