Art. -Nr.: HY-16350

BOLD-100

(Synonyms: NKP-1339; IT-139; KP-1339)

1 Cited Publications

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Based on 1 publication(s) in Google Scholar

BOLD-100 (NKP-1339; IT-139) is the first-in-class ruthenium-based anticancer agent in development against solid cancer with limited side effects. BOLD-100 induces G2/M cell cycle arrest, blockage of DNA synthesis, and induction of apoptosis via the mitochondrial pathway. BOLD-100 has a high tumor targeting potential, strongly binds to serum proteins such as albumin and transferrin and activates in the reductive tumor milieu.

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Reinheit: 95.20%
CAS. Nr.: 197723-00-5
Formel: C₁₄H₁₂Cl₄N₄NaRu
Molecular Weight:502.14

Speicherung:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

BOLD-100 Chemical Structure

CAS. Nr.: 197723-00-5

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle DNA/RNA Synthesis Isoform-spezifische Produkte anzeigen :

In Vitro

BOLD-100 (0-200 μM; 72 hours) has the anticancer activity against malignant cell lines of diverse origin, exhibits IC₅₀ values of 45-200 μM for KP1339 mono-therapy. It against Hepatoma cell line, Hep3B, HepG2, PLC/PRF/5 and HCC2 cells with the Mean IC₅₀ value of 186.3 μM, 165.4 μM, 124.4 μM, and 69.4 μM, respectively. It against Melanoma cell line, VM-1, VM-21,VM-48 with IC₅₀ values of 178 μM, 111 μM, and 143 μM, respectively. It against Lung cancer and Colon cancer cell lines, inhibits A549, VL-8, SW480 and HCT116 cells, respectively^[2].
BOLD-100 (0-150 μM; 24 hours) induces cell apoptosis alone. When it combines with sorafenib, it increases the numbers of the apopotic cells. Additionally, the p-PARP and caspase 7 cleavage is promoted either^[2].
BOLD-100 (0-150 μM; 24 hours) can promote phosphorylation of STAT3 and CREB expression, however, the decreasation is inhibited by sorafenib cotreatment^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[2]

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.

Apoptosis Analysis^[2]

Cell Line:

Hep3B cells
Concentration:

0 μM, 75 μM, 150 μM
Incubation Time:

72 hours
Result:

Promoted cell apoptosis as a concentration manner.

Western Blot Analysis^[2]

Cell Line:

Hep3B cells
Concentration:

0 μM, 75 μM, 150 μM
Incubation Time:

72 hours
Result:

Increased p-STAT3 and p-CREB expression in cells without sorafenib cotreatment.

In Vivo

BOLD-100 (intravenous injection; 30 mg/kg; once a week; 42sdays) combines with the multi-kinase inhibitor sorafenib and exhibits a further anticancer activity when compares to the BOLD-100 treatment alone in Hep3B xenografts grown in Balb/c SCID mice ^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Hep3B xenograft in Balb/c mice^[2]
Dosage:

30 mg/kg
Administration:

Intravenous injection
Result:

Had synergistic activity of KP1339 with sorafenib in vivo.

Chemical Information

CAS. Nr. 197723-00-5
Appearance Solid
Molecular Weight 502.14
Formel C₁₄H₁₂Cl₄N₄NaRu
Color Brown to dark brown
SMILES

[Cl-][Ru+3]([Cl-])([Cl-])([N]1=CC2=C(N1)C=CC=C2)([N]3=CC4=C(N3)C=CC=C4)[Cl-].[Na+]
Synonyms

NKP-1339; IT-139; KP-1339
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Publications (1)

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Journal Impact Factor

Biomater Res

Ultrasound-Targeted Nanobubbles Codelivering NKP-1339 and miR-142-5p for Synergistic Mitochondrial Immunogenic Cell Death and PD-L1 Inhibition in Cancer Therapy. [Abstract]

2025 Aug 8:29:0232. PMID: 40785846

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 59 mg/mL (117.50 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (285 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Robert Trondl, et al. NKP-1339, the first ruthenium-based anticancer drug on the edge to clinical application. Chemical Science. Chemical Science

[2]. Heffeter P, et al. The ruthenium compound KP1339 potentiates the anticancer activity of sorafenib in vitro and in vivo. Eur J Cancer. 2013 Oct;49(15):3366-75. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.9915 mL	9.9574 mL	19.9148 mL	49.7869 mL
	5 mM	0.3983 mL	1.9915 mL	3.9830 mL	9.9574 mL
	10 mM	0.1991 mL	0.9957 mL	1.9915 mL	4.9787 mL
	15 mM	0.1328 mL	0.6638 mL	1.3277 mL	3.3191 mL
	20 mM	0.0996 mL	0.4979 mL	0.9957 mL	2.4893 mL
	25 mM	0.0797 mL	0.3983 mL	0.7966 mL	1.9915 mL
	30 mM	0.0664 mL	0.3319 mL	0.6638 mL	1.6596 mL
	40 mM	0.0498 mL	0.2489 mL	0.4979 mL	1.2447 mL
	50 mM	0.0398 mL	0.1991 mL	0.3983 mL	0.9957 mL
	60 mM	0.0332 mL	0.1660 mL	0.3319 mL	0.8298 mL
	80 mM	0.0249 mL	0.1245 mL	0.2489 mL	0.6223 mL
	100 mM	0.0199 mL	0.0996 mL	0.1991 mL	0.4979 mL

BOLD-100

1 Cited Publications

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BOLD-100

Anti-Lung Cancer Compound Library

Cell Death Library

Bioactive Compound Library Max

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Publications Citing Use of MedChemExpress (MCE) BOLD-100

Alle DNA/RNA Synthesis Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

BOLD-100

Anti-Lung Cancer Compound Library

Cell Death Library

Bioactive Compound Library Max

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Publications Citing Use of MedChemExpress (MCE) BOLD-100

Alle DNA/RNA Synthesis Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

BOLD-100 Related Classifications

HY-16350 Related Classifications