| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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| ln Vitro |
CLZ-8 (compound 8) (0-160 μM, 48 h) strongly suppresses apoptosis that is dependent on PUMA [1]. In a dose-dependent way, CLZ-8 (0–1 μM, 2 hours) markedly increased the vitality of irradiation cells, considerably shielded HUVEC, and suppressed overexpressed PUMA [2]. Radiation-induced apoptosis is attenuated by CLZ-8 (0-1 μM, 24 hours) [2]. HUVEC is protected against DNA fragmentation by CLZ-8 (1 μM, 2 hours) [2].
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|---|---|
| ln Vivo |
Mice treated with CLZ-8 (0-400 mg/kg; ig; once) have strong anti-radiation effects [2].
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| Cell Assay |
Apoptosis analysis[1][2]
Cell Types: DLD-1 cells or HUVEC Cell Tested Concentrations: 0-160 μM (DLD-1) or 0.01, 0.1 and 1 μM (HUVEC) Incubation Duration: 48 hrs (hours) (DLD-1 ) or 24 hrs (hours) (HUVEC) Experimental Results: Dramatically inhibited PUMA-dependent apoptosis with an IC50 of 38.93 ± 0.91 μM. Attenuates radiation-induced apoptosis. Western Blot Analysis [2] Cell Types: HUVEC Cell Tested Concentrations: 0.001, 0.01, 0.1 and 1 μM Incubation Duration: 2 h Experimental Results: PUMA induction was inhibited and p53 levels were Dramatically diminished after radiation. Dramatically diminished MCL-1 levels and increased Bcl-XL levels. |
| Animal Protocol |
Animal/Disease Models: 6-8 weeks old male balb/c (Bagg ALBino) mouse [2]
Doses: 100, 200 and 400 mg/kg Route of Administration: intragastric (po) (po)administration once 30 minutes before irradiation. Experimental Results: Improved survival rate of irradiated mice. |
| References |
| Molecular Formula |
C22H23N3O2S
|
|---|---|
| Molecular Weight |
393.5019
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| Exact Mass |
393.151
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| CAS # |
678158-55-9
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| PubChem CID |
988971
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
3.2
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
28
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| Complexity |
599
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S1/C(=C(/[H])\C2C([H])=C([H])C(C3C([H])=C([H])C([H])=C([H])C=3[H])=C([H])C=2[H])/C(N=C1N1C([H])([H])C([H])([H])N(C([H])([H])C([H])([H])O[H])C([H])([H])C1([H])[H])=O
|
| InChi Key |
IBEWMFVUBLAYJT-SILNSSARSA-N
|
| InChi Code |
InChI=1S/C22H23N3O2S/c26-15-14-24-10-12-25(13-11-24)22-23-21(27)20(28-22)16-17-6-8-19(9-7-17)18-4-2-1-3-5-18/h1-9,16,26H,10-15H2/b20-16-
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| Chemical Name |
(5Z)-2-[4-(2-hydroxyethyl)piperazin-1-yl]-5-[(4-phenylphenyl)methylidene]-1,3-thiazol-4-one
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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 : ~50 mg/mL (~127.06 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.83 mg/mL (2.11 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 8.3 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 | 2.5413 mL | 12.7065 mL | 25.4130 mL | |
| 5 mM | 0.5083 mL | 2.5413 mL | 5.0826 mL | |
| 10 mM | 0.2541 mL | 1.2706 mL | 2.5413 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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