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1mg |
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2mg |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Purity: ≥98%
Silmitasertib (CX-4945; CX4945; CX 4945) is a potent, selective, orally bioavailable small-molecule inhibitor of CK2 (casein kinase 2) with potential anticancer activity. It inhibits CK2 with an IC50 of 1 nM in a cell-free assay, and shows less potency againt Flt3, Pim1 and CDK1 (inactive in cell-based assay). CX-4945 selectively binds to and inhibits the enzyme casein kinase II (CK2), which may lead to an inhibition of cellular proliferation. CK2 is a protein kinase overexpressed in a variety of cancer cell types and is correlated with malignant transformation, tumor growth and survival.
ln Vitro |
Cell-cycle arrest and selective apoptosis in cancer cells as compared to normal cells are caused by silmitasertib (CX-4945), which also attenuates PI3K/Akt signaling. The antiproliferative activity of silmitasertib (CX-4945) is correlated with the expression levels of the CK2α catalytic subunit. In order to buffer the PS-341-mediated proteotoxic stress in the ER lumen, leukemic cells cannot engage a functional UPR. Silmitasertib (CX-4945) with PS-341 therapy reduces pro-survival ER chaperon BIP/Grp78 expression[2]. Activation of the CK2-mediated PI3K/Akt/mTOR signaling pathways is suppressed and cytotoxicity and apoptosis are induced in hematological malignancies by silmitasertib (CX-4945) via downregulating CK2 expression[3].
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ln Vivo |
In murine xenograft models, silmitasertib (CX-4945) (25 or 75 mg/kg, po) is well tolerated and has shown strong anticancer activity with simultaneous decreases in the mechanism-based biomarker phospho-p21 (T145)[1].
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Animal Protocol |
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References |
[1]. Siddiqui-Jain A, et al. CX-4945, an orally bioavailable selective inhibitor of protein kinase CK2, inhibits prosurvival and angiogenic signaling and exhibits antitumor efficacy. Cancer Res. 2010 Dec 15;70(24):10288-98.
[2]. Buontempo F, et al. Synergistic cytotoxic effects of PS-341 and CK2 inhibitor CX-4945 in acute lymphoblastic leukemia: turning off the prosurvival ER chaperone BIP/Grp78 and turning on the pro-apoptotic NF-κB. Oncotarget. 2016 Jan 12;7(2):1323-40. [3]. Chon HJ, et al. The casein kinase 2 inhibitor, CX-4945, as an anti-cancer drug in treatment of human hematological malignancies. Front Pharmacol. 2015 Mar 31;6:70 |
Molecular Formula |
C19H12CLN3O2
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Molecular Weight |
349.77
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CAS # |
1009820-21-6
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Related CAS # |
Silmitasertib sodium salt;1309357-15-0
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SMILES |
O=C(C1=CC=C2C(N=C(NC3=CC=CC(Cl)=C3)C4=C2C=NC=C4)=C1)O
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Synonyms |
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.8590 mL | 14.2951 mL | 28.5902 mL | |
5 mM | 0.5718 mL | 2.8590 mL | 5.7180 mL | |
10 mM | 0.2859 mL | 1.4295 mL | 2.8590 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.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.