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CX-5461

Cat. No. M2293
CX-5461 Structure
Synonym:

Pidnarulex

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
2mg USD 47  USD47 In stock
5mg USD 97  USD97 In stock
10mg USD 162  USD162 In stock
25mg USD 290  USD290 In stock
50mg USD 498  USD498 In stock
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Quality Control & Documentation
Biological Activity

CX-5461 (Pidnarulex) is a potent small-molecule rRNA synthesis inhibitor with an IC50 of 0.11 μM. CX-5461 selectively blocks RNA PolI transcription,PIC assembly and SL1-rDNA interaction. CX-5461 indicates potent antiproliferative activity in cancer cells and induces autophagy incancer cells. CX-5461 shows potent antitumor activity in A375 and MiaPaca xenografts.

Product Citations
Customer Product Validations & Biological Datas
Source J Exp Clin Cancer Res (2018). Figure 4. CX-5461
Method RT-PCR analysis
Cell Lines GBM cells
Concentrations 1 μM
Incubation Time 48 h
Results CX-5461 could lead to a significant decrease of hTERT-FL in a dose-dependent manner and had no effect on hTERT-All
Chemical Information
Molecular Weight 513.61
Formula C27H27N7O2S
CAS Number 1138549-36-6
Solubility (25°C) Water 50 mg/mL (ultrasonic and adjust pH to 2 with HCl)
50 mM sodium phosphate (pH 3.5) : 10 mg/mL (Need ultrasonic)
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Robert Cornelison, et al. CX-5461 Treatment Leads to Cytosolic DNA-Mediated STING Activation in Ovarian Cancer

[2] Mitchell G Lawrence, et al. CX-5461 Sensitizes DNA Damage Repair-proficient Castrate-resistant Prostate Cancer to PARP Inhibition

[3] Elaine Sanij, et al. CX-5461 activates the DNA damage response and demonstrates therapeutic efficacy in high-grade serous ovarian cancer

[4] Yanhong Duo, et al. CX-5461-loaded nucleolus-targeting nanoplatform for cancer therapy through induction of pro-death autophagy

[5] Ada W Y Leung, et al. Copper-CX-5461: A novel liposomal formulation for a small molecule rRNA synthesis inhibitor

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Keywords: CX-5461, Pidnarulex supplier, DNA/RNA Synthesis, inhibitors, activators


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