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CX-4945 (Silmitasertib) (Synonyms: CX 4945;CX4945)

カタログ番号GC13037

CX-4945(シルミタセルチブ)は、経口投与可能で、高度に選択的かつ強力なCK2阻害剤であり、CK2αおよびCK2α'に対するIC50値が1 nMです。

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CX-4945 (Silmitasertib) 化学構造

Cas No.: 1009820-21-6

サイズ 価格 在庫数 個数
10mM (in 1mL DMSO)
$63.00
在庫あり
5mg
$57.00
在庫あり
10mg
$97.00
在庫あり
50mg
$243.00
在庫あり

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Cell experiment [1]:

Cell lines

Jurkat cells

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

Reaction Conditions

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

Applications

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.

Background

CX-4945(シルミタセルチブ)は、IC50値が1nMの強力で選択的なカゼインキナーゼ2(CK2)阻害剤です。ATP競合性を持ち、経口摂取可能です[1]。

CX-4945は、広範囲の腫瘍細胞株に対する抗増殖活性を持つことが報告されています。CX-4945は、Aktのセリン129でのリン酸化を抑制することによって、CK2調節PI3K/Aktシグナル伝達経路を抑制すると示唆されていますが、PTENを活性化させるわけではありません。さらに、CX-4945で処理された細胞はp21のリン酸化が減少し、全体的なp21およびp27の上昇が観察されました。CX-4945は乳癌細胞株BT-474でG2/M期に細胞周期停止を誘導することも示されています。また、乳癌細胞株BxPC-3ではG1期に細胞周期停止を引き起こします[1]。

CX-4945は、CX-4945およびBxPC-3由来のマウス異種移植モデルにおいて、phos-p21発現の低下と抗癌効果を誘導した[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.

Chemical Properties

Cas No. 1009820-21-6 SDF
同義語 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
溶解度 ≥ 8.74mg/mL in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.859 mL 14.2951 mL 28.5902 mL
5 mM 0.5718 mL 2.859 mL 5.718 mL
10 mM 0.2859 mL 1.4295 mL 2.859 mL
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Review for CX-4945 (Silmitasertib)

Average Rating: 5 ★★★★★ (Based on Reviews and 30 reference(s) in Google Scholar.)

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