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Seocalcitol (EB-1089) is a novel second generation vitamin D analog with potential antineoplastic activity. It binds to vitamin D receptor protein from human osteosarcoma MG-63 cells with Kd of 0.27 nM. Seocalcitol binds to and activates the vitamin D receptor, a cytoplasmic polypeptide expressed in normal vitamin D responsive tissues, but also overexpressed in certain cancers including hepatocellular carcinoma and pancreatic cancer.
| ln Vitro |
In mouse bone marrow cultures, osteoclast recruitment is stimulated by seocalcitol (EB 1089), with an EC50 of 0.1 nM. Bone resorption is stimulated by osteocalcitol, whose estimated EC50 is 0.03 nM[1]. In the kidney, seocalcitol (EB 1089) increases 24-carboxylase mRNA in a dose-dependent manner (EC50=0.4±0.13). Seocalcitol has a Kd value of 0.48±0.04 nM in the bridge. Seocalcitol's Kd in the bridge, however, is 1.43±0.19 nM)[2]. Cellular secretion is dose-dependently induced by seocalcitol (0.1–10 nM). Compared to 1 nM VD3, 1 nM Seocalcitol (EB 1089) was associated with higher lactation activity.
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| ln Vivo |
Compared to 1,25 (OH) 2VD3, the synthetic vitamin D analog seocalcitol (EB1089) has less hypercalcemic action. At a daily dose of 0.5 μg/kg body weight, theocalcidol, a long-term intraperitoneal (IP) product of C3H/Sy, had a strong inhibitory impact on the development of hepatocellular carcinoma (HCC) in a different investigation [4]. At 4 to 12 days of age (P4 to P12), theocalciferol (EB 1089) was given intraperitoneally at a dose of 0.38 or 1.25 μg/kg body weight (BW)/day, with daily doses in the postpartum reserve. Merely the maximum dosage of ceciocalcidol (1.25 μg/kg BW) greatly decreased weight growth when utilized either by itself or in conjunction with tretinoin, all-trans retinoic acid (RA), or dexamethasone [5].
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| References |
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| Additional Infomation |
Seocalcitol is a vitamin D3 analogue with potential antineoplastic activity. Seocalcitol binds to and activates the vitamin D receptor, a cytoplasmic polypeptide expressed in normal vitamin D responsive tissues, but also overexpressed in certain cancers including hepatocellular carcinoma and pancreatic cancer. Mediated through vitamin D receptor, this agent induces cancer cell differentiation, inhibits cancer cell growth and induces apoptosis. In addition, seocalcitol may also induce growth arrest and apoptosis independent of vitamin D receptor activation through mechanisms that are not fully elucidated.
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| Molecular Formula |
C₃₀H₄₆O₃
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|---|---|
| Molecular Weight |
454.68
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| Exact Mass |
454.344
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| CAS # |
134404-52-7
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| PubChem CID |
5288149
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| Appearance |
White to off-white solid powder
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
608.5±55.0 °C at 760 mmHg
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| Flash Point |
252.3±26.1 °C
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| Vapour Pressure |
0.0±4.0 mmHg at 25°C
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| Index of Refraction |
1.560
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| LogP |
7.02
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
33
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| Complexity |
812
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| Defined Atom Stereocenter Count |
6
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| SMILES |
CCC(CC)(/C=C/C=C/[C@@H](C)[C@H]1CC[C@@H]\2[C@@]1(CCC/C2=C\C=C/3\C[C@H](C[C@@H](C3=C)O)O)C)O
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| InChi Key |
LVLLALCJVJNGQQ-SEODYNFXSA-N
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| InChi Code |
InChI=1S/C30H46O3/c1-6-30(33,7-2)18-9-8-11-21(3)26-15-16-27-23(12-10-17-29(26,27)5)13-14-24-19-25(31)20-28(32)22(24)4/h8-9,11,13-14,18,21,25-28,31-33H,4,6-7,10,12,15-17,19-20H2,1-3,5H3/b11-8+,18-9+,23-13+,24-14-/t21-,25-,26-,27+,28+,29-/m1/s1
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| Chemical Name |
(1R,3S,5Z)-5-[(2E)-2-[(1R,3aS,7aR)-1-[(2R,3E,5E)-7-ethyl-7-hydroxynona-3,5-dien-2-yl]-7a-methyl-2,3,3a,5,6,7-hexahydro-1H-inden-4-ylidene]ethylidene]-4-methylidenecyclohexane-1,3-diol
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| Synonyms |
EB 1089EB-1089EB1089
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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 Note: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| 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 (~109.97 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.50 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 (5.50 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 | 2.1993 mL | 10.9967 mL | 21.9935 mL | |
| 5 mM | 0.4399 mL | 2.1993 mL | 4.3987 mL | |
| 10 mM | 0.2199 mL | 1.0997 mL | 2.1993 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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