An inhibitor of Src family kinases
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Alternative(s)
18168A-419259 (hydrochloride)
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A-419259

Item No. 25605

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
7-[trans-4-(4-methyl-1-piperazinyl)cyclohexyl]-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine
CAS Number
364042-47-7
Synonyms
  • RK-20449
Molecular Formula
C29H34N6O
Formula Weight
482.6
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: 10 mM
SMILES
NC1=C(C(C2=CC=C(OC3=CC=CC=C3)C=C2)=CN4[C@@H]5CC[C@@H](N6CCN(C)CC6)CC5)C4=NC=N1
InChi Code
InChI=1S/C29H34N6O/c1-33-15-17-34(18-16-33)22-9-11-23(12-10-22)35-19-26(27-28(30)31-20-32-29(27)35)21-7-13-25(14-8-21)36-24-5-3-2-4-6-24/h2-8,13-14,19-20,22-23H,9-12,15-18H2,1H3,(H2,30,31,32)/t22-,23-
InChi Key
FDVSOQRNTAPCHB-YHBQERECSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Product Description

    A-419259 is an inhibitor of Src family kinases, including Src, LCK, Lyn, and Hck (IC50s = 9, <3, <3, and 11.26 nM, respectively).1,2 It is selective for these kinases over c-Abl (IC50 = 3,000 nM) and PKC (IC50 = >33 μM).1 A-419259 inhibits growth of Philadelphia chromosome-positive (Ph+) K-562 and Meg-01 myeloid leukemia cells (IC50s = 0.1-0.3 and 0.1 μM, respectively), but not Ph- TF-1 and HEL cells. It induces apoptosis in K-562 cells in a concentration-dependent manner. A-419259 (300 nM) inhibits differentiation of murine embryonic stem cells while maintaining pluripotency.3 It reduces the total number of acute myeloid leukemia (AML) cells, as well as AML stem cells, in the bone marrow and spleen in mouse patient-derived xenograft (PDX) models of AML when administered at a dose of 30 mg/kg twice daily.4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Wilson, M.B., Schreiner, S.J., Choi, H.J., et al. Selective pyrrolo-pyrimidine inhibitors reveal a necessary role for Src family kinases in Bcr-Abl signal transduction and oncogenesis. Oncogene 21(53), 8075-8088 (2002).

    2. Pene-Dumitrescu, T., Peterson, L.F., Donato, N.J., 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 27(56), 7055-7069 (2008).

    3. Meyn, M.A., III, Schreiner, S.J., Dumitresco, T.P., et al. SRC family kinase activity is required for murine embryonic stem cell growth and differentiation. Mol. Pharmacol. 68(5), 1320-1330 (2005).

    4. Saito, Y., Yuki, H., Kuratani, M., et al. A pyrrolo-pyrimidine derivative targets human primary AML stem cells in vivo. Sci. Transl. Med. 5(181):181ra52, (2013).