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NKP-1339 (IT139; KP1339) is the first-in-class and potent ruthenium-based anticancer drug under clinical investigation for treating solid cancer with limited side effects. NKP-1339 causes the mitochondrial pathway to trigger apoptosis, stop DNA synthesis, and induce G2/M cell cycle arrest. Strongly binding to serum proteins like albumin and transferrin, NKP-1339 has a high potential for targeting tumors and activates in the reductive tumor milieu.
| ln Vitro |
BOLD-100 (0-200 μM; 72 hours) demonstrates IC50 values of 45-200?μM for KP1339 monotherapy and has anticancer activity against malignant cell lines of various origin. With mean IC50 values of 186.3 μM, 165.4 μM, 124.4 μM, and 69.4 μM against Hepatoma cell line, Hep3B, HepG2, PLC/PRF/5, and HCC2 cells, respectively. Its IC50 values are 178 μM, 111 μM, and 143 μM for the Melanoma cell line, VM-1, VM-21, and VM-48, respectively. It suppresses A549, VL-8, SW480, and HCT116 cells, respectively, against lung cancer and colon cancer cell lines[2].
BOLD-100 (0-150 μM; 24 hours) induces apoptosis only in cells. It increases the quantity of apoptotic cells when combined with sorafenib. Furthermore, either caspase 7 cleavage or p-PARP cleavage is promoted[2]. BOLD-100 (0-150 μM; 24 hours) can increase CREB expression and STAT3 phosphorylation, but sorafenib cotreatment prevents the decline[2]. |
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| ln Vivo |
BOLD-100 (intravenous injection; 30 mg/kg; once a week; 42sdays) in combination with the multi-kinase inhibitor sorafenib shows additional anticancer activity compared to BOLD-100 treatment alone in Hep3B xenografts grown in Balb/c SCID mice [2].
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| Cell Assay |
Cell Line: Hepatoma, Melanoma, Lung cancer and Colon cancer cell lines
Concentration: 0 μM, 50 μM, 100 μM, 150 μM and 200 μM Incubation Time: 72 hours Result: Has anti-cancer activity in diverse malignant tumour cell types. |
| Animal Protocol |
Hep3B xenograft in Balb/c mice
30 mg/kg Intravenous injection |
| References |
| Molecular Formula |
C₁₄H₁₂CL₄N₄NARU
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|---|---|
| Molecular Weight |
502.14
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| Elemental Analysis |
C, 33.49 H, 2.41 Cl, 28.24 N, 11.16 Na,4.58 Ru, 20.13
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| CAS # |
197723-00-5
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| Related CAS # |
BOLD-100 free base;783324-98-1
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| Appearance |
Solid powder
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| SMILES |
[Cl-][Ru+3]([N]1=CC2=CC=CC=C2N1)([Cl-])([Cl-])([N]3=CC4=CC=CC=C4N3)[Cl-].[Na+]
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| InChi Key |
WVVOCRYXBTVDRN-UHFFFAOYSA-J
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| InChi Code |
WVVOCRYXBTVDRN-UHFFFAOYSA-J
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| Chemical Name |
Sodium hydride; tetrachloro-bis(1H-indazol-2-yl)ruthenium
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| Synonyms |
NKP1339; IT-139; KP-1339; KP-1339; NKP 1339; KP 1339; IT 139; IT139; KP1339; Na[trans-RuCl4(Ind)2; sodium trans-[RuCl4(HInd)2,
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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: ≥ 59 mg/mL (~117.5 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 | 1.9915 mL | 9.9574 mL | 19.9148 mL | |
| 5 mM | 0.3983 mL | 1.9915 mL | 3.9830 mL | |
| 10 mM | 0.1991 mL | 0.9957 mL | 1.9915 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT01415297 | Completed | Drug: NKP-1339 | Solid Tumors | Niiki Pharma Inc. | October 2009 | Phase 1 |
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