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Silmitasertib sodium salt

Catalog No. T15024   CAS 1309357-15-0
Synonyms: CX-4945 sodium salt

Silmitasertib sodium salt (CX-4945 sodium salt) is a potent and orally bioavailable, highly selective inhibitor of CK2(IC50 of 1 nM, CK2α).

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Silmitasertib sodium salt Chemical Structure
Silmitasertib sodium salt, CAS 1309357-15-0
Pack Size Availability Price/USD Quantity
1 mg In stock $ 31.00
2 mg In stock $ 41.00
5 mg In stock $ 67.00
10 mg In stock $ 97.00
25 mg In stock $ 186.00
50 mg In stock $ 337.00
1 mL * 10 mM (in DMSO) In stock $ 74.00
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Purity: 99.49%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Silmitasertib sodium salt (CX-4945 sodium salt) is a potent and orally bioavailable, highly selective inhibitor of CK2(IC50 of 1 nM, CK2α).
Targets&IC50 CK2α:1 nM, CK2α':1 nM
In vitro Silmitasertib induces cytotoxicity and apoptosis, and exerts anti-proliferative effects in hematological tumors by downregulating CK2 expression and suppressing activation of CK2-mediated PI3K/Akt/mTOR signaling pathways[3]. Silmitasertib (CX-4945) resultes in cell-cycle arrest and selectively induces apoptosis in cancer cells relative to normal cells, attenuates PI3K/Akt signalingand. The antiproliferative activity of Silmitasertib is correlated with expression levels of the CK2α catalytic subunit, attenuation of PI3K/Akt signaling[1]. Silmitasertib with PS-341 treatment prevents leukemic cells from engaging a functional UPR in order to buffer the PS-341-mediated proteotoxic stress in ER lumen, and decreases pro-survival ER chaperon BIP/Grp78 expression[2].
In vivo Silmitasertib (CX-4945), administered at doses of 25 or 75 mg/kg orally, was well tolerated and demonstrated strong antitumor effects alongside significant decreases in the mechanistic biomarker phospho-p21 (T145) in murine xenograft models[1].
Synonyms CX-4945 sodium salt
Molecular Weight 371.75
Formula C19H11ClN3NaO2
CAS No. 1309357-15-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: 16.67 mg/mL (44.84 mM), Sonication is recommended.

DMSO: 6 mg/mL (16.13 mM), Sonication is recommended.

TargetMolReferences and Literature

1. Siddiqui-Jain A, et al. 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. 2. Kendall JJ, et al. CK2 blockade causes MPNST cell apoptosis and promotes degradation of β-catenin. Oncotarget. 2016 Aug 16;7(33):53191-53203. 3. Buontempo F, et al. Synergistic cytotoxic effects of PS-341 and CK2 inhibitor CX-4945 in acute lymphoblastic leukemia: turning off the prosurvival ER chaperone BIP/Grp78 and turning on the pro-apoptotic NF-κB. Oncotarget. 2016 Jan 12;7(2):1323-40. 4. Chon HJ, et al. The casein kinase 2 inhibitor, CX-4945, as an anti-cancer drug in treatment of human hematological malignancies. Front Pharmacol. 2015 Mar 31;6:70.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Anti-Cancer Drug Library Kinase Inhibitor Library Drug Repurposing Compound Library Anti-Cancer Clinical Compound Library Anti-Cancer Active Compound Library Endoplasmic Reticulum Stress Compound Library Bioactive Compounds Library Max Stem Cell Differentiation Compound Library Clinical Compound Library

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Emodin A-3 hydrochloride PI-828 XL413 TBCA FPFT-2216 Silmitasertib Casein kinase 1δ-IN-7

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Keywords

Silmitasertib sodium salt 1309357-15-0 Autophagy Metabolism Stem Cells Casein Kinase Silmitasertib CX4945 inhibit CX-4945 sodium salt Inhibitor CX-4945 sodium CX 4945 CX-4945 Silmitasertib sodium inhibitor

 

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