BOLD-100 (Synonyms: NKP-1339; IT-139; KP-1339)

Cat. No.: HY-16350 Purity: 98.14%: FAQs
Data Sheet SDS COA Handling Instructions

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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.

For research use only. We do not sell to patients.

BOLD-100 Chemical Structure

CAS No. : 197723-00-5

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent
10 mM * 1 mL in DMSO ready for reconstitution	USD 209	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 209	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 190	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 285	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 770	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1155	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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This product is a controlled substance and not for sale in your territory.

Other Forms of BOLD-100:

BOLD-100 free base Get quote

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Biological Activity
Purity & Documentation
References
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Description

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.

Clinical Trial

Molecular Weight

502.14

Formula

C₁₄H₁₂Cl₄N₄NaRu

CAS No.

197723-00-5

Appearance

Solid

Color

Light brown to khaki

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

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

Solvent & Solubility

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.

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* 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.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 98.14%

Select Batch:

Data Sheet (282 KB) SDS (393 KB)

COA (258 KB) RP-HPLC (214 KB)

Handling Instructions (2659 KB)

References

[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]

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 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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