RAPTA-C
Based on 1 Customer Validation
RAPTA-C is a ruthenium-based antimetastatic agent. RAPTA-C binds chromatin histones and interacts with DNA, leading to pH-dependent DNA damage and hypoxia selectivity. RAPTA-C inhibits angiogenesis, microvessel density, tumor growth, invasion, and proliferation, and induces apoptosis through the mitochondrial pathway, G2/M phase arrest, quiescence, and vascular normalization. RAPTA-C can be used in research on ovarian cancer, colorectal adenocarcinoma, breast cancer metastasis, and Ehrlich ascites carcinoma.
For research use only. We do not sell to patients.
- Purity : 99.30%
- CAS No.: 372948-28-2
- Formula: C16H23Cl2N3PRu
- Molecular Weight:460.32
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
In Vitro
RAPTA-C (31.4-134 µM; adhesion for 3 h, invasion for 48 h) significantly reduces the migration of OVCAR4 in a 3D organotypic model when added after cancer cell adhesion[2].
RAPTA-C (72 h) inhibits the viability of HUVEC, ECRF24, and LS174T cells with an ED50 of 300-500 μg/mL (500-1000 μM)[6].
RAPTA-C (31.4-134 µM; 2 h) shows dose-dependent ruthenium uptake in NOF, HPMC, and OVCAR4 cells, with higher accumulation in HPMC and NOF than in OVCAR4[2].
The PTA ligand pKa of RAPTA-C (compound 1) (0.1 M NaCl) is 3.13, lower than that of free PTA[4].
RAPTA-C binds calf thymus DNA and stabilizes the double helix, increasing Tm from 67 °C to 80 °C (ΔTm = 13 °C)[4].
RAPTA-C (100 µM; 24 h) results in 0.12 µg Ru/106 cells (2.55 × 10−4 M) in TS/A cells, indicating intracellular accumulation[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
In Vivo
RAPTA-C (compound 1) (100-400 mg/kg; intraperitoneal injection) reduces the number of lung metastases in CBA mice bearing MCa breast cancer without reducing primary tumor mass[4].
RAPTA-C reduces lung metastasis growth in CBA mice bearing MCa breast cancer, with no corresponding effect at the primary tumor site[6].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Swiss nu/nu (female, 6-8 weeks old, 20-30 g)[1]
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Dosage:100 mg/kg/day
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Administration:i.p.; daily
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Result:100 mg/kg/day single-agent inhibited tumor growth by 37%.
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Animal Model:CBA[4]
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Dosage:200 mg/kg once on day 5; 200 mg/kg on day 5 followed by a second 200 mg/kg on day 9; 100 mg/kg on days 5, 7, 9, and 11; 40 mg/kg daily from days 5 to 14; 400 mg/kg as a single injection
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Administration:i.p.; once on day 5, days 5 and 9, days 5, 7, 9, and 11, daily days 5-14, or single injection; days 5-14
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Result:At 200 mg/kg single dose, primary tumor was 3498 mg; lung metastases were 13.3; lung metastasis weight was 19.6.
At 200 mg/kg on day 5 and day 9 (200 mg/kg/day ×2), primary tumor was 3663 mg; lung metastases were 6.3; lung metastasis weight was 21.4.
Two of five mice in this group had no metastases at the end of the experiment.
At 100 mg/kg on days 5, 7, 9, and 11 (100 mg/kg/day ×4), primary tumor was 3472 mg; lung metastases were 7.3; lung metastasis weight was 18.7.
At 40 mg/kg daily from days 5 to 14 (40 mg/kg/day ×10), primary tumor was 4173 mg; lung metastases were 12.8; lung metastasis weight was 21.1.
At 400 mg/kg as a single injection, primary tumor was 3442 mg; lung metastases were 19.7; lung metastasis weight was 34.9.
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Animal Model:Swiss athymic (female, 7 weeks old)[5]
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Dosage:10 mg/kg per day; 40 mg/kg per day; 100 mg/kg per day
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Administration:i.p.; once daily; 11 consecutive days
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Result:Tumor growth of RAPTA-C-treated tumors at 100 mg/kg/day was inhibited by approximately 50% compared with control on the last experiment day.
Lower doses (10 and 40 mg/kg/day) did not lead to significant tumor growth inhibition.
Microvessel density was reduced in treated tumors at 100 mg/kg/day.
SMA staining showed that RAPTA-C administration resulted in normalized, more mature blood vessels covered by pericytes; newly formed immature vessels lacking pericytes (CD31+/SMA−) disappeared, and mature vessels (CD31+/SMA+) increased.
Treated tumors showed large areas of necrosis and small patches of Ki-67 negative tumor cells around remaining blood vessels.
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Animal Model:Swiss albino (approximately 25 g each; five mice per group)[10]
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Dosage:40 mg/kg body weight; 50 mg/kg body weight
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Administration:i.p.; once weekly; for 28 days
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Result:The tumour-inoculated mice demonstrated a dose-dependent reduction in tumour volume, with decreased rate of alopecia and vomiting during the administration programme.
About 50% of the EAC cell population was reduced using a dose of 40 mg/kg body weight.
At higher doses, for example 50 mg/kg body weight, approximately 75% of the cell population died.
After the 28th day of administration with a RAPTA-C dose of 40 mg/kg body weight per week, the content of hypoploid DNA (less than 2n DNA) was increased in the RAPTA-C-exposed group compared with the untreated cells.
The DNA content in S phases decreased from 6.2% to 3.6%.
Counts of the G2/M phases also decreased significantly, suggesting that RAPTA-C-induced DNA damage is followed by suppressed EAC proliferation.
The number of annexin V+/PI−, i.e. apoptotic, cells increased significantly compared with the untreated mice (4%), whereas there was no such fluorescence in the annexin V-/PI+ and annexin V+/PI+ quadrant, confirming a dose of approximately 40 mg/kg body weight RAPTA-C induced significant apoptosis in EAC cells.
A dose of 40 mg/kg body weight RAPTA-C markedly induced the expression of p53.
The expression of the upstream regulator of p53, JNK, was significantly higher than in the untreated cells.
It was found that in response to RAPTA-C exposure the expression of p21 significantly increased in the EAC-bearing host, with a simultaneous reduction in the expression of cyclin E, which is necessary to drive the cells towards the M phase.
Resulted in decreased expression of antiapoptotic Bcl-2 and increased expression of proapoptotic Bax protein, compared with the case in untreated mice.
After RAPTA-C exposure, cytosolic cytochrome c protein levels increased.
Less procaspase-9 was detected in the cell cytosol, suggesting that RAPTA-C increased cytochrome c expression, which caused cytochrome c mediated cleavage/activation of caspases to be elevated.
Increased survival of mice after exposure to RAPTA-C was associated with G2/M phase cell cycle arrest and apoptosis induction.
- Human pluripotent stem cell endothelial-cell differentiation
- Vascular/Branching Fractal Analysis
- Annexin V plus membrane-impermeant dye apoptosis staining
- Patient-Derived Orthotopic Xenograft (PDOX)
- Protocol for Cell Cycle
- Breast Cancer Modeling
- Cell Viability Determination by MTT Colorimetric Assay
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Flow cytometric DNA-content cell-cycle staining
- Endothelial Tube Formation Assay
- Patient-Derived Xenograft (PDX)
- Apoptosis Solutions
- Cell invasion
- Subcutaneous Cell-Line-Derived Xenograft
- Genotoxicity/Mutagenicity Study
- Endothelial Cell Migration/Angiogenic Sprouting Assay
- Orthotopic Cell-Line Xenograft
Chemical Information
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CAS No. 372948-28-2
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Appearance Solid
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Molecular Weight 460.32
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Formula C16H23Cl2N3PRu
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Color Yellow to orange
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SMILES
CC12=C3[Ru+2]145(C6=C52)(P78C[N@@](C9)C[N@@](C[N@@]9C8)C7)([Cl-])([Cl-])C6(C(C)C)=C43
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Synonyms
Ru(η6-p-cymene)Cl2(pta)
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : 25 mg/mL (54.31 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)
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (295 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[10]. Chatterjee S, et al. The ruthenium(II)-arene compound RAPTA-C induces apoptosis in EAC cells through mitochondrial and p53-JNK pathways. Journal of biological inorganic chemistry : JBIC : a publication of the Society of Biological Inorganic Chemistry. 2008 Sep;13(7):1149-55. [Content Brief]
Complete Stock Solution Preparation Table
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1724 mL | 10.8620 mL | 21.7240 mL | 54.3100 mL |
| 5 mM | 0.4345 mL | 2.1724 mL | 4.3448 mL | 10.8620 mL | |
| 10 mM | 0.2172 mL | 1.0862 mL | 2.1724 mL | 5.4310 mL | |
| 15 mM | 0.1448 mL | 0.7241 mL | 1.4483 mL | 3.6207 mL | |
| 20 mM | 0.1086 mL | 0.5431 mL | 1.0862 mL | 2.7155 mL | |
| 25 mM | 0.0869 mL | 0.4345 mL | 0.8690 mL | 2.1724 mL | |
| 30 mM | 0.0724 mL | 0.3621 mL | 0.7241 mL | 1.8103 mL | |
| 40 mM | 0.0543 mL | 0.2716 mL | 0.5431 mL | 1.3578 mL | |
| 50 mM | 0.0434 mL | 0.2172 mL | 0.4345 mL | 1.0862 mL |
RAPTA-C Related Classifications
HY-130326 Related Classifications
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