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NSC139021 (Synonyms: ERGi-USU)

Cat. No.: HY-112158 Purity: 99.62%
Handling Instructions

NSC139021 (ERGi-USU) is a highly selective inhibitor for the growth of ERG-positive cancer cells with IC50s ranging from 30 to 400 nM.

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

NSC139021 Chemical Structure

NSC139021 Chemical Structure

CAS No. : 1147-56-4

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 55 In-stock
Estimated Time of Arrival: December 31
100 mg USD 50 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Description

NSC139021 (ERGi-USU) is a highly selective inhibitor for the growth of ERG-positive cancer cells with IC50s ranging from 30 to 400 nM.

IC50 & Target

IC50: 30 to 400 nM (ERG-positive cancer cells)[1]

In Vitro

NSC139021 selectively inhibits growth of ERGpositive cancer cell lines with minimal effect on normal prostate or endothelial cells or ERG-negative tumor cell lines. The IC50 of NSC139021 for cell growth inhibition of responsive cell lines range between 30 nM to 400 nM. Combination of NSC139021 with enzalutamide shows additive effects in inhibiting growth of VCaP cells. A screen of kinases reveal that NSC139021 directly bound the ribosomal biogenesis regulator atypical kinase RIOK2 and induces ribosomal stress signature[1].

In Vivo

NSC139021 treatment inhibits growth of ERG-positive VCaP tumor xenografts with no apparent toxicity. Significant (P<0.05, P<0.005) inhibition of tumor growth is noted at day 26 in treatment groups indicating 44% (100 mg/kg) and 65% (150 mg/kg) reduction of tumor burden. At 100 mg/kg and 150 mg/kg, no apparent toxicity including weight loss, lethargy, diarrhea, loss of appetite, respiratory distress, or overall drug related toxicity is observed. [1].

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 : ≥ 62 mg/mL (242.85 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.9170 mL 19.5848 mL 39.1696 mL
5 mM 0.7834 mL 3.9170 mL 7.8339 mL
10 mM 0.3917 mL 1.9585 mL 3.9170 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (9.79 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (9.79 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[1]

To assess cell growth, To evaluate the ERG selectivity of the NSC139021, a panel of the following cell lines are assessed: ERG positive tumor cell lines (prostate cancer: VCaP; colon cancer: COLO320; leukemia: KG-1, MOLT-4; ERG negative prostate cancer cell lines (LNCaP, LAPC4, MDA PCa2b); normal prostate epithelium derived cell lines (BPH-1, RWPE-1); and primary endothelium derived cells (HUVEC). Monolayer of adherent cells are grown in their respective medium for 48 h followed by treatment with indicated dosage and time for the small molecule inhibitor NSC139021. Medium is replaced every 24 h containing the same concentration of the small molecule compound. Cells are counted by using trypan blue exclusion method. Cell morphology is documented by photography in all indicated time points. IC50 is calculated using GraphPad Prism 6 software[1].

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

Animal Administration
[1]

Mice[1]

The VCaP prostate cancer cells are injected into lower right dorsal flank of the male athymic nude mice (6-8 weeks old and weighing 27 to 30g). when tumors are palpable, mice are randomly separated into 2 experimental groups and into one control group of 6 mice in each group. In the treatment groups mice are injected intraperitoneally (I.P) with 100 mg/kg of NSC139021 or 150 mg/kg of NSC139021 while the control group are injected with vehicle (1:1[v/v], DMSO/PEG300) only. Growth in tumor volume is recorded weekly by using digital calipers and tumor volumes are calculated[1].

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

References
Molecular Weight

255.30

Formula

C₁₃H₉N₃OS

CAS No.

1147-56-4

SMILES

OC1=C(/N=N/C2=NC=CS2)C3=CC=CC=C3C=C1

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
NSC139021
Cat. No.:
HY-112158
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NSC139021

Cat. No.: HY-112158