1. Cell Cycle/DNA Damage
    Apoptosis
  2. DNA/RNA Synthesis
    Apoptosis
  3. NKP-1339

NKP-1339 (Synonyms: IT-139; KP-1339)

Cat. No.: HY-16350 Purity: 95.92%
Handling Instructions

NKP-1339 (IT-139; KP-1339) is the first-in-class ruthenium-based anticancer agent in development against solid cancer with limited side effects. NKP-1339 induces G2/M cell cycle arrest, blockage of DNA synthesis, and induction of apoptosis via the mitochondrial pathway. NKP-1339 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.

NKP-1339 Chemical Structure

NKP-1339 Chemical Structure

CAS No. : 197723-00-5

Size Price Stock Quantity
10 mM * 1  mL in DMSO USD 464 In-stock
Estimated Time of Arrival: December 31
5 mg USD 420 In-stock
Estimated Time of Arrival: December 31
10 mg USD 600 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1800 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2520 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

NKP-1339 (IT-139; KP-1339) is the first-in-class ruthenium-based anticancer agent in development against solid cancer with limited side effects. NKP-1339 induces G2/M cell cycle arrest, blockage of DNA synthesis, and induction of apoptosis via the mitochondrial pathway. NKP-1339 has a high tumor targeting potential, strongly binds to serum proteins such as albumin and transferrin and activates in the reductive tumor milieu[1].

IC50 & Target

Apoptosis[1]

In Vitro

NKP-1339 (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].
NKP-1339 (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].
NKP-1339 (0-150 μM; 24 hours) can promote phosphorylation of STAT3 and CREB expression, however, the decreasation is inhibited by sorafenib cotreatment[2].

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

NKP-1339 (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 NKP-1339 treatment alone in Hep3B xenografts grown in Balb/c SCID mice [2].

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

SMILES

[Cl-][Ru+3]([N]1=CC2=CC=CC=C2N1)([Cl-])([Cl-])([N]3=CC4=CC=CC=C4N3)[Cl-].[Na+]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 59 mg/mL (117.50 mM)

*"≥" 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
*Please refer to the solubility information to select the appropriate solvent.
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

NKP-1339IT-139KP-1339NKP1339NKP 1339IT139IT 139KP1339KP 1339DNA/RNA SynthesisApoptosisapoptosis?Hep3B ColoncancermalignanttumorHepatomaMelanomaInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number *

 

Organization name *

Country or Region *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product name:
NKP-1339
Cat. No.:
HY-16350
Quantity:
MCE Japan Authorized Agent: