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。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1009820-21-6
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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. |
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.
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. |
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Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
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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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
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