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| 25mg |
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| 50mg |
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Purity: ≥98%
VR23 (VR-23; VR 23) is a highly potent and selective inhibitor of trypsin-like proteasome with potential antitumor activity. Its IC50 values are 1 nM, 50-100 nM, and 3 μM for trypsin-like, chymotrypsin-like, and caspase-like proteasomes, respectively. With MDA-MB-231 or RPMI 8226 cancer cells engrafted, VR23 shows remarkable in vivo antitumor efficacy in ATH490 athymic mice.
| Targets |
trypsin-like proteasome (IC50 = 1 nM); chymotrypsin-like proteasome (IC50 = 50-100 nM); caspase-like proteasome (IC50 = 3 μM)
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| ln Vitro |
VR23 is a novel type of proteasome inhibitor that specifically targets the β2 subunit of the 20S proteasome. Several myeloma cells, including those resistant to PS-341, are killed by VR23 in a synergistic manner. VR23 is a structurally unique inhibitor of proteasomes that has promising anti-cancer properties.
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| ln Vivo |
VR23 demonstrates potent antiangiogenic and antitumor properties in mice.
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| Enzyme Assay |
On a 96-well clustered plate, exponentially growing cells are either treated with various drug concentrations or left untreated (control) for a duration of 6 hours. Proteasomes that have been extracted using 0.5% NP40 buffer are combined with equal volumes of samples to create a 100 μL total volume. These are then placed in black-bottom 96-well plates at 37°C and incubated with 25 μmol/L of fluorogenic substrates (LRR-specific for trypsin-like activity, LLE-specific for caspase-like activity, and SUVY-specific for chymotrypsin-like activity). Every five minutes, the wavelengths of 360 nm (excitation) and 480 nm (emission) are used to measure fluorescence.
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| Cell Assay |
There are assays for SRB and clonogenic drugs conducted. With Graph Pad Prism V 4.02, IC50 values are computed using a sigmoidal dose-response curve (variable slope).
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| Animal Protocol |
ATH490 athymic mice engrafted with MDA-MB-231 or RPMI 8226 cancer cells
30mg/kg i.p. |
| References |
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| Molecular Formula |
C19H16CLN5O6S
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|---|---|---|
| Molecular Weight |
477.88
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| Exact Mass |
477.05
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| Elemental Analysis |
C, 47.75; H, 3.37; Cl, 7.42; N, 14.66; O, 20.09; S, 6.71
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| CAS # |
1624602-30-7
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| Related CAS # |
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| PubChem CID |
73442847
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| Appearance |
Yellow solid powder
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| Density |
1.6±0.1 g/cm3
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| Boiling Point |
699.3±65.0 °C at 760 mmHg
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| Flash Point |
376.7±34.3 °C
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| Vapour Pressure |
0.0±2.2 mmHg at 25°C
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| Index of Refraction |
1.697
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| LogP |
3.49
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
32
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| Complexity |
807
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| Defined Atom Stereocenter Count |
0
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| SMILES |
ClC1C([H])=C([H])C2C(C=1[H])=NC([H])=C([H])C=2N1C([H])([H])C([H])([H])N(C([H])([H])C1([H])[H])S(C1C([H])=C([H])C(=C([H])C=1[N+](=O)[O-])[N+](=O)[O-])(=O)=O
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| InChi Key |
PDQVZPPIHADUOO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H16ClN5O6S/c20-13-1-3-15-16(11-13)21-6-5-17(15)22-7-9-23(10-8-22)32(30,31)19-4-2-14(24(26)27)12-18(19)25(28)29/h1-6,11-12H,7-10H2
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| Chemical Name |
7-chloro-4-[4-(2,4-dinitrophenyl)sulfonylpiperazin-1-yl]quinoline
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0926 mL | 10.4629 mL | 20.9258 mL | |
| 5 mM | 0.4185 mL | 2.0926 mL | 4.1852 mL | |
| 10 mM | 0.2093 mL | 1.0463 mL | 2.0926 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.
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