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A 419259 trihydrochloride

Catalog No. TQ0132   CAS 1435934-25-0
Synonyms: RK 20449 trihydrochloride

A 419259 trihydrochloride (RK 20449 trihydrochloride) is an Src family kinases inhibitor (IC50s: 9 nM, 3 nM and 3 nM for Src, Lck and Lyn).

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A 419259 trihydrochloride Chemical Structure
A 419259 trihydrochloride, CAS 1435934-25-0
Pack Size Availability Price/USD Quantity
1 mg In stock $ 48.00
2 mg In stock $ 68.00
5 mg In stock $ 109.00
10 mg In stock $ 179.00
25 mg In stock $ 335.00
50 mg In stock $ 587.00
100 mg In stock $ 839.00
500 mg In stock $ 1,670.00
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Purity: 100%
Purity: 99.47%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description A 419259 trihydrochloride (RK 20449 trihydrochloride) is an Src family kinases inhibitor (IC50s: 9 nM, 3 nM and 3 nM for Src, Lck and Lyn).
Targets&IC50 Lyn:3 nM, Lck:3 nM, Src:9 nM
In vitro A-419259 inhibits K-562 cells (IC50: 0.1~0.3 μM), and Meg-01 proliferation (IC50: ~0.1 μM). A-419259 also potently induces apoptosis in K-562 cells beginning at 0.1 μM and increasing in a dose-dependent manner. PP2 inhibits Src kinase autophosphorylation in both Ph+ cell lines (K-562 and Meg-01) with an IC50 between 3 and 10 μM, while A-419259 blocks kinase activation between 0.1 and 0.3 μM. A-419259 strongly inhibits DAGM/Bcr-Abl cell proliferation in the absence of IL-3 (IC50: 0.1~0.3 μM) [1]. A-419259 inhibits overall SFK activity in K562 and other CML cell lines with an IC50 value of 0.1-0.3 μM [2].
Kinase Assay In vitro kinase assays are performed on His(6)-tagged Lck (residues 62-509) and full-length c-Abl purified from Sf-9 cells, and commercial sources of Lyn, Src and PKC. Lck, Lyn, Src and Abl activities are measured with an ELISA-based assay. Flat bottom 96-well ELISA plates are incubated with a 200 μg/mL solution of Poly(Glu, Tyr) 4 : 1 substrate in phosphate-buffered saline (PBS) for 1 h at 37°C and then washed with PBS containing 0.1% Tween-20 (PBS-T). Inhibitor dilutions are added to the washed plates already containing the appropriate enzyme in kinase assay buffer (250 mM Mopso, pH 6.75, 10 mM MgCl2, 2 mM MnCl2, 2.5 mM DTT, 0.02% BSA, 2 mM Na3VO4, 5% DMSO, 5 μM ATP). After incubation at room temperature for 20 min, plates are washed three times with PBS-T and plate-bound phosphotyrosine is detected with an anti-phosphotyrosine-HRP antibody conjugate and subsequent color development with K-Blue reagents [1].
Cell Research K-562 cells are grown in RPMI 1640 supplemented with 10% fetal calf serum (FCS), and 50 g/mL Gentamycin. Meg-01 cells are cultured in Vitacell modified RPMI 1640 (ATCC), supplemented with 10% FCS and 50 μg/mL Gentamycin. The human GM-CSF-dependent myeloid leukemia cell line TF-1 is grown in RPMI 1640 supplemented with 10% FCS, 50 μg/mL Gentamycin, and 1 ng/mL of recombinant human GM-CSF. DAGM murine myeloid leukemia cells are cultured in RPMI 1640 supplemented with 10% FCS, 50 μg/mL Gentamycin, and 0.5 ng/mL recombinant IL-3. Concentrated stock solutions of PP2 (5 mM) and A-419259 (2 mM) are prepared in DMSO and stored at -20°C. Cellular proliferation is measured using the Live/Dead growth assay. This assay employs calcein-AM, a fluorogenic esterase substrate that is taken up by viable cells and hydrolyzed intracellularly, releasing a green fluorescent product. Briefly, 10^4 cells are plated per well in 96-well plates for each day of a 4-day time course. Various concentrations of PP2, A-419259 or vehicle control are added to the wells (five wells per concentration per day) and the plates are incubated at 37°C. At each time point, one plate is centrifuged at 1500 g for 10 min to pellet the cells. Cells are washed with PBS, and calcein-AM is added to each well to a final concentration of 1 μM. Plates are incubated in the dark at room temperature for 1 h. The plates are then read at 485/530 nm (excitation/emission) using a fluorescent plate reader and data are analyzed with SoftMax Pro software [1].
Synonyms RK 20449 trihydrochloride
Molecular Weight 592
Formula C29H37Cl3N6O
CAS No. 1435934-25-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: ≥53 mg/mL (89.53 mM)

TargetMolReferences and Literature

1. Wilson MB, et al. Selective pyrrolo-pyrimidine inhibitors reveal a necessary role for Src family kinases in Bcr-Abl signal transduction and oncogenesis. Oncogene. 2002 Nov 21;21(53):8075-88. 2. Pene-Dumitrescu T, et al. An inhibitor-resistant mutant of Hck protects CML cells against the antiproliferative and apoptotic effects of the broad-spectrum Src family kinase inhibitor A-419259.Oncogene. 2008 Nov 27;27(56):7055-69.

Related compound libraries

This product is contained In the following compound libraries:
Tyrosine Kinase Inhibitor Library Bioactive Compound Library Angiogenesis related Compound Library Inhibitor Library Anti-Cancer Metabolism Compound Library Bioactive Compounds Library Max

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Keywords

A 419259 trihydrochloride 1435934-25-0 Angiogenesis Tyrosine Kinase/Adaptors Src RK20449 Trihydrochloride A 419259 RK 20449 RK-20449 A-419259 Trihydrochloride RK20449 A419259 RK-20449 Trihydrochloride Inhibitor RK 20449 Trihydrochloride inhibit RK 20449 trihydrochloride A-419259 A 419259 Trihydrochloride A419259 Trihydrochloride inhibitor

 

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