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| 1mg |
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| 5mg |
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| 10mg |
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| 25mg |
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| Targets |
The compound targets several cellular pathways. It is an inhibitor of stress-induced GRP78 (glucose-regulated protein 78) upregulation, a key ER chaperone. By disrupting ER homeostasis, BOLD-100 induces ER stress and the unfolded protein response (UPR). It also affects lysosome function and autophagy. The ruthenium metal center is thought to be activated in the reducing tumor environment to form a bioactive species.
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| ln Vitro |
In pre-clinical studies, BOLD-100 has been shown to have broad anti-tumor activity against various cancer cell lines, including those resistant to conventional chemotherapies. By disrupting ER homeostasis and inducing a lethal unfolded protein response (UPR), it leads to cancer cell death via apoptosis and necrosis. It is not cross-resistant with platinum-based drugs, as it has a different mechanism of action.
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| ln Vivo |
BOLD-100 has high tumor targeting potential and is in clinical development for the treatment of advanced solid tumors. Phase I and II clinical trials have demonstrated that BOLD-100 is well-tolerated and shows promising signs of anti-tumor activity, particularly in patients with colorectal, pancreatic, and biliary tract cancers. A specific animal protocol is not detailed, but the compound strongly binds to serum proteins and is activated in the reducing tumor environment.
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| Enzyme Assay |
BOLD-100 is not an enzyme inhibitor in the traditional sense. Its mechanism is studied by assessing its effects on cellular processes. For example, the ability to induce ER stress is measured by treating cancer cells with the compound and then analyzing the levels of ER stress marker proteins (e.g., CHOP, GRP78, XBP-1 splicing) by Western blot or qPCR. Its ruthenium-based activation is studied via mass spectrometry after incubation with proteins like albumin and transferrin.
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| Cell Assay |
Cellular assays are performed to evaluate the anti-cancer activity of BOLD-100. A panel of human cancer cell lines (e.g., A2780 ovarian, HCT116 colon, MIA PaCa-2 pancreatic) are seeded in 96-well plates and treated with varying concentrations of BOLD-100 for 72 hours. Cell viability is assessed using a standard MTT or CellTiter-Glo assay to calculate IC50 values. The effect on the cell cycle is analyzed by propidium iodide staining and flow cytometry.
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| Animal Protocol |
The in vivo anti-tumor activity of BOLD-100 is evaluated in mouse xenograft models. In a typical protocol, female athymic nude mice are injected subcutaneously with human cancer cells (e.g., MIA PaCa-2 or HCT116). When tumors reach a certain size (e.g., 100-150 mm3), the mice are randomized to receive BOLD-100 intravenously, often via tail vein injection (e.g., 30 mg/kg, once weekly for 2-3 weeks). Tumor volume is measured by calipers. The compound is known to strongly bind to serum proteins, which may contribute to its pharmacokinetic profile.
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| ADME/Pharmacokinetics |
BOLD-100 has a favorable pharmacokinetic profile due to its high binding affinity for serum proteins like albumin and transferrin. This binding serves as a natural carrier, allowing the drug to accumulate in the tumor microenvironment via the enhanced permeability and retention (EPR) effect. The ruthenium center is inert in the blood stream but is activated by reduction in the hypoxic tumor environment. This activation mechanism contributes to its tumor-selective toxicity.
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| Toxicity/Toxicokinetics |
In Phase I clinical trials, BOLD-100 has been shown to be well-tolerated with a manageable side effect profile, which is a significant advantage over traditional platinum-based chemotherapies. Its primary toxicities appear to be hematological and dose-limiting. Detailed pre-clinical toxicology data are not provided here, but the clinical tolerability indicates an acceptable safety profile for an anticancer agent.
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| References | |
| Additional Infomation |
BOLD-100 is a novel, clinical-stage ruthenium-based anticancer drug candidate. It represents a promising alternative to platinum-based chemotherapeutics, with a distinct mechanism of action and a potentially better tolerability profile. As of the latest updates, BOLD-100 is an investigational drug that has completed Phase I/II clinical trials. It has not yet received regulatory approval for sale and continues to be evaluated for the treatment of solid tumors.
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| CAS # |
783324-98-1
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| Related CAS # |
BOLD-100;197723-00-5
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| Appearance |
Light brown to khaki solid powder
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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.) |
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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