CX-4945 (Silmitasertib)

Catalog No. A11060

CX-4945 (Silmitasertib)是有效的，选择性CK2(casein kinase 2)抑制剂，可抑制人脐静脉内皮细胞迁移，管形成，并阻止癌细胞中CK2依赖性缺氧诱导的因子1α（HIF-1α）转录。

Product Citations

Xixi Zhao, .et al. Phosphorylation and Stabilization of PD-L1 by CK2 Suppresses Dendritic Cell Function, Cancer Res, 2022, Jun 6;82(11):2185-2195 PMID: 35385574
Janeen H. Trembley, .et al. CX-4945 and siRNA-Mediated Knockdown of CK2 Improves Cisplatin Response in HPV(+) and HPV(-) HNSCC Cell Lines, Biomedicines, 2021, May; 9(5): 571 PMID: 34070147
Tianzhi Huang, .et al. PRMT6 methylation of RCC1 regulates mitosis, tumorigenicity, and radiation response of glioblastoma stem cells, Mol Cell, 2021, Mar 18;81(6):1276-1291 PMID: 33539787
M Afzal, .et al. Protein kinase CK2 impact on intracellular calcium homeostasis in prostate cancer, Molecular and Cellular Biochemistry, 2020, 470, pages131-143
Zaman MS, .et al. Protein kinase CK2 is involved in zinc homeostasis in breast and prostate cancer cells, Biometals, 2019, Oct 3 PMID: 31583500
Fukumoto Y, .et al. Human Rad17?C-terminal tail is phosphorylated by concerted action of CK1δ/ε and CK2 to promote interaction with the 9-1-1 complex, Biochem Biophys Res Commun, 2019, Sep 17;517(2):310-316 PMID: 31353086
Fukumoto Y, .et al. Casein kinase 2 promotes interaction between Rad17 and the 9-1-1 complex through constitutive phosphorylation of the C-terminal tail of human Rad17, Biochem Biophys Res Commun, 2018, Oct 2;504(2):380-386 PMID: 29902452
ST Ribeiro, .et al. Casein kinase 2 controls the survival of normal thymic and leukemic γδ T cells via promotion of AKT signaling, Leukemia, 2017, Jul; 31(7): 1603-1610 PMID: 27899804
Valentina Gandin, .et al. mTORC1 and CK2 coordinate ternary and eIF4F complex assembly, Nat Commun, 2016, 7: 11127 PMID: 27040916
Ampofo E, .et al. Protein Kinase CK2 Regulates Leukocyte-Endothelial Cell Interactions during Ischemia and Reperfusion in Striated Skin Muscle, Eur Surg Res, 2016, 57(1-2):111-24 PMID: 27287005
Emmanuel Ampofo, .et al. Role of protein kinase CK2 in the dynamic interaction of platelets, leukocytes and endothelial cells during thrombus formation., Thromb Res., 2015, Nov;136(5):996-1006 PMID: 26381437
Emmanuel Ampofo, .et al. Inhibition of protein kinase CK2 suppresses tumor necrosis factor (TNF)-α-induced leukocyte-endothelial cell interaction., Biochim Biophys Acta., 2015, Oct;1852(10 Pt A):2123-36 PMID: 26189586
A. Margarida Gomes, .et al. Adult B-cell acute lymphoblastic leukemia cells display decreased PTEN activity and constitutive hyperactivation of PI3K/Akt pathway despite high PTEN protein levels, Haematologica, 2014, 99(6): 1062-1068 PMID: 24561792

Technical details

Catalog Num	A11060
M. Wt	349.8
Formula	C19H12ClN3O2
Purity	>98%
Storage	at -20°C 3 years Powder
CAS No.	1009820-21-6
Synonyms	Silmitasertib, CX 4945, CX4945
SMILES	C1=CC(=CC(=C1)Cl)NC2=C3C=CN=CC3=C4C=CC(=CC4=N2)C(=O)O

Biological Activity

Targets

CK2 (Cell-free assay)
1 nM

Solubility *

In vitro (25°C)	DMSO	14 mg/mL (40.02 mM)
	Water	Insoluble
	Ethanol	Insoluble
In vivo	1% CMC Na	28 mg/mL
* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Preparing Stock Solutions

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.1 mM	28.59 mL	142.94 mL	285.88 mL
0.5 mM	5.72 mL	28.59 mL	57.18 mL
1 mM	2.86 mL	14.29 mL	28.59 mL
5 mM	0.57 mL	2.86 mL	5.72 mL

*The above data is based on the productmolecular weight 349.8 . Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.