CX-4945 CAS: 1009820-21-6
MF: C19H12ClN3O2
MW: 349.77

CX-4945 (CAS 1009820-21-6)

CX-4945 | CAS 1009820-21-6 is rated 5.0 out of 5 by 2.
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Alternate Names: CX-4945 is also known as Silmitasertib.
Application: CX-4945 is an ATP-competitive CK2 protein kinase inhibitor, able to suppress Akt signaling and inhibit HUVEC proliferation.
CAS Number: 1009820-21-6
Purity: ≥95%
Molecular Weight: 349.77
Molecular Formula: C19H12ClN3O2
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data (including water content).
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CX-4945 (Silmitasertib) is an ATP-competitive CK2 protein kinase inhibitor with a Ki and an IC50 of 0.38 and 1 nM for recombinant human CK2α, respectively. CX-4945 has broad-spectrum anti-proliferative activity in multiple cancer cell lines. The anti-proliferative activity of CX-4945 against cancer cells correlated with expression levels of the CK2α catalytic subunit. Attenuation of PI3K/Akt signaling by CX-4945 was evidenced by dephosphorylation of Akt on the CK2-specific S129 site and the canonical S473 and T308 regulatory sites. CX-4945 suppresses Akt signaling and inhibits proliferation of HUVEC Cells. CX-4945 causes cell-cycle arrest and selectively induced apoptosis in certain cancer cells. In models of angiogenesis, CX-4945 inhibited human umbilical vein endothelial cell migration, tube formation, and blocked CK2-dependent hypoxia-induced factor 1 alpha (HIF-1α) transcription in cancer cells. Collectively, CX-4945 inhibits pro-angiogenic CK2 signaling in vitro and in vivo.


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. Journal of Medicinal Chemistry 54(2), 635-654 (2011).
2. Ferguson, A.D., Sheth, P.R., Basso, A.D., et al.Structural basis of CX-4945 binding to human protein kinase CK2. FEBS Letters 585(1), 104-110 (2011).
3. Siddiqui-Jain, A., Drygin, D., Streiner, N., et al.CX-4945, an orally bioavailable selective inhibitor of protein kinase CK2, inhibits prosurvival and angiogenic signaling and exhibits antitumor efficacy. Cancer Research 70(24), 10288-10298 (2010).
4. Agarwal, M., Nitta, R.T., and Li, G.Casein Kinase 2: A novel player in glioblastoma therapy and cancer stem cells. J.Mol.Genet.Med. 8(1), 1-18 (2013).
5. Quotti Tubi, L., Gurrieri, C., Brancalion, A., et al.Inhibition of protein kinase CK2 with the clinical-grade small ATP-competitive compound CX-4945 or by RNA interference unveils its role in acute myeloid leukemia cell survival, p53-dependent apoptosis and daunorubicin-induced cytotoxicity. J.Hematol.Oncol. 6, 1-15 (2013).
6. Kim, H., Choi, K., Kang, H., et al.Identification of a novel function of CX-4945 as a splicing regulator. PLoS One 9(4), e94978 (2014).

Appearance :
Powder
Physical State :
Solid
Solubility :
Soluble in water (<1.2 mg/ml), DMSO (≥65 mg/ml), and ethanol (<1.2 mg/ml).
Storage :
Store at -20° C
Boiling Point :
~568.5° C at 760 mmHg (Predicted)
Density :
~1.5 g/cm3 (Predicted)
Refractive Index :
n20D 1.79 (Predicted)
IC50 :
Casein kinase IIα: IC50 = 1 nM (human); ZIP-kinase: IC50 = 17 nM (human); TBK1: IC50 = 35 nM (human); CLK3: IC50 = 41 nM (human); HIPK3: IC50 = 45 nM (human)
pK Values :
pKa: 2.96 (Predicted), pKb: 4.04 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
MDL Number :
MFCD13184796
SMILES :
C1=CC(=CC(=C1)Cl)NC2=C3C=CN=CC3=C4C=CC(=CC4=N2)C(=O)O

Download SDS (MSDS)

Certificate of Analysis

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CX-4945 (CAS 1009820-21-6)  Product Citations

See how others have used CX-4945 (CAS 1009820-21-6). Click on the entry to view the PubMed entry .

Citations 1 to 8 of 8 total

PMID: # 30600261  Pankow, S.|Bamberger, C.|Yates, JR.| et al. 2019. Sci Signal. 12:

PMID: # 30142881  Lertsuwan, J.|Lertsuwan, K.|Sawasdichai, A.|Tasnawijitwong, N.|Lee, KY.|Kitchen, P.|Afford, S.|Gaston, K.|Jayaraman, PS.|Satayavivad, J.| et al. 2018. Cancers (Basel). 10:

PMID: # 28223413  Viscarra, JA. et al. 2017. Sci Signal. 10:

PMID: # 27707883  de Bourayne, M.|Gallais, Y.|El Ali, Z.|Rousseau, P.|Damiens, MH.|Cochet, C.|Filhol, O.|Chollet-Martin, S.|Pallardy, M.|Kerdine-Römer, S.| et al. 2017. J. Leukoc. Biol. 101: 703-715.

PMID: # 28873435  Lustri, AM. et al. 2017. PLoS ONE. 12: e0183932.

PMID: # 27033073  Misticone, S. et al. 2016. Methods in molecular biology (Clifton, N.J.). 1388: 95-110.

PMID: # 24616922  FEBS J. 851-61.

PMID: # 32759324  J. Virol.

Citations 1 to 8 of 8 total

What is the appearance of the compound?

Asked by: two2igm05
Thank you for your question. CX-4945, sc-364475, is in orange powder form.
Answered by: Chemical Support 4
Date published: 2017-04-04
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Rated 5 out of 5 by from worked good Dissolved well in DMSO and worked as expected.....
Date published: 2018-01-08
Rated 5 out of 5 by from Kim et al Kim et al. (PubMed ID 26318800) used CX-4945, a CK2 inhibitor, to block the FAK-Src-pacillin signaling pathway and TGF- -induced cancer cell metastasis. -SCBT Publication Review
Date published: 2015-02-10
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