PeptideDB

RK-20448 479501-40-1

RK-20448 479501-40-1

CAS No.: 479501-40-1

RK-20448 is an ATP-competitive inhibitor of Lck, Src, KDR/VEGF2R and Tie-2 with IC50 values of 0.24, 1.19, 10.74 and 5.8
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RK-20448 is an ATP-competitive inhibitor of Lck, Src, KDR/VEGF2R and Tie-2 with IC50 values of 0.24, 1.19, 10.74 and 5.85 µM, respectively. RK-20448 also inhibits BLK, Csk, Fyn and Lyn with IC50 values of 0.37, 4.27, 2.03 and 0.43 µM, respectively. RK-20448 is the cis isomer of A-419259.

Physicochemical Properties


Molecular Formula C29H34N6O
Molecular Weight 482.62
CAS # 479501-40-1
Appearance White to off-white solid powder
SMILES

CN1CCN(C2CCC(N3C4=NC=NC(N)=C4C(C4=CC=C(OC5=CC=CC=C5)C=C4)=C3)CC2)CC1

Storage

Powder-20°C 3 years

4°C 2 years

In solvent -80°C 6 months

-20°C 1 month

Shipping Condition Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity


Targets Lck 0.24 μM (IC50); Blk 0.37 μM (IC50); Fyn 2.03 μM (IC50); Tie2 5.85 μM (IC50); VEGFR2 10.74 μM (IC50)
References

[1]. A pyrrolo-pyrimidine derivative targets human primary AML stem cells in vivo. Sci Transl Med. 2013 Apr 17;5(181):181ra52.

[2]. Hematopoietic cell kinase as a nexus for drug repurposing: implications for cancer and HIV therapy. J Biomol Struct Dyn. 2024 Mar 26:1-11.


Solubility Data


Solubility (In Vitro) DMSO : ~25 mg/mL (~51.80 mM; with ultrasonication (<60°C))
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.0720 mL 10.3601 mL 20.7202 mL
5 mM 0.4144 mL 2.0720 mL 4.1440 mL
10 mM 0.2072 mL 1.0360 mL 2.0720 mL
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.