| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| ln Vitro |
RA190 covalently binds to cysteine 88 of the ubiquitin receptor RPN13 in 19S regulatory granules, inhibits proteasome action, and induces the fast accumulation of polyubiquitinated proteins. Multiple myeloma (MM) lines, especially those resistant to bortezomib, are sensitive to RA190 through endoplasmic reticulum stress-associated apoptosis. RA190 stabilizes the target of the human papillomavirus (HPV) E6 oncoprotein and preferentially kills HPV-transformed cells [1].
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| ln Vivo |
RA190 inhibits the activity of proteasomes in skin and muscle and is distributed to plasma and major organs, excluding the brain. Multiple myeloma and ovarian cancer xenografts grow much slower when RA190 is administered, and oral RA190 treatment slows the growth of tumors in HPV16+ syngeneic mice without altering the spontaneous responses of HPV-specific CD8+ T cells [1].
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| References |
| Molecular Formula |
C28H23CL5N2O2
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|---|---|
| Molecular Weight |
596.7594
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| Exact Mass |
596.017
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| CAS # |
1617495-03-0
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| Related CAS # |
1617572-02-7;1617495-03-0 (HCl);
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| PubChem CID |
126843229
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| Appearance |
Light yellow to yellow solid powder
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
37
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| Complexity |
809
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| Defined Atom Stereocenter Count |
1
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| SMILES |
ClC1=C(C([H])=C([H])C(=C1[H])/C(/[H])=C1\C(/C(=C(/[H])\C2C([H])=C([H])C(=C(C=2[H])Cl)Cl)/C([H])([H])N(C([C@]([H])(C([H])([H])C2C([H])=C([H])C([H])=C([H])C=2[H])N([H])[H])=O)C\1([H])[H])=O)Cl.Cl[H]
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| InChi Key |
UMWXLEVUBFNYIK-VCCJZKHWSA-N
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| InChi Code |
InChI=1S/C28H22Cl4N2O2.ClH/c29-22-8-6-18(12-24(22)31)10-20-15-34(28(36)26(33)14-17-4-2-1-3-5-17)16-21(27(20)35)11-19-7-9-23(30)25(32)13-19;/h1-13,26H,14-16,33H2;1H/b20-10-,21-11-;/t26-;/m0./s1
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| Chemical Name |
(3Z,5Z)-1-[(2S)-2-amino-3-phenylpropanoyl]-3,5-bis[(3,4-dichlorophenyl)methylidene]piperidin-4-one;hydrochloride
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
DMSO : ≥ 100 mg/mL (~167.57 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.38 mg/mL (3.99 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 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 23.8 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6757 mL | 8.3786 mL | 16.7572 mL | |
| 5 mM | 0.3351 mL | 1.6757 mL | 3.3514 mL | |
| 10 mM | 0.1676 mL | 0.8379 mL | 1.6757 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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