| Identification | Back Directory | [Name]
5-[(3-chlorophenyl)amino]-Benzo[c]-2,6-naphthyridine-8-carboxylic acid | [CAS]
1009820-21-6 | [Synonyms]
CX-4945
CS-1985
Silmitasertib
CX-4945, >=98%
CX-4945, CX4945
mitasertib (CX-4945)
Silmitasertib(CX-4945)
CX-4945 Silmitasertib
SILMITASERTIB; CX 4945; CX4945
CX-4945 (SILMITASERTIB);CX 4945; CX4945
CX4945 CX-4945; CX 4945; SILMITASERTIB.
5-[(3-chlorophenyl)amino]-Benzo[c]-2,6-naphthyridine-8-carboxylic acid
Silmitasertib, 98%, a potent and selective ATP-competitive CK2 inhibitor
Benzo[c]-2,6-naphthyridine-8-carboxylic acid, 5-[(3-chlorophenyl)amino]-
5-[(3-Chlorophenyl)amino]benzo[c]-2,6-naphthyridine-8-carboxylic acid CX-4945 (Silmitasertib) | [Molecular Formula]
C19H12ClN3O2 | [MDL Number]
MFCD13184796 | [MOL File]
1009820-21-6.mol | [Molecular Weight]
349.77 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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] | [in vivo]
Silmitasertib (CX-4945) (25 or 75 mg/kg, p.o.) is well tolerated and demonstrated robust antitumor activity with concomitant reductions of the mechanism-based biomarker phospho-p21 (T145) in murine xenograft models[1]. | [IC 50]
CK2α: 1 nM (IC50); CK2α': 1 nM (IC50) | [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. |
|
|