| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 250mg |
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Purity: ≥98%
Adarotene (ST-1926), a synthetic, phenolic hydroxyl retinoid with proapoptotic activity, is an atypical retinoid and a promising anti-tumour agent with selective apoptotic activity on the leukaemic blast. The anti-tumour activity of the compound has been associated with its capacity to induce DNA double stranded breaks. ( Eur J Cancer. 2012 Dec 11. S0959-8049(12)00909-4.).
| ln Vitro |
Adarotene, with an IC50 ranging from 0.1 to 0.3 µM, inhibits the development of numerous human tumor cell lines in a dose-dependent manner. Depending on the tumor cells IGROV-1 and DU145, adarotene induces cells to accumulate in the G1/S or S phase of the cell cycle [1]. Adarotene exhibits apoptotic and cytotoxic properties against a range of leukemia and cancerous cells, including recently isolated AML blasts in primary culture. The ligand-binding domain of RARγ is similar to the molecular target of ST1926's apoptotic action in myeloid leukemia cells. When cells are treated with alpha-adarotene, intracellular calcium accumulates quickly [2].
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| ln Vivo |
In nude mice, adarotene (15, 20 mg/kg, orally administered) can considerably suppress the formation of tumors in human ovarian cancer A2780/DX and human melanoma MeWo [1]. Oral administration of adarotene (30, 40 mg/kg) has been shown to significantly and dose-dependently prolong the longevity of SCID mice harboring NB4 without evident harm [2].
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| References |
[1]. Cincinelli R, et al. A novel atypical retinoid endowed with proapoptotic and antitumor activity. J Med Chem. 2003 Mar 13;46(6):909-12.
[2]. Garattini E, et al. ST1926, a novel and orally active retinoid-related molecule inducing apoptosis in myeloid leukemia cells: modulation of intracellular calcium homeostasis. Blood. 2004 Jan 1;103(1):194-207 |
| Molecular Formula |
C25H26O3
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|---|---|
| Molecular Weight |
374.4721
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| CAS # |
496868-77-0
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| SMILES |
O=C(O)/C=C/C1=CC=C(C2=CC=C(O)C(C34C[C@H]5C[C@@H](C4)C[C@H](C5)C3)=C2)C=C1
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| InChi Key |
QAWBIEIZDDIEMW-RXJOCBMKSA-N
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| InChi Code |
InChI=1S/C25H26O3/c26-23-7-6-21(20-4-1-16(2-5-20)3-8-24(27)28)12-22(23)25-13-17-9-18(14-25)11-19(10-17)15-25/h1-8,12,17-19,26H,9-11,13-15H2,(H,27,28)/b8-3+/t17-,18+,19-,25?
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| Chemical Name |
(E)-3-(3'-((3r,5r,7r)-adamantan-1-yl)-4'-hydroxy-[1,1'-biphenyl]-4-yl)acrylic acid
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| Synonyms |
ST1926 ST 1926 ST-1926
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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 : ~25 mg/mL (~66.76 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.68 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 (6.68 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6704 mL | 13.3522 mL | 26.7044 mL | |
| 5 mM | 0.5341 mL | 2.6704 mL | 5.3409 mL | |
| 10 mM | 0.2670 mL | 1.3352 mL | 2.6704 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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