CX-4945 Chemical Properties

Boiling point:

568.5±50.0 °C(Predicted)

Density 

1.490

storage temp. 

Store at -20°C

solubility 

≥103.5 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH

form 

Orange powder.

pka

2.96±0.30(Predicted)

color 

Yellow to orange

Safety Information

HS Code 

29339900

CX-4945 Usage And Synthesis

Uses

CX-4945 is a protein kinase CK2 inhibitor resulting in cancer cell death and prevention of proliferation. Anti-leukemia agent.

Biological Activity

cx-4945 (silmitasertib) is a potent and selective casein kinase 2 (ck2) inhibitor with ic50 value of 1 nm. it is atp-competitive and can be taken orally [1].cx-4945 has been reported to have antiproliferative activity against a wide range of tumor cell lines. it is suggested that cx-4945 suppresses the ck2 regulated pi3k/akt signaling pathway by inhibiting akt phosphorylation at serine 129, but not by activating pten. additionally, cells treated with cx-4945 had a reduction of p21 phophorylation and an up-regulations of total p21 and p27. cx-4945 has been shown to induce cell-cycle arrest at g2/m phase in breast cancer cell line bt-474. it also causes cell-cycle arrest at g1 phase the breast cancer cell line bxpc-3) [1].in cx-4945 and bxpc-3 derived mouse xenograft model, cx-4945 induced a reduction of phos-p21 expression along with anti-carcinoma effects [1]

References

[1] siddiqui-jain a1, drygin d, streiner n, chua p, pierre f, o'brien se, bliesath j, omori m, huser n, ho c, proffitt c, schwaebe mk, ryckman dm, rice wg,anderes k. 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.

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