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| ln Vitro |
RSC-1255 (249C) (1 μM; 1 h) inhibited V-ATPase-mediated proton pump function and lysosomal acidification in HEK293T cells [1]. RSC-1255 (1 μM; 1 h) altered V-ATPase assembly and increased membrane-associated V1 subunit levels in HEK293T cells [1]. RSC-1255 exhibited potent cell growth inhibitory activity in human cancer cell lines, with IC50 values of 0.073 μM for A549 (KRAS mutation), 0.06 μM for LOX IMVI (BRAFV600E), and 0.022 μM for MelJuso (HRASG13D/NRASQ61L) [1]. RSC-1255 (0–10 μM; 72 h) selectively reduced cell viability in KRAS mutant MEFs, with KRASG13D and KRASG12V cells being the most sensitive [1]. RSC-1255 (1 μM; 2, 4, 8, 20, 24 h) blocked autophagy flux in A549 cells and increased SQSTM1/p62 and LC3-II levels in a time-dependent manner [1]. RSC-1255 (1 μM; 1 h) increased the lysosomal pH of KRASG13D MEFs, reversing their highly acidic basal state [1]. RSC-1255 (1 μM; 1 h) inhibited V-ATPase-dependent proton transport in FITC-loaded lysosomes, with the most significant inhibition observed in KRASG13D MEFs [1]. RSC-1255 (1 μM; 24 h) increased the size of autophagic vesicles and blocked lysosome-autophagosome fusion in KRASG13D, KRASG12V and BRAFV600E MEFs[1]. RSC-1255 (1 μM; 2 h) significantly reduced macropinocytosis in MEFs, with the strongest inhibitory effect in KRASG13D cells[1]. RSC-1255 (1 μM; 24 h) induced apoptosis in KRAS mutant MEFs, with the highest Annexin V⁺/PI⁺ levels in KRASG13D, KRASG12V and BRAFV600E cells[1].
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| ln Vivo |
RSC-1255 (249 C) (10 mg/kg; intraperitoneal injection (ip); once or twice daily) significantly inhibited tumor growth in xenograft models of KRAS-mutant lung and colorectal cancer [1].
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: HEK293T cells Tested Concentrations: 1 μM Incubation Duration: 1h Experimental Results: Increased membrane-associated V1 subunit B2 was observed, indicating altered V-ATPase assembly after treatment. Western Blot Analysis[1] Cell Types: A549 cells Tested Concentrations: 1 μM Incubation Duration: 2 , 4 , 8 , 20 , 24 h Experimental Results: Time-dependent accumulation of SQSTM1/p62 and LC3-II, indicating autophagic flux inhibition. Cell Viability Assay[1] Cell Types: MEF KRAS mutants (KRASG13D, KRASG12V, KRASG12D, KRASG12S, KRASG12C, KRASQ61L, KRASQ61R, WT) Tested Concentrations: 0-10 μM Incubation Duration: 72 h Experimental Results: Highest sensitivity in KRASG13D and KRASG12V MEFs with the lowest IC50 values; minimal sensitivity in WT MEFs. Apoptosis Analysis[1] Cell Types: MEFs expressing KRASG13D, KRASG12V, BRAFV600E and other KRAS mutants Tested Concentrations: 1 μM Incubation Duration: 24h Experimental Results: Increased of Annexin V+/PI+ apoptotic cells, with KRASG13D,KRASG12V and BRAFV600E MEFs showing the strongest apoptotic responses. |
| Animal Protocol |
Animal/Disease Models: A549 (KRASG12S) lung cancer xenografts were established in five-week-old athymic mice.
Doses: 10 mg/kg Route of Administration: Intraperitoneal injection (i.p.); twice daily Experimental Results: Significantly reduced tumor volumes in A549 xenograft-bearing mice during the treatment period. Increased LC3-I/II levels in tumor tissues, indicating autophagy inhibition in vivo. No significant systemic toxicity, with normal body weight, organ weights and hematological parameters. Animal/Disease Models: SW48 xenograft models bearing parental or KRAS-mutant SW48 cells (KRASG12D/+, KRASG12V/+, KRASG13D/+) were established in five-six-week-old athymic mice]. Doses: 10 mg/kg Route of Administration: Intraperitoneal injection (i.p.); 2 weeks. Experimental Results: Significant tumor growth inhibition in KRAS-mutant SW48 xenografts, with the strongest effects in KRASG13D/+ and KRASG12V+ tumors. Minimal response in parental SW48 tumors, consistent with lower in vitro sensitivity. No significant changes in body weight or systemic toxicity during treatment. |
| References |
| Molecular Formula |
C27H25CLF4N4O3
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|---|---|
| Molecular Weight |
564.96
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| CAS # |
2171015-78-2
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| Appearance |
Typically exists as solids at room temperature
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 1.7700 mL | 8.8502 mL | 17.7004 mL | |
| 5 mM | 0.3540 mL | 1.7700 mL | 3.5401 mL | |
| 10 mM | 0.1770 mL | 0.8850 mL | 1.7700 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.
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