| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Targets |
Topoisomerase I (indirectly, as a metabolite of the active topoisomerase I inhibitor irinotecan). RPR121056 itself has negligible pharmacological activity as a topoisomerase I inhibitor. It is formed from irinotecan by CYP3A4, and it does not further convert to the active metabolite SN-38. It is a structurally related camptothecin analog with an open lactone ring and a modified piperidino side chain.
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| ln Vitro |
In vitro, RPR121056 is inactive as a topoisomerase I inhibitor. Unlike irinotecan and its active metabolite SN-38, RPR121056 does not induce DNA single-strand breaks or cell cycle arrest in cancer cell lines. It is used as a negative control in bioactivity assays to distinguish the parent drug from its pharmacologically inert metabolites. It shows no significant cytotoxicity in human cancer cell lines at concentrations up to 100 uM. It also does not inhibit acetylcholinesterase (AChE), unlike irinotecan which directly inhibits AChE.
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| ln Vivo |
No in vivo activity is associated with RPR121056 itself, as it is an inactive metabolite. In humans, it circulates in plasma after irinotecan administration and is primarily excreted in urine and bile. It does not contribute to the anticancer efficacy of irinotecan, which is mediated by SN-38. However, it may serve as a pharmacokinetic marker for CYP3A4 activity. In animal studies, it is a major metabolite in the plasma and tissues of rodents and dogs following irinotecan administration.
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| Enzyme Assay |
No non-cellular binding assays are performed with RPR121056 for direct target engagement, as it is an inactive metabolite. For analytical purposes, standard solutions of RPR121056 (1-1000 ng/mL) are analyzed by reversed-phase high-performance liquid chromatography (RP-HPLC) with fluorescence detection (excitation 365 nm, emission 425 nm). A C18 column (e.g., 250 × 4.6 mm, 5 um particle size) is used with a mobile phase consisting of acetonitrile and 50 mM KH2PO4 buffer (pH 4.0) at a flow rate of 1.0 mL/min. The concentration is determined by comparing peak areas to a calibration curve prepared from authentic standard solutions.
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| Cell Assay |
RPR121056 is not used in cell-based assays for biological activity, as it is an inactive metabolite. However, for metabolite profiling studies, human cancer cells (e.g., HCT-116 colon cancer cells) are treated with irinotecan (10-100 uM, 24-48 hours). Following incubation, cell culture supernatants are collected, and intracellular contents are lysed. RPR121056 concentrations in the lysates and media are quantified by LC-MS/MS (electrospray ionization positive mode) using a deuterated internal standard (e.g., RPR121056-d3). The extraction is performed using solid-phase extraction (SPE) or protein precipitation with acetonitrile prior to LC-MS/MS analysis.
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| Animal Protocol |
Animal studies are not conducted with RPR121056 alone. In metabolite profiling studies in rodents or non-human primates, animals are administered irinotecan intravenously at doses of 10-50 mg/kg. Blood samples are collected at multiple time points (e.g., 0, 0.5, 1, 2, 4, 8, 12, 24 hours post-dose) into heparinized tubes containing a phosphatase inhibitor to stabilize the lactone ring. Plasma is separated by centrifugation, and RPR121056 is quantified by LC-MS/MS. The metabolite is also measured in urine and fecal homogenates to determine its excretory route. These studies confirm that RPR121056 is a major circulating metabolite.
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| ADME/Pharmacokinetics |
Metabolism / Metabolites
7-Ethyl-10-[4-N-(5-aminovaleric acid)-1-piperidinyl]carbonyloxycamptothecin is a known human metabolite of irinotecan. As a metabolite, RPR121056 is produced from irinotecan in humans with an elimination half-life of 10-20 hours. It is primarily excreted renally, and its concentration in plasma can exceed that of the parent drug and SN-38 due to its longer half-life. The metabolite does not undergo further significant metabolic conversion. The area under the plasma concentration-time curve (AUC) of RPR121056 increases proportionally with irinotecan dose. It is not known to be a substrate for P-glycoprotein (P-gp). Its plasma protein binding is low. No oral bioavailability data exist because it is not administered as a drug. |
| Toxicity/Toxicokinetics |
RPR121056 is not a drug and has no associated therapeutic toxicity. As an inactive metabolite of irinotecan, its formation represents a detoxification pathway. The safety profile of RPR121056 itself is not relevant to clinical use, as it is not administered to patients. If formed in large amounts, it does not contribute to the major clinical toxicities of irinotecan, which include severe diarrhea (mediated by SN-38) and myelosuppression. In preclinical models, the metabolite is not cytotoxic and has no observed genotoxic potential. It is considered safe for use as an analytical reference standard.
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| References | |
| Additional Infomation |
APC is a pyranoindoquinoline.
RPR121056 is a research-grade compound, specifically an analytical reference standard for studying the metabolism and disposition of the anticancer drug irinotecan (CPT-11). It is not a drug itself and has no clinical applications or approved therapeutic indications. It is available from chemical suppliers for research use only. Its detection and quantification in biological fluids (plasma, urine, feces) are essential for pharmacokinetic studies, drug-drug interaction assessments, and therapeutic drug monitoring of irinotecan therapy in cancer patients. The compound is also known as APC (aminopentane carboxylic acid) in the medical literature. |
| Molecular Formula |
C₃₃H₃₈N₄O₈
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|---|---|
| Molecular Weight |
618.67682
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| Exact Mass |
618.268
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| CAS # |
181467-56-1
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| PubChem CID |
10077584
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
953.5±65.0 °C at 760 mmHg
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| Flash Point |
530.5±34.3 °C
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| Vapour Pressure |
0.0±0.3 mmHg at 25°C
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| Index of Refraction |
1.679
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| LogP |
2.92
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
45
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| Complexity |
1260
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CCC1=C2CN3C(=CC4=C(C3=O)COC(=O)[C@@]4(CC)O)C2=NC5=C1C=C(C=C5)OC(=O)N6CCC(CC6)NCCCCC(=O)O
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| InChi Key |
BSVVZICJFYZDJJ-XIFFEERXSA-N
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| InChi Code |
InChI=1S/C33H38N4O8/c1-3-21-22-15-20(45-32(42)36-13-10-19(11-14-36)34-12-6-5-7-28(38)39)8-9-26(22)35-29-23(21)17-37-27(29)16-25-24(30(37)40)18-44-31(41)33(25,43)4-2/h8-9,15-16,19,34,43H,3-7,10-14,17-18H2,1-2H3,(H,38,39)/t33-/m0/s1
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| Chemical Name |
(S)-5-((1-(((4,11-diethyl-4-hydroxy-3,14-dioxo-3,4,12,14-tetrahydro-1H-pyrano[3',4'
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| Synonyms |
RPR121056 RPR-121056 RPR 121056 APC
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~200 mg/mL (~323.27 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6163 mL | 8.0817 mL | 16.1634 mL | |
| 5 mM | 0.3233 mL | 1.6163 mL | 3.2327 mL | |
| 10 mM | 0.1616 mL | 0.8082 mL | 1.6163 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
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