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Purity: ≥98%
Oridonin (NSC-250682; Isodonol) is a novel, naturally occurring and cell-permeable diterpenoid extracted from Rabdosia rubescens with anticancer activity. Oridonin is a substance that acts as an AKT inhibitor and has anti-tumor, anti-bacterial, and anti-inflammatory properties. Its IC50 values for AKT1 and AKT2 are 8.4 and 8.9 μM, respectively. By activating the intrinsic apoptotic pathway and inducing a caspase-3-mediated degradation, oridonin exposure causes apoptosis in leukemic cells that have been exposed to AE. The anti-NF-B compound oridonin also exhibits antiproliferative (ED50 ~ 2.7 µg/ml in lymphoid malignant cells) and antiangiogenic (significantly inhibits network formation of HMEC-1 cells at 2.5 µg/m) properties.
| Targets |
Akt1 (IC50 = 8.4 μM); Akt2 (IC50 = 8.9 μM)
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| ln Vitro |
Oridonin is an ATP-competitive AKT inhibitor with IC50 values for AKT1 and AKT2 of 8.4 and 8.9 M, respectively. By targeting AKT1/2, oridonin (5, 10 or 20 μM) obviously stops the growth of the ESCC cells KYSE70, KYSE410, and KYSE450. In KYSE70, KYSE410, and KYSE450 cells, oridonin (10 or 20 μM) causes G2/M phase cell cycle arrest and, at 20 μM, induces apoptosis. Additionally, the combination of cisplatin or 5-FU with oridonin (5, 10 or 20 μM) enhances the inhibition of esophageal squamous cell carcinoma (ESCC) cell growth[1]. AKT/mTOR signaling is preferentially suppressed by oridonin (0.1 and 1 μM). Additionally, oridonin (1 μM) selectively inhibits the growth of breast cancer cells by activating AKT signaling excessively[2].
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| ln Vivo |
Oridonin (160 mg/kg, p.o.) shows significant reduction in the tumor growth without obvious weigh loss in SCID mice bearing EG9 and HEG18 tumor cells. Treatment with oridonin also reduces the amount of Ki-67, phosphorylated AKT, GSK-3, or mTOR expressed in mice[1]. In nude mice, oridonin (15 mg/kg, i.p.) inhibits breast cancer cell growth by hyperactivating AKT signaling[2].
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| Enzyme Assay |
For the AKT kinase assay, the ADP-Glo™ Kinase Assay Kit is used. Active AKT1 or AKT2 kinase and inactive GSK-3β as substrate are mixed by 1× reaction buffer and then added to a white 96-well plate. Pure ATP provided in the kit is serially diluted obtain a final concentration of 0, 1, 10, 50, and 100 μM. GSK-3β is diluted with DMSO until a final concentration of 2.5, 5, 10, or 20 μM is reached. Using the Luminoskan Ascent plate reader, the combined solution is incubated at room temperature to measure the amount of luciferase activity. [1]
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| Cell Assay |
Cells are seeded (6×103 cells/well for KYSE70; 2.5×103 cells/well for KYSE410; 2×103 cells/well for KYSE450) in 96-well plates and incubated for 24 h and then treated with different amounts of Oridonin or vehicle. The MTT assay is used to measure cell proliferation after incubation for 24, 48, or 72 hours. For anchorage-independent cell growth assessment, cells (2.5, 5 or 10 μM Oridonin) suspended in complete medium are added to 0.3% agar with vehicle, 2.5, 5 or 10 μM Oridonin in a top layer over a base layer of 0.5% agar with vehicle, 2.5, 5 or 10 μM Oridonin.
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| Animal Protocol |
Mice: Breast cancer cells are isolated, resuspended in 40% Matrigel-Basement Membrane Matrix, free of LDEV, and then injected (100 L per site) into the fourth pair of mammary fat pads of naked mice (CrTac: NCr-Foxn1nu). Tumors are measured in two dimensions using manual calipers. Tumor volume is calculated using the formula: Volume = 0.5 × length × width × width. Tumor volume is measured every 2-3 days. Tumors are collected and then fixed in 70% ethanol for an hour before being histopathologically examined. Mice are given either the vehicle (1% Pluronic F68) or oridonin (15 mg/kg) intraperitoneally (IP) every day. In 1-methyl-2 pyrolidone and polyethylene glycol 300 (PEG300), BEZ235 is reconstituted 1:9. By oral gavage, mice are administered this compound formulation at a dose of 45 mg/kg daily (QD)[2].
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| References | |
| Additional Infomation |
Oridonin is an organic heteropentacyclic compound and ent-kaurane diterpenoid with formula C20H28O6 isolated from the leaves of the medicinal herb Rabdosia rubescens. It has a role as an antineoplastic agent, an angiogenesis inhibitor, an apoptosis inducer, an anti-asthmatic agent, a plant metabolite and an antibacterial agent. It is an organic heteropentacyclic compound, an enone, a cyclic hemiketal, a secondary alcohol and an ent-kaurane diterpenoid.
Oridonin has been reported in Isodon japonicus, Isodon macrocalyx, and other organisms with data available. |
| Molecular Formula |
C20H28O6
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| Molecular Weight |
364.43
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| Exact Mass |
364.188
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| Elemental Analysis |
C, 65.92; H, 7.74; O, 26.34
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| CAS # |
28957-04-2
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| Related CAS # |
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| PubChem CID |
5321010
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
599.8±50.0 °C at 760 mmHg
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| Melting Point |
248-250ºC
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| Flash Point |
215.0±23.6 °C
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| Vapour Pressure |
0.0±3.9 mmHg at 25°C
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| Index of Refraction |
1.635
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| LogP |
1.44
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
26
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| Complexity |
717
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| Defined Atom Stereocenter Count |
9
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| SMILES |
O1C([H])([H])C23C([H])(C([H])([H])C([H])([H])C(C([H])([H])[H])(C([H])([H])[H])C2([H])C([H])(C1(C12C(C(=C([H])[H])C([H])(C([H])([H])C([H])([H])C31[H])C2([H])O[H])=O)O[H])O[H])O[H]
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| InChi Key |
SDHTXBWLVGWJFT-BAFGBBEMSA-N
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| InChi Code |
InChI=1S/C20H28O6/c1-9-10-4-5-11-18-8-26-20(25,19(11,14(9)22)15(10)23)16(24)13(18)17(2,3)7-6-12(18)21/h10-13,15-16,21,23-25H,1,4-8H2,2-3H3/t10-,11-,12-,13+,15+,16-,18+,19-,20-/m0/s1
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| Chemical Name |
(1S,2S,5S,8R,9S,10S,11R,15S,18R)-9,10,15,18-tetrahydroxy-12,12-dimethyl-6-methylidene-17-oxapentacyclo[7.6.2.15,8.01,11.02,8]octadecan-7-one
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| Synonyms |
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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 |
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| 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: 62.5~72 mg/mL (171.5~197.6 mM)
Water: ~20 mg/mL warming (~134.1 mM) Ethanol: ~34 mg/mL (~93.3 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.71 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 20.8 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: ≥ 2.08 mg/mL (5.71 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 20.8 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. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.71 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 5% DMSO+20%PEG 300+ddH2O: 12.5mg/ml Solubility in Formulation 5: ≥ 5 mg/mL (13.72 mM) (saturation unknown) in 10% 1-Methyl-2-pyrrolidinone 90% PEG300 (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7440 mL | 13.7201 mL | 27.4401 mL | |
| 5 mM | 0.5488 mL | 2.7440 mL | 5.4880 mL | |
| 10 mM | 0.2744 mL | 1.3720 mL | 2.7440 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05130892 | Completed | Drug: Tranilast Drug: Colchicine |
NLRP3 hsCRP |
Wuhan Union Hospital, China | November 15, 2021 | Phase 4 |
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