Oprozomib (ONX-0912)Proteasome inhibitor CAS# 935888-69-0 |
Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
| Cas No. | 935888-69-0 | SDF | Download SDF |
| PubChem ID | 25067547 | Appearance | Powder |
| Formula | C25H32N4O7S | M.Wt | 532.61 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | ONX-0912,ONX0912,ONX 0912,PR 047,Oprozomib | ||
| Solubility | DMSO : ≥ 50 mg/mL (93.88 mM) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | N-[(2S)-3-methoxy-1-[[(2S)-3-methoxy-1-[[(2S)-1-[(2R)-2-methyloxiran-2-yl]-1-oxo-3-phenylpropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]-2-methyl-1,3-thiazole-5-carboxamide | ||
| SMILES | CC1=NC=C(S1)C(=O)NC(COC)C(=O)NC(COC)C(=O)NC(CC2=CC=CC=C2)C(=O)C3(CO3)C | ||
| Standard InChIKey | SWZXEVABPLUDIO-WSZYKNRRSA-N | ||
| Standard InChI | InChI=1S/C25H32N4O7S/c1-15-26-11-20(37-15)24(33)29-19(13-35-4)23(32)28-18(12-34-3)22(31)27-17(21(30)25(2)14-36-25)10-16-8-6-5-7-9-16/h5-9,11,17-19H,10,12-14H2,1-4H3,(H,27,31)(H,28,32)(H,29,33)/t17-,18-,19-,25+/m0/s1 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Oprozomib (ONX 0912) is an orally bioavailable inhibitor for CT-L activity of 20S proteasome β5 and LMP7 with IC50 values of 36 nM and 82 nM, respectively. | |||||
| Targets | 20S proteasome β5 | 20S proteasome LMP7 | ||||
| IC50 | 36 nM | 82 nM | ||||
| Cell experiment: | |
| Cell lines | The human HNSCC cell lines UMSCC-22A, UMSCC-22B, 1483, UMSCC-1, and Cal33. |
| Preparation method | The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months. |
| Reacting condition | 48 h; IC50 values ranging from 58.9 to185.7 nmol/L in 8 different HNSCC cell lines. |
| Applications | In trypan blue exclusion assays, ONX 0912 exhibited IC50 values ranging from 58.9 to185.7 nmol/L in 8 different HNSCC cell lines. In the 4 HNSCC cell lines (UMSCC-1, UMSCC-22B, 1483, and UMSCC-1) examined, treatment ONX 0912 resulted in processing of caspase-3 to active subunits and cleavage of the caspase substrate PARP. |
| Animal experiment: | |
| Animal models | Athymic nude mice |
| Dosage form | 30 mg/kg; Oral taken. |
| Application | Using nude mice harboring HNSCC xenograft tumors, oral administration of 30 mg/kg ONX 0912 effectively inhibited CT-L activity in normal and HNSCC tumor tissues. Treatments (10 mg/kg and 30 mg/kg) were administered via oral gavage once a day on 2 consecutive days and repeated weekly for 2 weeks. Treatment with 10 mg/kg ONX 0912 did not have a significant effect on tumor growth, relative to treatment with vehicle alone. In contrast, highly significant inhibition of HNSCC tumor growth was seen with 30 mg/kg ONX 0912 (P = 0.003). These results show that consecutive-day treatment with orally administered ONX 0912, using a dose that has previously been shown to be well tolerated, leads to inhibition of HNSCC tumor growth. |
| Other notes | Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
| References: [1] Zang Y, Thomas S M, Chan E T, et al. Carfilzomib and ONX 0912 inhibit cell survival and tumor growth of head and neck cancer and their activities are enhanced by suppression of Mcl-1 or autophagy[J]. Clinical Cancer Research, 2012, 18(20): 5639-5649. | |
Oprozomib (ONX-0912) Dilution Calculator
Oprozomib (ONX-0912) Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 1.8775 mL | 9.3877 mL | 18.7755 mL | 37.5509 mL | 46.9387 mL |
| 5 mM | 0.3755 mL | 1.8775 mL | 3.7551 mL | 7.5102 mL | 9.3877 mL |
| 10 mM | 0.1878 mL | 0.9388 mL | 1.8775 mL | 3.7551 mL | 4.6939 mL |
| 50 mM | 0.0376 mL | 0.1878 mL | 0.3755 mL | 0.751 mL | 0.9388 mL |
| 100 mM | 0.0188 mL | 0.0939 mL | 0.1878 mL | 0.3755 mL | 0.4694 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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ONX-0912 (as known as oprozomib), discovered during a medicinal chemistry effort using tripeptide epoxyketones, is an orally bio-available and potent proteasome inhibitor that inhibits growth and induces apoptosis in bortezomib resistant multiple myeloma (MM) cells. Although ONX-0912, an analog of carfilzomib, is structurally distinct from bortezomib, it possesses the same ability as bortezomib to predominantly inhibit chymotrypsin-like activity of the proteasome. ONX-0912 exhibits significant anti-MM activities to reduce tumor progression and prolong survival in many animal tumor model studies, which are associated with activation of caspase-3, caspase-8, caspase-9, and poly(ADP) ribose polymerase and inhibition of anglogensis and MM cells migration.
Reference
Dharminder Chauhan, Ajita V. Singh, Monette Aujay, Christopher J. Kirk, Madhavi Bandi, Bryan Ciccarelli, Noopur Raje, Paul Richardson, and Kenneth C. Anderson. A novel oraaly active proteasome inhibitor ONX 0912 triggers in vitro and in vivo cytotoxicity in multiple myeloma. Blood 2010; 116(23): 4906-4915
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