A Src kinase inhibitor
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KX2-391

Item No. 21429

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5-[4-[2-(4-morpholinyl)ethoxy]phenyl]-N-(phenylmethyl)-2-pyridineacetamide
CAS Number
897016-82-9
Synonyms
  • KX 01
  • Tirbanibulin
Molecular Formula
C26H29N3O3
Formula Weight
431.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMSO: 15 mg/mlDMSO:PBS (pH 7.2) (1:1): 0.5 mg/mlEthanol: 1 mg/ml
λmax
268 nm
SMILES
O=C(CC1=NC=C(C2=CC=C(OCCN3CCOCC3)C=C2)C=C1)NCC4=CC=CC=C4
InChi Code
InChI=1S/C26H29N3O3/c30-26(28-19-21-4-2-1-3-5-21)18-24-9-6-23(20-27-24)22-7-10-25(11-8-22)32-17-14-29-12-15-31-16-13-29/h1-11,20H,12-19H2,(H,28,30)
InChi Key
HUNGUWOZPQBXGX-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $60

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    10 mg

    $90

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    50 mg

    $357

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    100 mg

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    Product Description

    KX2-391 is an inhibitor of Src kinase (IC50 = ~20 nM).1 It is selective for Src over PDGFR, EGFR, JAK1, JAK2, Lck, and ZAP-70. KX2-391 induces cell cycle arrest at the G2/M phase and apoptosis in breast cancer cells expressing estrogen receptor α (ERα).2 It inhibits the growth of Huh7, PLC/PRF/5, Hep3B, and HepG2 cells (GI50s = 9, 13, 26, and 60 nM, respectively).3 KX2-391 (10 mg/kg) decreases spleen weight and the number of splenic leukemia cells in a mouse model of FLT3 bearing internal-tandem duplication and F691L mutant (FLT3-ITD-F691L) acute myeloid leukemia (AML).4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Naing, A., Cohen, R., Dy, G.K., et al. A phase I trial of KX2-391, a novel non-ATP competitive substrate-pocket- directed SRC inhibitor, in patients with advanced malignancies. Invest. New Drugs 31(4), 967-973 (2013).

    2. Anbalagan, M., Carrier, L., Glodowski, S., et al. KX-01, a novel Src kinase inhibitor directed toward the peptide substrate site, synergizes with tamoxifen in estrogen receptor α positive breast cancer. Breast Cancer Res. Treat. 132(2), 391-409 (2012).

    3. Lau, G.M., Lau, G.M., Yu, G.-L., et al. Expression of Src and FAK in hepatocellular carcinoma and the effect of Src inhibitors on hepatocellular carcinoma in vitro. Dig. Dis. Sci. 54(7), 1465-1474 (2009).

    4. Wang, P., Xiao, X., Zhang, Y., et al. A dual inhibitor overcomes drug-resistant FLT3-ITD acute myeloid leukemia. J. Hematol. Oncol. 14(1), 105 (2021).