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KP1019 124875-20-3

KP1019 124875-20-3

CAS No.: 124875-20-3

KP1019 (FFC14A) is a Ru(III)-based anti-metastatic and cytotoxic anti-cancer compound. KP1019 induces DNA damage and apo
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This product is for research use only, not for human use. We do not sell to patients.

KP1019 (FFC14A) is a Ru(III)-based anti-metastatic and cytotoxic anti-cancer compound. KP1019 induces DNA damage and apoptosis in cancer/tumor cells.

Physicochemical Properties


Molecular Formula C21H19CL4N6RU
Molecular Weight 598.29775929451
Exact Mass 596.947
CAS # 124875-20-3
Appearance Typically exists as solid at room temperature
LogP 7.446
SMILES

[Ru-2](Cl)(Cl)(Cl)Cl.N1=CC2C=CC=CC=2N1.N1=CC2C=CC=CC=2N1.N1C2C=CC=CC=2C=[NH+]1

HS Tariff Code 2934.99.9001
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)

Biological Activity


ln Vitro KP1019 is absorbed by yeast, causing mutations, a delay in the cell cycle, and cell death. found that rad1Δ, rev3Δ, and rad52Δ yeasts are highly sensitive to KP1019, indicating that recombination, translesion synthesis (TLS), and nucleotide excision repair (NER) all contribute to drug tolerance Function[1]. This study looked at the KP1019 sensitivity of DNA repair-deficient strains. KP1019 causes DNA damage and apoptosis in colon cancer cells and suppresses the growth of ovarian tumor cells. In mammalian cell lines, KP1019 induces several DNA adducts and interstrand cross-links [1].
ln Vivo In the MCa breast cancer model, KP1019 therapy reduces the growth of the main tumor. None of the therapies in this tumor model slowed the growth of pulmonary metastases [3].
Animal Protocol Animal/Disease Models: CBA female mice bearing mouse breast cancer [3]
Doses: 40 mg/kg and 80 mg/kg
Route of Administration: IP; 40 mg/kg on days 6 to 11 and 7, 9 and Results at 80 mg/kg for 11 days at two dose levels: Inhibition of primary tumor growth.
References

[1]. The anticancer ruthenium complex KP1019 induces DNA damage, leading to cell cycle delay and cell death in Saccharomyces cerevisiae. Mol Pharmacol. 2013 Jan;83(1):225-34.

[2]. Comparison of KP1019 and NAMI-A in tumour-mimetic environments. Metallomics. 2016 Aug 1;8(8):762-73.

[3]. Inhibitory Effects of the Ruthenium Complex KP1019 in Models of Mammary Cancer Cell Migration and Invasion. Met Based Drugs. 2009;2009:681270.


Solubility Data


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
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
(e.g. IP/IV/IM/SC)
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution 50 μL Tween 80 850 μL Saline)
*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).
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)]
*Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO 100 μLPEG300 200 μL castor oil 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10: 10 : 80 (i.e. 100 μL Ethanol 100 μL Cremophor 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300:Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH 400 μLPEG300 50 μL Tween 80 450 μL 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).
Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 1.6714 mL 8.3570 mL 16.7140 mL
5 mM 0.3343 mL 1.6714 mL 3.3428 mL
10 mM 0.1671 mL 0.8357 mL 1.6714 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.