A-419259

SKU: orb1710519

Description

A-419259 (RK-20449) is a potent and selective small molecule inhibitor of Src-family kinases (SFKs), such as Src, LCK, and Lyn, with IC50 values in the low nanomolar range (3-9 nM). This apoptosis-inducing compound is a valuable research tool for studying SFK signaling in oncology and immunology, with applications in both in vitro cellular assays and in vivo model systems.

Research Area

Cardiovascular Research, Cell Biology, Signal Transduction

Key Properties

• CAS Number: 364042-47-7
• MW: 482.62
• Purity: >99.99% (May vary between batches)
• Formula: C₂₉H₃₄N₆O
• SMILES: NC1=C2C(=CN(C2=NC=N1)[C@H]3CC[C@@H](CC3)N4CCN(C)CC4)C5=CC=C(OC6=CC=CC=C6)C=C5
• Target: Src,Apoptosis
• Solubility: H2O:< 0.1 mg/mL (insoluble);DMSO:10 mg/mL (20.72 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.07 mM)

Bioactivity

• Target IC50:
  Lck:<3 nM|Lyn:<3 nM
• In Vitro:
  A-419259 selectively inhibits Src kinases (IC₅₀ < 0.003 μM), blocks proliferation, and induces apoptosis in Bcr-Abl⁺ leukemia cells by suppressing Stat5 and Erk signaling, with minimal effect on normal cells.
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• 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 phosphate buffered saline (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 analysed with SoftMax Pro software .
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Src, RK20449, RK-20449, RK 20449, A 419259, Abl, A-419259, A419259, Lck, Lyn

Compound Identifiers

PubChem CID

6539952