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9-cis-UAB30

Alias: (9Z)-UAB-30
9-cis-UAB30 is a ralcinol agonist.
9-cis-UAB30
9-cis-UAB30 Chemical Structure CAS No.: 205252-57-9
Product category: Oct
This product is for research use only, not for human use. We do not sell to patients.
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500mg
1g
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Product Description
9-cis-UAB30 is a rexinoid agonist. 9-cis-UAB30 significantly reduces the proliferation, viability, and migration ability of patient-derived xenografts (PDX). 9-cis-UAB30 induces cell cycle arrest, manifested by a significant increase in the proportion of cells in G1 phase and a significant decrease in the proportion of cells in S phase. This is achieved by downregulating the activity of SKP2 and/or the 20S proteasome, thereby increasing the stability of the p27kip1 protein. 9-cis-UAB30 downregulates the expression levels of stem cell marker mRNAs (Oct4, Nanog, Sox2, nestin) and upregulates the expression levels of differentiation marker mRNAs (β3-tubulin, NSE, HOXC9, GAP43). At the tested dose, 9-cis-UAB30 has no adverse effects on the central nervous system or cardiovascular system. 9-cis-UAB30 can be used to study neuroblastoma, cutaneous T-cell lymphoma, and breast cancer.
Biological Activity I Assay Protocols (From Reference)
ln Vitro
9-cis-UAB30 (0-50 μM, 96 hours) can induce neurite growth in COA6 cells at concentrations as low as 10 μM[1]. 9-cis-UAB30 (0-100 μM, 96 hours) significantly reduces the proliferation and survival rate of COA3 and COA6 cells[1]. 9-cis-UAB30 (25-50 μM, 3-7 days) significantly reduces the migration and invasion abilities of COA3 and COA6 cells[1]. 9-cis-UAB30 (0-50 μM, 24 hours) significantly increases the proportion of G1 phase cells and decreases the proportion of S phase cells in COA3 and COA6 cells, indicating that cell cycle arrest occurs at the G1/S phase transition point[1]. 9-cis-UAB30 (0-100 μM, 24-96 hours) significantly reduced and effectively targeted CD133-positive or CD133-enriched cells in COA3 and COA6 cells [1]. 9-cis-UAB30 (0-50 μM, 7 days) significantly reduced the number of tumor spheroids formed in COA3 and COA6 cells [1]. 9-cis-UAB30 (0-25 μM, 72 hours) significantly downregulated the mRNA expression levels of stem cell markers (Oct4, Nanog, Sox2, nestin) in COA3 and COA6 PDX cells and upregulated the mRNA expression levels of differentiation markers (β3-tubulin, NSE, HOXC9, GAP43) [1]. Treatment with 9-cis-UAB30 (5-50 μM, 42-48 h) for 24 h and 48 h significantly inhibited the viability of MyLa and HuT78 cells[2]. 9-cis-UAB30 has potent inhibitory activity against a variety of cutaneous T-cell lymphoma (CTCL) cell lines, including MyLa cells (IC50 = 34.7 μM), HuT78 cells (IC50 = 34.7 μM) and HH cells (IC50 = 34.7 μM)[2]. 9-cis-UAB30 (10-25 μM, 6-24 h) increased the expression level of p27kip1 protein in MyLa cells, HuT78 cells and HH cells, while decreasing the expression level of SKP2 protein[2]. 9-cis-UAB30 (10-25 μM, 6-24 h) did not change the homeostatic level of p27kip1 mRNA in MyLa, HuT78 and HH cells, but significantly reduced the level of SKP2 mRNA; CKS1B mRNA was unaffected [2]. 9-cis-UAB30 (25 μM, 12-24 h) inhibited the activity of the 20S proteasome, but its effect varied in different cell lines: significant inhibition was observed in HuT78 cells at 18-24 h; inhibition was observed in HH cells at 24 h; and no significant effect was observed in MyLa cells [2].
ln Vivo
9-cis-UAB30 (0-100 mg/kg, septum, once daily for 28 days) was primarily monitored for a no-observed adverse effect level (NOAEL) of 3 mg/kg/day, while doses of 15-100 mg/kg showed some hepatotoxicity [3]. 9-cis-UAB30 (0-100 mg/kg, minimum, once daily for 28 days) was non-toxic to pugs and had no adverse effects on the central nervous system and cardiovascular system [3].
Cell Assay
Cell Proliferation Assay[1]
Cell Types: COA3 and COA6 PDX cells
Tested Concentrations: 0 μM, 10 μM, 25 μM, 50 μM, 100 μM
Incubation Duration: 96 h
Experimental Results: Significantly reduced the proliferation rate of COA3 and COA6 cells.
RT-PCR[1]
Cell Types: COA3 and COA6 PDX cells
Tested Concentrations: 0 μM, 10 μM, 25 μM
Incubation Duration: 72 h
Experimental Results: Downregulated the mRNA abundance of stem cell markers (Oct 4, Nanog, Sox 2, nestin). Upregulated the mRNA abundance of differentiation markers (β3-tubulin, NSE, HOXC9, GAP43).
Cell Viability Assay[2]
Cell Types: MyLa cells, HuT78 cells
Tested Concentrations: 0 μM, 10 μM, 25 μM
Incubation Duration: 72 h
Experimental Results: In MyLa cells, 50 μM reduced cell number within 24 hours; at 48 hours, both 25 μM and 50 μM inhibited cell viability. In HuT78 cells, 5 μM inhibited cell viability within 24 hours.
References

[1]. https://pubmed.ncbi.nlm.nih.gov/33010553/

[2]. https://pubmed.ncbi.nlm.nih.gov/29599065/

[3]. https://pubmed.ncbi.nlm.nih.gov/21649485/

[4]. https://pubmed.ncbi.nlm.nih.gov/20335511/

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C20H22O2
Molecular Weight
294.39
CAS #
205252-57-9
Appearance
Typically exists as solids at room temperature
Synonyms
(9Z)-UAB-30
HS Tariff Code
2934.99.9001
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)
Solubility Data
Solubility (In Vitro)
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
Solubility (In Vivo)
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

Injection Formulations
(e.g. IP/IV/IM/SC)
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution 50 μL Tween 80 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO 400 μLPEG300 50 μL Tween 80 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).
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Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO 900 μL (20% SBE-β-CD in saline)]
*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.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO 100 μLPEG300 200 μL castor oil 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10: 10 : 80 (i.e. 100 μL Ethanol 100 μL Cremophor 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH 400 μLPEG300 50 μL Tween 80 450 μL Saline)


Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).
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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders


Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.3969 mL 16.9843 mL 33.9685 mL
5 mM 0.6794 mL 3.3969 mL 6.7937 mL
10 mM 0.3397 mL 1.6984 mL 3.3969 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.

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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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