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CX-4945 (Silmitasertib)

Potent, selective, and ATP-competitive CK2 inhibitor

CX-4945 (Silmitasertib)

Catalog No. A8330
Size Price Stock Qty
Evaluation Sample $28.00  All Inclusive In stock
5mg $150.00 In stock
10mg $282.00 In stock
50mg $1,056.00 In stock

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Sample solution is provided at 25 µL, 10mM.

Quality Control

Quality Control & MSDS

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Chemical structure

CX-4945 (Silmitasertib)

Related Biological Data

CX-4945 (Silmitasertib)

Related Biological Data

CX-4945 (Silmitasertib)

Biological Activity

Description CX-4945 (Silmitasertib) is a potent and selective inhibitor of CK2 (casein kinase 2) with IC50 of 1 nM.
Targets CK2α CK2α'        
IC50 1 nM 1 nM        

Protocol

Cell experiment [1]:

Cell lines

Jurkat cells

Preparation method

This product is soluble in DMSO mostly at 45 mM. It is also soluble in water with no more than 1 mM.

Reacting condition

4d; IC50=0.1 μM

Applications

CK2 inhibition was confirmed by measuring the phosphorylation level of the CK2 specific phosphorylation site on Akt (S129). CX-4945 induced dephosphorylation of Akt (S129) and a rapid dephosphorylation of the Akt substrate p21 (T145). Apoptosis was induced by CX-4945. CX-4945 was also found to potently inhibit endogenous intracellular CK2 activity with an IC50 of 0.1 μM in Jurkat cells.

Animal experiment [1]:

Animal models

Athymic mice

Dosage form

75 mg/kg; bid; oral taken

Application

CX-4945 was tested for in vivo efficacy in established human prostate PC3 xenograft model in athymic mice. Mice bearing subcutaneous PC3 tumors were treated with CX-4945 (25 mg/kg, 50 mg/kg, and 75 mg/kg, p.o, bid). CX-4945 demonstrated tumor growth inhibition (TGI = 19%, 40%, and 86%, respectively) compared to vehicle treated control, and a dose responsive efficacy was observed. Last, CX-4945 was well tolerated in mice as assessed by minimal changes in body weight during the course of treatment compared to vehicle control.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

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]. Journal of medicinal chemistry, 2010, 54(2): 635-654.

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Chemical Properties

Cas No. 1009820-21-6 SDF Download SDF
Synonyms CX 4945;CX4945
Chemical Name 5-(3-chloroanilino)benzo[c][2,6]naphthyridine-8-carboxylic acid
Canonical SMILES C1=CC(=CC(=C1)Cl)NC2=C3C=CN=CC3=C4C=CC(=CC4=N2)C(=O)O
Formula C19H12ClN3O2 M.Wt 349.77
Solubility Soluble in DMSO Storage Store at -20°C
Shipping Condition: Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

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Background

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.