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UC-514321 (UC514321), an analog of NSC370284, is more effective than NSC-370284 as an inhibitor of STAT/TET1. It acts by directly binding to STAT3/5 and suppressing the viability of AML cells with high level of TET1 expression both in vitro and in vivo.
| ln Vitro |
UC-514321 causes AML cells to undergo more apoptosis, but not normal HSPCs[1]. The suppression of AML cell viability by UC-514321 (0-500 nM, 48 hours) is dependent on TET1 signaling [1].
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|---|---|
| ln Vivo |
In an AML mouse model, UC-514321 (2.5 mg/kg, ip, once daily for 10 days) shows better anti-tumor activity than NSC370284 [1].
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: MONOMAC-6, THP-1, KOCL-48, KASUMI-1, ML-2, and NB4 cells. Tested Concentrations: 0-500 nM. Incubation Duration: 48 hrs (hours). Experimental Results: Most Dramatically repressed MONOMAC-6 cell viability. demonstrated no inhibitory effect on the viability of TET1-low AML. RT-PCR[1] Cell Types: MONOMAC-6 cells. Tested Concentrations: 0-500 nM. Incubation Duration: 48 hrs (hours). Experimental Results: Functioned as TET1-transcription inhibitors in TET1-high AMLs and their anti-leukemic effects are TET1-dependent. |
| Animal Protocol |
Animal/Disease Models: MLL-AF9-AML mice and AE9a-AML model[1].
Doses: 2.5 mg/kg. Route of Administration: IP., once per day, for 10 days. Experimental Results: demonstrated an improved therapeutic effect in AML mouse models in vivo. Prolonged the median survival over three fold. |
| References |
| Molecular Formula |
C26H35NO5
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|---|---|
| Molecular Weight |
441.559808015823
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| Exact Mass |
441.251
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| CAS # |
299420-83-0
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| PubChem CID |
339892
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| Appearance |
White to off-white solid powder
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| LogP |
5.5
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
32
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| Complexity |
599
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O1CCN(CC1)C(C1=C(C=C2C(=C1)OCO2)O)C1C=C(C(=C(C=1)C(C)(C)C)O)C(C)(C)C
|
| InChi Key |
XNARHFDDQALZPZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C26H35NO5/c1-25(2,3)18-11-16(12-19(24(18)29)26(4,5)6)23(27-7-9-30-10-8-27)17-13-21-22(14-20(17)28)32-15-31-21/h11-14,23,28-29H,7-10,15H2,1-6H3
|
| Chemical Name |
6-[(3,5-ditert-butyl-4-hydroxyphenyl)-morpholin-4-ylmethyl]-1,3-benzodioxol-5-ol
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| Synonyms |
UC514321 UC 514321
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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) |
Ethanol : ~50 mg/mL (~113.23 mM)
DMSO : ~25 mg/mL (~56.62 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.66 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. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.66 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 25.0 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 | 2.2647 mL | 11.3235 mL | 22.6470 mL | |
| 5 mM | 0.4529 mL | 2.2647 mL | 4.5294 mL | |
| 10 mM | 0.2265 mL | 1.1323 mL | 2.2647 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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