Silmitasertib

Cat.NO.:A103748 Purity:98%

Product Details of Silmitasertib

CAS No. :	1009820-21-6
Formula :	C₁₉H₁₂ClN₃O₂
M.W :	349.77
SMILES Code :	O=C(C1=CC=C2C(N=C(NC3=CC=CC(Cl)=C3)C4=C2C=NC=C4)=C1)O
Synonyms :	CX-4945
MDL No. :	MFCD13184796
InChI Key :	MUOKSQABCJCOPU-UHFFFAOYSA-N
Pubchem ID :	24748573

Safety of Silmitasertib

GHS Pictogram:
Signal Word:	Warning
Hazard Statements:	H302-H315-H319-H332-H335
Precautionary Statements:	P261-P280-P305+P351+P338

Related Pathways of Silmitasertib

DNA

Hedgehog

Isoform Comparison

Biological Activity

Target

CK2

CK2, IC50:1 nM

In Vitro:

Cell Line U87MG T98G U251 MCF-7 HCT-116 H1299 cells HNSCC cells (OSC19, UMSCC1, MDA1586) PDX cells (WVUSCC-AR2, WVUSCC-AR5) Cal-27 UM1 HSC-3 HSC-4	Concentration	Treated Time	Description	References

U87MG	25 μM	6 h	To study the effect of CK2 inhibitor on ECE1c stability, results showed that ECE1cK6R exhibited enhanced stability both in the presence and absence of silmitasertib.	PMC9914402
T98G	25 μM	6 h	To study the effect of CK2 inhibitor on ECE1c stability, results showed that ECE1cK6R exhibited enhanced stability both in the presence and absence of silmitasertib.	PMC9914402
U251	25 μM	6 h	To study the effect of CK2 inhibitor on ECE1c stability, results showed that ECE1cK6R exhibited enhanced stability both in the presence and absence of silmitasertib.	PMC9914402
MCF-7	1 μM	24 h	To evaluate the effect of Silmitasertib on cell viability. Results showed a significant reduction in cell viability.	PMC6530875
HCT-116	2 μM	48 h	To assess the impact of Silmitasertib on apoptosis. Results indicated an increase in apoptotic cells.	PMC6530875
H1299 cells	37 μM	1 h	To investigate the effect of Silmitasertib on N protein LLPS, results showed that Silmitasertib had no detectable effect on N protein LLPS.	PMC8035206
HNSCC cells (OSC19, UMSCC1, MDA1586)	0.5-10 µM	12-24 h	To evaluate the effect of Silmitasertib on HNSCC cell invasion, results showed that Silmitasertib significantly reduced extracellular matrix (ECM) degradation and invadopodia formation.	PMC6445698
PDX cells (WVUSCC-AR2, WVUSCC-AR5)	0.5-10 µM	24 h	To evaluate the effect of Silmitasertib on PDX cell invasion, results showed that Silmitasertib significantly reduced extracellular matrix (ECM) degradation and invadopodia formation.	PMC6445698
Cal-27	10, 20, 40 µM	24, 48 h	To test the effect of Silmitasertib combined with DDP treatment on the viability of Cal-27 cells, the results showed that the combined treatment significantly reduced cell viability.	PMC8592591
UM1	10, 20, 40 µM	24, 48 h	To test the effect of Silmitasertib combined with DDP treatment on the viability of UM1 cells, the results showed that the combined treatment significantly reduced cell viability.	PMC8592591
HSC-3	10, 20, 40 µM	12 h	To observe the effect of Silmitasertib on macropinocytosis in HSC-3 cells, the results showed that Silmitasertib induced cell vacuolation.	PMC8592591
HSC-4	10, 20, 40 µM	12 h	To observe the effect of Silmitasertib on macropinocytosis in HSC-4 cells, the results showed that Silmitasertib induced cell vacuolation.	PMC8592591

In Vivo:

Species BALB/c nude mice Mice Mice Nude mice	Animal Model ovarian cancer xenograft model Xenograft model HNSCC orthotopic tongue tumor model Cal-27 xenograft model	Administration	Dosage	Frequency	Description	References

BALB/c nude mice	ovarian cancer xenograft model	oral	60 mg/kg	twice daily, until the end of the experiment	Silmitasertib significantly inhibited tumor growth	PMC11743126
Mice	Xenograft model	Oral	50 mg/kg	Once daily for 21 days	To determine the efficacy of Silmitasertib in reducing tumor growth. Results showed a significant reduction in tumor volume.	PMC6530875
Mice	HNSCC orthotopic tongue tumor model	Oral	50 mg/kg	Twice daily for three weeks	To evaluate the effect of Silmitasertib on HNSCC orthotopic tongue tumor invasion, results showed that Silmitasertib significantly reduced tumor invasion and perineural invasion.	PMC6445698
Nude mice	Cal-27 xenograft model	Peritumoral injection	60 mg/kg	Once every 5 days for 4 weeks	To verify the tumor suppressive effect of Silmitasertib combined with DDP in vivo, the results showed that the combined treatment significantly inhibited tumor growth.	PMC8592591

Clinical Trial:

NCT Number	Conditions	Phases	Recruitment	Completion Date	Locations

NCT00891280	Advanced Solid Tumors … More >> Breast Cancer Inflammatory Breast Cancer Castleman’s Disease Multiple Myeloma Less <<	Phase 1	Unknown	December 2011	United States, Arizona … More >> Mayo Clinic Arizona Recruiting Scottsdale, Arizona, United States, 85259 Contact: Clinical Trials Office Mayo Clinic Cancer Center 507-538-7623 Principal Investigator: Donald Northfelt, MD United States, Colorado Front Range Cancer Specialists Recruiting Fort Collins, Colorado, United States, 80528 Contact: P. Zeller 970-212-7609 Principal Investigator: Robert F Marschke, MD Front Range Cancer Specialists Recruiting Loveland, Colorado, United States, 80528 Contact: Pat Zeller 970-212-7609 Principal Investigator: R. McFarland, MD United States, Texas U T M D Anderson Cancer Center Recruiting Houston, Texas, United States, 77030 Contact: R. Alvarez, MD ralvarez@mdanderson.org Principal Investigator: R. Alvarez, MD Less <<
NCT03571438	Kidney Cancer	Not Applicable	Recruiting	September 30, 2024	France … More >> Grenoble Alps Hospital Recruiting Grenoble, France, 38043 Contact: Jean-Luc Descotes, PU-PH Less <<
NCT02128282	Cholangiocarcinoma	Phase 1 Phase 2	Recruiting	November 2021	United States, Arizona … More >> Mayo Clinic Recruiting Scottsdale, Arizona, United States, 85259-5499 Contact: Mayo Clinic Clinical Trials Office 855-776-0015 Principal Investigator: Mitesh Borad, M.D. United States, Colorado University of Colorado- Denver Recruiting Aurora, Colorado, United States, 80045 Contact: Amy Szilard 720-848-0702 Amy.Szilard@ucdenver.edu Principal Investigator: Sarah (Lindsey) Davis, MD United States, Florida Mayo Clinic Recruiting Jacksonville, Florida, United States, 32224 Contact: Mayo Clinic Clinical Trials Office 855-776-0015 Principal Investigator: Kabir Mody, MD United States, Minnesota Mayo Clinic Recruiting Rochester, Minnesota, United States, 55905 Contact: Mayo Clinic Clinical Trials Office 855-776-0015 Principal Investigator: Joleen Hubbard, MD United States, Texas Texas Oncology – Baylor Charles A. Sammons Cancer Center Recruiting Dallas, Texas, United States, 75246 Contact: Tammy Carmical, RN 214-370-1937 tammy.carmical@usoncology.com Principal Investigator: Carlos Becerra, M.D. Texas Oncology-Tyler Recruiting Tyler, Texas, United States, 75702 Contact: Karen Poe, RN 903-579-9869 karen.poe@usoncology.com Principal Investigator: Donald A Richards, M.D. Korea, Republic of Asan Medical Center Recruiting Seoul, Songpa-gu, Korea, Republic of, 138-736 Contact: Heung-Moon Chang, MD 82-3010-3219 ext 3210 changhm@amc.seoul.kr Contact: Seok kyung Jeong 82-2-3010-5634 jsk0213@amc.seoul.kr Samsung Medical Center Recruiting Seoul, Korea, Republic of Contact: Eunyou Lee 82-2-3410-0955 ley0709@samsung.com Principal Investigator: Joon Oh Park, MD Seoul National University Hospital Recruiting Seoul, Korea, Republic of Contact: Myoungsun Choi 82-2-2072-7612 iamyou3@hanmail.net Principal Investigator: Do-Youn Oh, MD Severance Hospital, Yonsei University Health System Recruiting Seoul, Korea, Republic of Contact: So Young Hwang 82-2-2228-8180 syhwang@yuhs.ac Principal Investigator: Sun Young Rha, MD Taiwan China Medical University Hospital Recruiting Taichung City, Taiwan Contact: Pei-Chen Hsu +886-4-2205-2121 peggyshiu0807@gmail.com Principal Investigator: Li-Yuan Bai, M.D. Less <<
NCT01199718	Multiple Myeloma	PHASE1	UNKNOWN	2025-09-11	Kettering, Ohio, 45249, United… More >> States\|Oregon Health Science University, Portland, Oregon, 97239, United States\|Springfield, Oregon, 97477, United States\|Greenville, South Carolina, 29605, United States\|Norfolk, Virginia, 23502, United States\|Yakima, Washington, 98902, United States Less <<
NCT04668209	Coronavirus	PHASE2	TERMINATED	2022-10-19	Banner University Medical Cent… More >>er Phoenix, Phoenix, Arizona, 85006, United States\|Banner University Medical Center Tucson, Tucson, Arizona, 85724, United States Less <<
NCT05817708	COVID-19	PHASE1	COMPLETED	2023-06-20	Taipei Medical University Hosp… More >>ital, Taipei, 110301, Taiwan Less <<
NCT03897036	Carcinoma, Basal Cell	PHASE1	ACTIVE_NOT_RECRUITING	2025-12-23	University of Colorado Anschut… More >>z Medical Campus, Aurora, Colorado, 80045, United States\|H. Lee Moffitt Cancer Center & Research Institute, Inc., Tampa, Florida, 33612, United States\|University of Texas MD Anderson Cancer Center, Houston, Texas, 77030, United States\|Inova Schar Cancer Institute, Fairfax, Virginia, 22031, United States Less <<

Protocol

Bio Calculators

Preparing Stock Solutions

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.86mL

0.57mL

0.29mL

14.30mL

2.86mL

1.43mL

28.59mL

5.72mL

2.86mL

References

[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]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.

[3]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.

Details

Reviews

There are no reviews yet.

Be the first to review “Silmitasertib”

Products

Product Details of Silmitasertib

Safety of Silmitasertib

Related Pathways of Silmitasertib

Isoform Comparison

Biological Activity

Protocol

References

Details

Reviews

3′-Bromo-4′-fluoroacetanilide

PIPERAZINE， 1，4-BIS(2-CHLOROETHYL)-

Quick Links

Support Links

Locations