1009820-21-6 Usage
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.
Check Digit Verification of cas no
The CAS Registry Mumber 1009820-21-6 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,0,0,9,8,2 and 0 respectively; the second part has 2 digits, 2 and 1 respectively.
Calculate Digit Verification of CAS Registry Number 1009820-21:
(9*1)+(8*0)+(7*0)+(6*9)+(5*8)+(4*2)+(3*0)+(2*2)+(1*1)=116
116 % 10 = 6
So 1009820-21-6 is a valid CAS Registry Number.
1009820-21-6Relevant articles and documents
Novel CK2-Specific Pt(II) Compound Reverses Cisplatin-Induced Resistance by Inhibiting Cancer Cell Stemness and Suppressing DNA Damage Repair in Non-small Cell Lung Cancer Treatments
Wang, Yuanjiang,Wang, Xinyi,Xu, Gang,Gou, Shaohua
, p. 4163 - 4178 (2021/05/04)
Cancer stem cells (CSCs) have a pivotal impact in drug resistance, tumor metastasis, and progression of various cancer entities, including in non-small cell lung cancer (NSCLC). A CK2 inhibitor HY1 was found to show potent CSC inhibitory effects in A549 cells. By taking advantage of inherent CK2 specificity and CSC inhibition of HY1, a Pt(II) agent (HY1-Pt) was developed by conjugation of HY1 with an active Pt(II) unit to reverse cisplatin-induced resistance in A549/cDDP cell treatment. In vitro biological studies indicated that HY1-Pt can target CK2, suppress DNA damage repair, reinforce cellular accumulation of platinum, and reverse resistance apart from effectively inhibiting CSCs through Wnt/β-catenin signal pathway in A549/cDDP cells. Significantly, HY1-Pt presented an acceptable pharmacokinetic behavior and exhibited higher tumor growth inhibitory efficacy than cisplatin either in A549 or A549/cDDP xenograft models with low toxicity. Overall, HY1-Pt is a promising drug candidate for NSCLC treatment.
PROTEIN KINASE MODULATORS
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Page/Page column 26, (2009/10/01)
The invention relates in part to molecules having certain biological activities that include, but are not limited to, inhibiting cell proliferation, modulating protein kinase activity and modulating polymerase activity. Molecules of the invention can modulate Pim kinase activity and/or FMS-like tyrosine kinase (Flt) activity. The invention also relates in part to methods for using such molecules.
