| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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R59022 (R-59022; DKGI-I) is a novel and potent DGKalpha inhibitor and serotonin receptor antagonist. It inhibits diacylglycerol kinase with IC50 of 2.8 μM.
| ln Vitro |
59-022 (1 minute, 10 μM) strengthens the aggregation [2]. R 59-022 (30 uM, 0–60 minutes) causes basophils to release more normetins [3]. In HeLa and U87 cells, R 59-022 (40 uM, 30 minutes) activates PKC [4]. In Vero cells, R 59-022 (0-10 uM, 4 hours) bursts EBOV [5].
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| ln Vivo |
The median survival of SCID mice transplanted with U87 GBM cells was significantly increased by R 59-022 (2 mg/kg, intraperitoneal injection, 12 days) [6].
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| Cell Assay |
Western Blot Analysis [4]
Cell Types: HeLa Cell Tested Concentrations: 40 uM Incubation Duration: 30 minutes Experimental Results: Phosphorylation of PKC downstream targets increased approximately 2.5-fold. |
| Animal Protocol |
Animal/Disease Models: SCID (severe combined immunodeficient) mouse implanted with U87 GBM cells [6]
Doses: 10 mg/kg Route of Administration: intraperitoneal (ip) injection Experimental Results: Median survival increased and tumor volume diminished. |
| References |
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| Additional Infomation |
6-[2-[4-[(4-fluorophenyl)-phenylmethylidene]-1-piperidinyl]ethyl]-7-methyl-5-thiazolo[3,2-a]pyrimidinone is a diarylmethane.
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| Molecular Formula |
C27H26FN3OS
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|---|---|
| Molecular Weight |
459.58
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| Exact Mass |
459.178
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| CAS # |
93076-89-2
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| Related CAS # |
R 59-022 hydrochloride;93076-98-3
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| PubChem CID |
3012
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| Appearance |
White to off-white solid powder
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| Density |
1.26g/cm3
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| Boiling Point |
619.8ºC at 760mmHg
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| Flash Point |
328.6ºC
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| Index of Refraction |
1.654
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| LogP |
5.281
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
33
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| Complexity |
868
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C1N2C(SC=C2)=NC(C)=C1CCN1CC/C(=C(\C2C=CC(F)=CC=2)/C2C=CC=CC=2)/CC1
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| InChi Key |
MFVJXLPANKSLLD-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C27H26FN3OS/c1-19-24(26(32)31-17-18-33-27(31)29-19)13-16-30-14-11-22(12-15-30)25(20-5-3-2-4-6-20)21-7-9-23(28)10-8-21/h2-10,17-18H,11-16H2,1H3
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| Chemical Name |
6-[2-[4-[(4-fluorophenyl)-phenylmethylidene]piperidin-1-yl]ethyl]-7-methyl-[1,3]thiazolo[3,2-a]pyrimidin-5-one
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| Synonyms |
R59022 R 59022 R-59022
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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 |
| 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 : ~62.5 mg/mL (~135.99 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.44 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 (5.44 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.44 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1759 mL | 10.8795 mL | 21.7590 mL | |
| 5 mM | 0.4352 mL | 2.1759 mL | 4.3518 mL | |
| 10 mM | 0.2176 mL | 1.0879 mL | 2.1759 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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