| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| 1g |
|
||
| 2g |
|
||
| 5g |
|
||
| 10g |
|
||
| Other Sizes |
|
Purity: ≥98%
NSC139021 (also known as ERGi-USU) is a novel, potent and highly selective inhibitor for the growth of ERG-positive cancer cells with IC50s ranging from 30 to 400 nM.
| ln Vitro |
NSC139021 mostly suppresses the proliferation of ERG-positive cancer cell lines while having no effect on ERG-negative tumor cell lines, normal prostate cells, or endothelial cells. For sensitive cell lines, NSC139021's IC50 for inhibiting cell growth ranged from 30 nM to 400 nM. When combined, NSC139021 and enzalutamide had additive effects on the development of VCaP cells. NSC139021 directly binds the atypical kinase RIOK2, which regulates ribosome biogenesis, and causes ribosomal stress signals, according to kinase screening [1].
|
|---|---|
| ln Vivo |
Treatment with NSC139021 prevented ERG-positive VCaP tumor xenografts from growing without showing any signs of harm. Tumor growth was considerably (P<0.05, P<0.005) suppressed in the treatment groups on day 26, which corresponded to a 44% (100 mg/kg) and 65% (150 mg/kg) decrease in tumor burden. At the 100 mg/kg and 150 mg/kg dosages, no notable toxicities were noted, such as weight loss, somnolence, diarrhea, lack of appetite, respiratory distress, or overall drug-related toxicity. [1].
|
| References |
| Molecular Formula |
C13H9N3OS
|
|---|---|
| Molecular Weight |
255.2951
|
| Exact Mass |
255.047
|
| CAS # |
1147-56-4
|
| PubChem CID |
93572
|
| Appearance |
Pink to red solid powder
|
| Density |
1.4g/cm3
|
| Boiling Point |
523.251ºC at 760 mmHg
|
| Melting Point |
138-139 °C
|
| Flash Point |
270.253ºC
|
| Vapour Pressure |
0mmHg at 25°C
|
| Index of Refraction |
1.728
|
| LogP |
4.417
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
18
|
| Complexity |
313
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
S1C([H])=C([H])N=C1/N=N/C1=C(C([H])=C([H])C2=C([H])C([H])=C([H])C([H])=C21)O[H]
|
| InChi Key |
IOMXCGDXEUDZAK-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C13H9N3OS/c17-11-6-5-9-3-1-2-4-10(9)12(11)15-16-13-14-7-8-18-13/h1-8,17H
|
| Chemical Name |
1-(1,3-thiazol-2-yldiazenyl)naphthalen-2-ol
|
| Synonyms |
NSC-139021; ERGi-USU; NSC 139021; ERGi USU; NSC139021; ERGiUSU;
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ≥ 62 mg/mL (~242.85 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.79 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (9.79 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA