A potent, orally bioavailable CK2 inhibitor
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CX-4945

Item No. 16779

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5-[(3-chlorophenyl)amino]-benzo[c]-2,6-naphthyridine-8-carboxylic acid
CAS Number
1009820-21-6
Synonyms
  • Silmitasertib
Molecular Formula
C19H12ClN3O2
Formula Weight
349.8
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMF:PBS(pH 7.2)(1:1): 0.5 mg/mlDMSO: 15 mg/ml
λmax
209, 240, 260, 360 nm
SMILES
OC(C1=CC2=NC(NC3=CC(Cl)=CC=C3)=C(C=CN=C4)C4=C2C=C1)=O
InChi Code
InChI=1S/C19H12ClN3O2/c20-12-2-1-3-13(9-12)22-18-15-6-7-21-10-16(15)14-5-4-11(19(24)25)8-17(14)23-18/h1-10H,(H,22,23)(H,24,25)
InChi Key
MUOKSQABCJCOPU-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

    $69

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    1 mg

    $120

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    5 mg

    $227

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    10 mg

    $381

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    Product Description

    CX-4945 is a potent, orally bioavailable inhibitor of casein kinase 2 (CK2; Ki = 0.38 nM) that competes with ATP by filling the small ATP binding site on the catalytic CK2α subunit, conferring selectivity.1,2,3 It inhibits proliferation in a panel of cancer cell lines that overexpress CK2 and prevents tumor growth of breast and pancreatic cancer cell xenografts in mice.3 CX-4945 blocks survival and induces apoptosis in cancer stem cells and is effective against glioblastomas and acute myeloid leukemia cells.4,5 CX-4945 also inhibits Cdc2-like kinases (Clk; IC50s = 82.3, 3.8, and 90 nM for Clk1, Clk2, and Clk3, respectively), interfering with alternative splicing.6

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Pierre, F., Chua, P.C., O'Brien, S.E., et al. Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. J. Med. Chem. 54(2), 635-654 (2011).

    2. Ferguson, A.D., Sheth, P.R., Basso, A.D., et al. Structural basis of CX-4945 binding to human protein kinase CK2. FEBS Lett. 585(1), 104-110 (2011).

    3. Siddiqui-Jain, A., Drygin, D., Streiner, N., et al. CX-4945, an orally bioavailable selective inhibitor of protein kinase CK2, inhibits prosurvival and angiogenic signaling and exhibits antitumor efficacy. Cancer Res. 70(24), 10288-10298 (2010).

    4. Agarwal, M., Nitta, R.T., and Li, G. Casein Kinase 2: A novel player in glioblastoma therapy and cancer stem cells. J. Mol. Genet. Med. 8(1), 1000094 (2013).

    5. Quotti Tubi, L., Gurrieri, C., Brancalion, A., et al. Inhibition of protein kinase CK2 with the clinical-grade small ATP-competitive compound CX-4945 or by RNA interference unveils its role in acute myeloid leukemia cell survival, p53-dependent apoptosis and daunorubicin-induced cytotoxicity. J. Hematol. Oncol. 6, 78 (2013).

    6. Kim, H., Choi, K., Kang, H., et al. Identification of a novel function of CX-4945 as a splicing regulator. PLoS One 9(4), e94978 (2014).