Referencia número: HY-13323

CX-5461

Name: CX-5461
Brand: MedChemExpress
SKU: HY-13323
Price: 132.00 USD
Availability: InStock
Rating: 5 (72 reviews)

72 Cited Publications

Revisión del cliente

Based on 72 publication(s) in Google Scholar

CX-5461 is a selective, orally active RNA polymerase I inhibitor. CX-5461 disrupts the formation of the SL1-rDNA complex, thereby blocking the transcription initiation of ribosomal RNA without altering the activity of RNA polymerase II, DNA replication, or protein translation processes. CX-5461 upregulates the expression of p21, MDM2, Sestrin1/2, and phosphorylated AMPKα, and reduces the level of phosphorylated Akt. CX-5461 induces G2/G2/M cell cycle arrest, Autophagy, Apoptosis, and cellular senescence, and activates CHK1, CHK2, and RPA. CX-5461 can be used in research related to osteosarcoma, cervical cancer, hematologic malignancies, high-grade serous ovarian cancer, and solid tumors.

Para uso exclusivo en investigación. No vendemos a pacientes.

Pureza: 99.67%
No. CAS: 1138549-36-6
Fòrmula: C₂₇H₂₇N₇O₂S
Peso molecular:513.61

Almacenamiento:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

CX-5461 Chemical Structure

No. CAS: 1138549-36-6

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Ensayo clínico
Chemical Information
Publications (72)
Solvente y solubilidad
- In Vitro
- In Vivo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

IC₅₀ & Target

RNA Polymerase

AMPKα

Chk1

Chk2

Ver todos los productos específicos de isoformas DNA/RNA Synthesis :

Ver todos los productos específicos de isoformas AMPK :

Ver todos los productos específicos de isoformas Akt :

Ver todos los productos específicos de isoformas Checkpoint Kinase (Chk) :

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	IC₅₀	0.12 μM Compound: CX-5461	Antiproliferative activity against human A2780 cells incubated for 4 days by MTT assay Antiproliferative activity against human A2780 cells incubated for 4 days by MTT assay	[PMID: 31803394]
HeLa	IC₅₀	6.89 μM Compound: CX-5461	Cytotoxicity against human HeLa cells Cytotoxicity against human HeLa cells	[PMID: 34124673]

In Vitro

CX-5461 (0.5-5 μM; 72 h) inhibits the proliferation of MNNG/HOS and U2-OS osteosarcoma cell lines and induces G₂ phase cell cycle arrest (but does not induce apoptosis), with an IC₅₀ of 0.5-1.5 μM; this drug exerts stronger efficacy on MNNG/HOS cells, while exerting minimal effects on normal NIH3T3 fibroblasts^[1].
CX-5461 (1-5 μM; 72 h) inhibits mTOR activity in MNNG/HOS and U2-OS osteosarcoma cell lines. Its mechanism of action involves downregulating the Akt/mTOR signaling pathway in MNNG/HOS cells, while upregulating the AMPK/mTOR signaling pathway in U2-OS cells^[1].
CX-5461 inhibits the viability of cervical cancer C33A cells, HeLa cells, and normal keratinocyte HaCat cells, with distinct IC₅₀ values for each cell line^[2].
CX-5461 potently and selectively inhibits Pol I-mediated rRNA transcription, exhibiting 200- to 300-fold higher selectivity for Pol I transcription over Pol II-mediated transcription in HCT-116, A375 and MIA PaCa-2 solid tumor cells^[5].
CX-5461 induces p53-dependent apoptotic cell death in p53 wild-type hematologic cancer cell lines (SR, MV 4;11), with viability IC₅₀ values of 5 nM and 12 nM, respectively, while p53-null K562 cells show 10- to 20-fold reduced sensitivity^[3].
CX-5461 (300 nM; 24 h) induces autophagy in A375 melanoma cells and MIA PaCa-2 pancreatic cancer cells, which is evidenced by enhanced LC3B-II staining and concentration-dependent accumulation of acidic vesicular organelles^[5].
CX-5461 (300 nM; 24 h) induces cellular senescence in A375 melanoma cells and MIA PaCa-2 pancreatic cancer cells, as detected by senescence-associated β-galactosidase staining^[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[1]

Cell Line:

human osteosarcoma MNNG/HOS (mutant p53), U2-OS (wild-type p53), murine NIH3T3 fibroblast
Concentration:

0.5-5 μM (viability assays); 0.5-5 μM (cell cycle analysis)
Incubation Time:

72 h (viability assays); 72 h (cell cycle analysis)
Result:

Markedly reduced cell viability in MNNG/HOS and U2-OS cells with IC₅₀ values of 0.5-1.5 μM.
Reduced viability at a slightly lower concentration in MNNG/HOS cells compared to U2-OS cells.
Showed no clear effect on NIH3T3 cells.
Induced accumulation of MNNG/HOS and U2-OS cell populations in the G₂ fraction with no sub-G₁ peak.
Caused no significant cell cycle changes in NIH3T3 cells.

Western Blot Analysis^[1]

Cell Line:

human osteosarcoma MNNG/HOS, U2-OS
Concentration:

1-5 μM
Incubation Time:

72 h
Result:

Inhibited phosphorylated mTOR (Ser²⁴⁴⁸) expression in a dose-dependent manner in both cell lines without affecting total mTOR levels.
Downregulated phosphorylated Akt (Ser⁴⁷³) in MNNG/HOS cells with no change to phosphorylated AMPKα (Thr¹⁷²).
Upregulated phosphorylated AMPKα (Thr¹⁷²) in U2-OS cells with no change to phosphorylated Akt (Ser⁴⁷³).

In Vivo

CX-5461 (50 mg/kg; i.p.; five consecutive days per week; 3 weeks) exerts in vivo antitumor activity against U2-OS osteosarcoma xenografts, reducing tumor volume without causing significant weight loss^[1].
CX-5461 (50 mg/kg; once every 3 days; 3 total doses) prolongs survival of mice with p53 wild-type Eμ-Myc lymphoma, restores white blood cell counts, eliminates >99% of peripheral blood tumor cells, and preserves normal B cells with minimal adverse effects^[3].
CX-5461 (125 mg/kg; i.p.; once weekly; 25 days) potently inhibits growth of human MV 4;11 biphenotypic B myelomonocytic leukemia xenografts in nude mice, induces p53 target gene expression, and is well tolerated^[3].
CX-5461 (50 mg/kg; p.o.; once daily, every 3 days) produces 69% tumor growth inhibition in a murine MIA PaCa-2 pancreatic carcinoma xenograft model with favorable tolerability^[5].
CX-5461 (50 mg/kg; p.o.; once daily, every 3 days) produces 79% tumor growth inhibition in a murine A375 melanoma xenograft model with favorable tolerability^[5].
CX-5461 (50 mg/kg; p.o.; single dose) represses Pol I transcription by 84% in p53 wild-type Eμ-Myc lymphoma cells in vivo, reduces tumor burden and spleen size to near-normal levels, and induces p53-mediated apoptosis within 24 hr while sparing normal cells^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

athymic nu/nu (5-week-old female; subcutaneous xenograft model via injection of 5×10⁶ U2-OS cells)^[1]
Dosage:

50 mg/kg
Administration:

i.p.; five consecutive days per week; 3 weeks
Result:

Reduced tumor volume to approximately 450 mm³ by day 21 post-treatment initiation, versus ~850 mm³ in the vehicle group.
Showed no significant body weight loss compared to controls.

Animal Model:

C57BL/6 (wild-type recipients; p53 wild-type Eμ-Myc lymphoma cells on C57BL/6 background)^[3]
Dosage:

50 mg/kg
Administration:

p.o.; single dose
Result:

Repressed Pol I transcription in lymph node tumor cells by 84% at 1 hr posttreatment.
Reduced lymph node tumor burden to 3.1% GFP-tagged malignant cells at 24 hr posttreatment.
Reduced spleen weight to 0.14 g at 24 hr posttreatment.
Detected activation of p53 and p21, and markers of apoptosis including cleaved CASPASE 3 and increased subG1 cell population within 6 hr of treatment.

Animal Model:

CrTac:Ncr-Foxn1nu (female, 6-8 weeks old)^[3]
Dosage:

125 mg/kg
Administration:

i.p.; once weekly; 25 days
Result:

Exhibited potent antitumor activity, with significant inhibition of tumor growth over the 25-day study period.
Increased tumor levels of the p53 transcriptional target gene p21 relative to vehicle-treated mice.
Showed well-tolerated treatment.

Animal Model:

NCr nu/nu fisol (5- to 6-week-old female, Balb/c origin, subcutaneous inoculation of 5×10⁶ MIA PaCa-2 human pancreatic cancer cells)^[5]
Dosage:

50 mg/kg
Administration:

p.o.; once daily, every 3 days
Result:

Achieved 69% tumor growth inhibition (TGI) on day 31.
Showed no significant changes in animal body weights.

Animal Model:

NCr nu/nu fisol (5- to 6-week-old female, Balb/c origin, subcutaneous inoculation of 5×10⁶ A375 human melanoma cells)^[5]
Dosage:

50 mg/kg
Administration:

p.o.; once daily, every 3 days
Result:

Achieved 79% tumor growth inhibition (TGI) on day 32.
Showed no significant changes in animal body weights.

Ensayo clínico

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

No. CAS 1138549-36-6
Appearance Solid
Peso molecular 513.61
Fòrmula C₂₇H₂₇N₇O₂S
Color White to yellow
SMILES

CC1=NC=C(CNC(C2=C3N(C4=NC(N5CCN(CCC5)C)=CC=C4C2=O)C6=C(S3)C=CC=C6)=O)N=C1
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (72)

All Cell Proliferation/Viability AssayCell Imaging/StainingRT-PCRWB

Sort by:

Journal Impact Factor

Nature

Mapping and engineering RNA-driven architecture of the multiphase nucleolus. [Abstract]

2025 Aug;644(8076):557-566. PMID: 40604277
Science

Different repair pathways support intact or truncated insertions by R2 retrotransposon protein. [Abstract]

2026 Feb 26;391(6788):eadz3121. PMID: 41231928
Cell

RNA damage compartmentalization by DHX9 stress granules. [Abstract]

2024 Mar 28;187(7):1701-1718.e28. PMID: 38503283
Mol Cancer

AI-based classification of anticancer drugs reveals nucleolar condensation as a predictor of immunogenicity. [Abstract]

2024 Dec 20;23(1):275. PMID: 39702289
Nat Cell Biol

Stalled replication fork protection limits cGAS-STING and P-body-dependent innate immune signalling. [Abstract]

2022 Jul;24(7):1154-1164. PMID: 35817959
Cancer Res

Combined Inactivation of CTPS1 and ATR Is Synthetically Lethal to MYC-Overexpressing Cancer Cells. [Abstract]

2022 Mar 15;82(6):1013-1024. PMID: 35022212
J Extracell Vesicles

Plant exosomes fused with engineered mesenchymal stem cell-derived nanovesicles for synergistic therapy of autoimmune skin disorders. [Abstract]

2023 Oct;12(10):e12361. PMID: 37859568
Nat Commun

Coacervate droplets as pH-regionalized protocells. [Abstract]

2026 Feb 2;17(1):2252. PMID: 41629347
Nat Commun

Phase separated condensates of ATRX regulate neural progenitor identity. [Abstract]

2025 Jul 14;16(1):6489. PMID: 40659667
Nat Commun

Phosphorylation of a nuclear condensate regulates cohesion and mRNA retention. [Abstract]

2025 Jan 4;16(1):390. PMID: 39755675
Nat Commun

G-quadruplex stabilization provokes DNA breaks in human PKD1, revealing a second hit mechanism for ADPKD. [Abstract]

2025 Jan 2;16(1):121. PMID: 39747084
Nat Commun

Androgen deprivation induces double-null prostate cancer via aberrant nuclear export and ribosomal biogenesis through HGF and Wnt activation. [Abstract]

2024 Feb 9;15(1):1231. PMID: 38336745
Nat Commun

Glutamine deficiency in solid tumor cells confers resistance to ribosomal RNA synthesis inhibitors. [Abstract]

2022 Jun 28;13(1):3706. PMID: 35764642
Nat Commun

A role for Tau protein in maintaining ribosomal DNA stability and cytidine deaminase-deficient cell survival. [Abstract]

2017 Sep 25;8(1):693. PMID: 28947735
Mol Cell

Endogenous YAP/TAZ partitioning in TEAD condensates orchestrates the Hippo response. [Abstract]

2025 Sep 18;85(18):3425-3442.e10. PMID: 40914169
Nucleic Acids Res

Guanine quadruplexes in the RNA genome of the tick-borne encephalitis virus: their role as a new antiviral target and in virus biology. [Abstract]

2022 May 6;50(8):4574-4600. PMID: 35420134
Sci Adv

TERT accelerates BRAF mutant-induced thyroid cancer dedifferentiation and progression by regulating ribosome biogenesis. [Abstract]

2023 Sep;9(35):eadg7125. PMID: 37647391

CX-5461 purchased from MedChemExpress. Usage Cited in: Sci Adv. 2023 Sep;9(35):eadg7125. [Abstract]

Effects of CX-5461 dihydrochloride (0-500 nM) on colony formation of BCPAP, 312BTC, and OCM1 cells.

CX-5461 purchased from MedChemExpress. Usage Cited in: Sci Adv. 2023 Sep;9(35):eadg7125. [Abstract]

Effects of CX-5461 dihydrochloride on survival of BCPAP, 312BTC, and OCM1 cells in CCK8 assay.

CX-5461 purchased from MedChemExpress. Usage Cited in: Sci Adv. 2023 Sep;9(35):eadg7125. [Abstract]

H&E and Ki67 staining of BCPAP and OCM1 xenografts with vehicle or CX-5461 dihydrochloride.

CX-5461 purchased from MedChemExpress. Usage Cited in: Sci Adv. 2023 Sep;9(35):eadg7125. [Abstract]

Representative thyroid differentiation-associated genes PAX8, DIO1, THRA, THRB, FOXE1, and TSHR qPCR results of K1, BCPAP, and SW1736 after CX-5461 dihydrochloride (100 nM, 0-48 h) treatment for 0, 24, and 48 hours.

CX-5461 purchased from MedChemExpress. Usage Cited in: Sci Adv. 2023 Sep;9(35):eadg7125. [Abstract]

Western blots show PAX8 and NIS change of K1, BCPAP, 312BTC, and SW1736 treated by CX-5461 dihydrochloride (100 nM) for 0, 24, and 48 hours.
Mol Biomed

Lactate-driven pyrimidine synthesis promotes ferroptosis resistance in hepatocellular carcinoma. [Abstract]

2026 Apr 17;7(1):53. PMID: 41996004
Blood Cancer Discov

Rapid Transcription Dynamics Confers Cytarabine Resistance in Acute Myeloid Leukemia. [Abstract]

2026 Jul 1;7(4):624-641. PMID: 42149820
Cell Death Dis

Pre-rRNAs control mitosis by maintaining chromosomal segregation through protecting SMC2 from AURKA-mediated phosphorylation. [Abstract]

2025 Nov 7;16(1):812. PMID: 41203590
Cell Death Dis

LncRNA SNHG26 promotes gastric cancer progression and metastasis by inducing c-Myc protein translation and an energy metabolism positive feedback loop. [Abstract]

2024 Mar 29;15(3):236. PMID: 38553452
Cell Commun Signal

Elevation of effective p53 expression sensitizes wild-type p53 breast cancer cells to CDK7 inhibitor THZ1. [Abstract]

2022 Sep 5;20(1):96. PMID: 36058938
Clin Cancer Res

Targeting RNA-Polymerase I in Both Chemosensitive and Chemoresistant Populations in Epithelial Ovarian Cancer. [Abstract]

2017 Nov 1;23(21):6529-6540. PMID: 28778862

CX-5461 purchased from MedChemExpress. Usage Cited in: Clin Cancer Res. 2017 Nov 1;23(21):6529-6540. [Abstract]

Western blot analysis verifying G2/M phase arrest in 6 cell lines. Treatment with IC₅₀ dosages of CX-5461 shows an increase in expression of pCDC2(tyr15) and Cyclin-B versus untreated controls at 72 hours.

CX-5461 purchased from MedChemExpress. Usage Cited in: Clin Cancer Res. 2017 Nov 1;23(21):6529-6540. [Abstract]

Western blot analysis shows activation of the pCHK1(ser317) and pCHK2(T68), downstream substrates of ATM and ATR kinases. TP53 wild type cell lines show a subsequent activation of p21 but drug response is independent of TP53 status.
Acta Biomater

CX-5461-loaded nucleolus-targeting nanoplatform for cancer therapy through induction of pro-death autophagy. [Abstract]

2018 Oct 1:79:317-330. PMID: 30172068
J Transl Med

RBIS regulates ribosome biogenesis to affect progression in lung adenocarcinoma. [Abstract]

2024 Dec 25;22(1):1147. PMID: 39722009
Dev Cell

CircRNA-encoded RIPK1-98 protein drives lung adenocarcinoma progression. [Abstract]

2026 Mar 12:S1534-5807(26)00079-1. PMID: 41825439
Int J Biol Macromol

TBC1D14 inhibits ribosome biogenesis to reduce lymph node metastasis in head and neck squamous cell carcinoma by mediating DDX31 ubiquitination. [Abstract]

2025 Sep;322(Pt 1):146723. PMID: 40784392
Int J Biol Macromol

Trained immunity driven by Enterococcus faecalis ribosomal protein S11 enhances antigen presentation and boosts influenza vaccine efficacy via nanoparticle delivery. [Abstract]

2025 Jun;315(Pt 1):144179. PMID: 40381785
Mol Ther Oncol

Targeting the ribosome to treat multiple myeloma. [Abstract]

2024 Feb 7;32(1):200771. PMID: 38596309
EMBO J

RAD54L coordinates the nucleolar DNA damage response to maintain rDNA stability. [Abstract]

2026 Jul 23. PMID: 42493648
Free Radic Biol Med

CX-5461 ameliorates disease in lupus-prone mice by triggering B-cell ferroptosis via p53-SLC7A11-ALOX12 pathway. [Abstract]

2024 Oct:223:325-340. PMID: 39111584
EMBO Mol Med

NF45/NF90-mediated rDNA transcription provides a novel target for immunosuppressant development. [Abstract]

2021 Mar 5;13(3):e12834. PMID: 33555115
Cell Prolif

Hypertranscription of rDNA Responsible for Nucleolar Remodelling is a Doorman for Acquiring Pluripotency. [Abstract]

2025 Oct;58(10):e70052. PMID: 40320363
Anal Chem

Single-Molecule Detection on Intrastrand Interactions among G4 Clusters. [Abstract]

2025 Jun 10;97(22):11617-11626. PMID: 40408126
Mol Cancer Ther

APTO-253 Stabilizes G-quadruplex DNA, Inhibits MYC Expression, and Induces DNA Damage in Acute Myeloid Leukemia Cells. [Abstract]

2018 Jun;17(6):1177-1186. PMID: 29626127
Eur J Med Chem Rep

2025 Dec.
Life Sci

CAD drives Angiotensin II-induced vascular smooth muscle cell activation via upregulation of pyrimidine biosynthesis and rRNA synthesis. [Abstract]

2026 Jun 9:401:124530. PMID: 42264140
J Cell Biol

Real-time imaging of RNA polymerase I activity in living human cells. [Abstract]

2023 Jan 2;222(1):e202202110. PMID: 36282216
Matrix Biol

Loss of MMP9 disturbs cranial suture fusion via suppressing cell proliferation, chondrogenesis and osteogenesis in mice. [Abstract]

2024 Dec:134:93-106. PMID: 39374863
Eur J Pharmacol

VOPP1, a determinant of the sensitivity of non-small cell lung cancer cells to NAE inhibitors. [Abstract]

2025 Sep 15:1003:177942. PMID: 40651787
Molecules

CX-5461 Inhibits Pancreatic Ductal Adenocarcinoma Cell Growth, Migration and Induces DNA Damage. [Abstract]

2019 Dec 4;24(24):4445. PMID: 31817270
Am J Pathol

MYC-Mediated Ribosomal Gene Expression Sensitizes Enzalutamide-resistant Prostate Cancer Cells to EP300/CREBBP Inhibitors. [Abstract]

2021 Jun;191(6):1094-1107. PMID: 33705753
Cell Signal

CX-5461 inhibits cell proliferation and induces ferroptosis of colorectal cancer cells by inactivating Nrf2 pathway. [Abstract]

2025 Nov:135:111998. PMID: 40664345
FASEB J

Transient inhibition of rDNA transcription in donor cells improves ribosome biogenesis and preimplantation development of embryos derived from somatic cell nuclear transfer. [Abstract]

2020 Jun;34(6):8283-8295. PMID: 32323360
Development

Ribosome biogenesis is essential for hemogenic endothelial cells to generate hematopoietic stem cells. [Abstract]

2024 Nov 1;151(21):dev202875. PMID: 39324287
Exp Cell Res

Metastatic breast cancer cells adapt to a soft environment with limited involvement of mechanotransduction. [Abstract]

2025 Jun 2;450(2):114629. PMID: 40466802
Biochimie

Probing the folding pathways of four-stranded intercalated cytosine-rich motifs at single base-pair resolution. [Abstract]

2022 Apr 20;199:81-91. PMID: 35452743
Invest New Drugs

Discovery of MTR-106 as a highly potent G-quadruplex stabilizer for treating BRCA-deficient cancers. [Abstract]

2021 Oct;39(5):1213-1221. PMID: 33710464
Tissue Cell

Combined inhibition of WEE1 by AZD1775 synergistically enhances CX-5461 mediated DNA damage and induces cytotoxicity in glioblastoma. [Abstract]

2025 Dec:97:103093. PMID: 40839955
Open Biol

The histone deacetylase inhibitor Scriptaid targets G-quadruplexes. [Abstract]

2025 Feb;15(2):240183. PMID: 39965659
Life Sci Alliance

FUS (fused in sarcoma) is a component of the cellular response to topoisomerase I-induced DNA breakage and transcriptional stress. [Abstract]

2019 Feb 26;2(2):e201800222. PMID: 30808650
Biochim Biophys Acta Gen Subj

c-MYC G-quadruplex binding by the RNA polymerase I inhibitor BMH-21 and analogues revealed by a combined NMR and biochemical Approach. [Abstract]

2018 Mar;1862(3):615-629. PMID: 29229300
G3 (Bethesda)

CX-5461 and doxorubicin activate a shared DNA damage-associated transcriptional response in human cardiomyocytes. [Abstract]

2026 Mar 4;16(3):jkag008. PMID: 41543508
Res Sq

2026 Apr 2.
bioRxiv

2026 Apr 4.
bioRxiv

2026 Mar 18.
Autophagy Rep

TFEB confers resistance against the chemotherapeutic agent CX-5461. [Abstract]

2026 Feb 13;5(1):2624259. PMID: 41717449
bioRxiv

2026 Jan 7.
bioRxiv

Dual RNA Polymerase I Inhibition with CX-5461 and BMH-21 Synergizes in Breast Cancer by Activating p53-Dependent Stress. [Abstract]

2025 Nov 20:2025.11.19.689351. PMID: 41332727
bioRxiv

2025 Aug 19.
bioRxiv

2025 Jul 23.
bioRxiv

2025 May 10.
bioRxiv

2025 January 21.
bioRxiv

2024 November 28.
bioRxiv

Active RNA synthesis patterns nuclear condensates. [Abstract]

2024 Oct 13:2024.10.12.614958. PMID: 39498261
bioRxiv

Mapping and engineering RNA-controlled architecture of the multiphase nucleolus. [Abstract]

2024 Sep 29:2024.09.28.615444. PMID: 39386460
bioRxiv

2023 Jan 31.
Utrecht University

2023 Feb.
bioRxiv

2021 Dec.
Biomed Pharmacother

Combined inhibition of RNA polymerase I and mTORC1/2 synergize to combat oral squamous cell carcinoma. [Abstract]

2021 Jan:133:110906. PMID: 33190037
Patent

US20190169215A1
Oncotarget

Human cytomegalovirus and Herpes Simplex type I virus can engage RNA polymerase I for transcription of immediate early genes. [Abstract]

2017 Oct 29;8(57):96536-96552. PMID: 29228551

CX-5461 purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 Oct 29;8(57):96536-96552. [Abstract]

Protein levels of HCMV IE (IE1:IE72, IE2:IE86) and pp65 are detected by WB analysis in untreated and pre-treated HCMV infected cells 72hpi.

Solvente y solubilidad

In Vitro:

0.5 M HCl : 25 mg/mL (48.68 mM; ultrasonic and warming and heat to 60°C)

50 mM Sodium phosphate (pH 3.5) : 10 mg/mL (19.47 mM; Need ultrasonic)

DMSO : 2 mg/mL (3.89 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.9470 mL

9.7350 mL

19.4700 mL

5 mM

0.3894 mL

1.9470 mL

3.8940 mL

10 mM

0.1947 mL

0.9735 mL

1.9470 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculadora de molaridad

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 15% Cremophor EL 85% Saline

Solubility: 10 mg/mL (19.47 mM); Suspended solution; Need ultrasonic

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (305 KB)
SDS (396 KB)
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COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Li L, et al. CX-5461 induces autophagy and inhibits tumor growth via mammalian target of rapamycin-related signaling pathways in osteosarcoma. OncoTargets and therapy. 2016;9:5985-5997. [Content Brief]

[2]. Liu X, et al. RNA polymerase I inhibitor CX-5461 suppresses cervical cancer cell growth by inducing DNA damage and mitotic catastrophe and enhances cisplatin sensitivity. Biochemical pharmacology. 2026 Jun;248:117828. [Content Brief]

[3]. Bywater MJ, et al. Inhibition of RNA polymerase I as a therapeutic strategy to promote cancer-specific activation of p53. Cancer cell. 2012 Jul 10;22(1):51-65. [Content Brief]

[4]. Sanij E, et al. CX-5461 activates the DNA damage response and demonstrates therapeutic efficacy in high-grade serous ovarian cancer. Nature communications. 2020 May 26;11(1):2641.

[5]. Drygin D, et al. Targeting RNA polymerase I with an oral small molecule CX-5461 inhibits ribosomal RNA synthesis and solid tumor growth. Cancer research. 2011 Feb 15;71(4):1418-30. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO / 50 mM Sodium phosphate (pH 3.5) / 0.5 M HCl	1 mM	1.9470 mL	9.7350 mL	19.4700 mL	48.6751 mL
50 mM Sodium phosphate (pH 3.5) / 0.5 M HCl	5 mM	0.3894 mL	1.9470 mL	3.8940 mL	9.7350 mL
	10 mM	0.1947 mL	0.9735 mL	1.9470 mL	4.8675 mL
	15 mM	0.1298 mL	0.6490 mL	1.2980 mL	3.2450 mL
0.5 M HCl	20 mM	0.0974 mL	0.4868 mL	0.9735 mL	2.4338 mL
	25 mM	0.0779 mL	0.3894 mL	0.7788 mL	1.9470 mL
	30 mM	0.0649 mL	0.3245 mL	0.6490 mL	1.6225 mL
	40 mM	0.0487 mL	0.2434 mL	0.4868 mL	1.2169 mL

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CX-5461

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CX-5461

Publications Citing Use of MedChemExpress (MCE) CX-5461

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