| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| 100mg | |||
| Other Sizes |
| Targets |
The action targets of Caudatin are the VEGF-VEGFR2-AKT/FAK signaling axis; IC50 for inhibiting HUVEC proliferation = 23.6 ± 2.1 μM[1]
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|---|---|
| ln Vitro |
1. HUVEC proliferation inhibition: Caudatin (10/20/40 μM) inhibited proliferation in concentration-time-dependent manner. At 72 h, inhibition rates were 28.3±3.1% (10 μM), 45.6±3.8% (20 μM), 68.2±4.5% (40 μM); IC50 = 23.6±2.1 μM (MTT) [1]
2. HUVEC migration suppression: 40 μM Caudatin reduced VEGF-induced migration by 72.4±5.8% (Transwell, crystal violet staining) [1] 3. HUVEC tube formation inhibition: 40 μM Caudatin decreased tube length by 65.7±4.9% and branch number by 68.3±5.2% (Matrigel assay) [1] 4. Signaling downregulation: 40 μM Caudatin reduced VEGF-induced p-VEGFR2 (78.5±6.1%), p-AKT (71.2±5.4%), p-FAK (69.3±5.7%); total proteins unchanged (Western blot) [1] |
| ln Vivo |
Nude mouse HCT116 xenograft model (groups: control, Caudatin 20/40 mg/kg, ip, q2d×21d):
1. Tumor growth inhibition: 40 mg/kg reduced volume by 56.7±4.5% and weight by 58.3±4.2% [1] 2. MVD reduction: 40 mg/kg decreased CD31+ MVD from 48.1±3.5 to 18.2±2.3 vessels/field (62.1±5.3% reduction) [1] 3. Signaling inhibition: 40 mg/kg reduced tumor p-VEGFR2 (68.5±5.8%), p-AKT (63.2±4.9%), p-FAK (61.7±5.1%) (Western blot) [1] |
| Cell Assay |
1. HUVEC culture: EGM-2 (10% FBS, growth factors), 37°C/5% CO₂, passages 3–8 [1]
2. MTT assay: 5×10³ cells/well (96-well), Caudatin + VEGF, 24/48/72 h; MTT (5 mg/mL) → DMSO, read 570 nm [1] 3. Transwell assay: 1×10⁵ cells/upper chamber (8 μm), VEGF + Caudatin; 24 h, crystal violet staining, count migrated cells [1] 4. Tube formation: Matrigel-coated 96-well, 2×10⁴ cells/well + Caudatin + VEGF; 6 h, quantify tube length/branches [1] 5. Western blot: Caudatin + VEGF for 1 h; RIPA lysis, BCA quantification, detect p-VEGFR2/VEGFR2/p-AKT/AKT/p-FAK/FAK/β-actin [1] |
| Animal Protocol |
1. Animals: BALB/c nude mice (4–6 weeks, 18–22 g), SPF environment (22±2°C, 12 h light/dark) [1]
2. Xenograft: 1×10⁷ HCT116 cells/mouse (sc, right flank); tumor volume = (length×width²)/2 [1] 3. Drug admin: Caudatin dissolved in DMSO + saline (DMSO <1%, 2/4 mg/mL); 20/40 mg/kg ip, q2d×21d; control = saline-DMSO [1] 4. Sample collection: Sacrifice, excise tumor (weigh/photograph); fix part in 4% paraformaldehyde (CD31 IHC), store rest at -80°C (Western blot) [1] |
| Toxicity/Toxicokinetics |
1. In vitro experiments: Caudatin (concentration up to 40 μM) can maintain NHFF cell viability >85% (MTT assay) [1] 2. In vivo experiments: No weight loss; normal serum ALT/AST/BUN/Cr levels; no liver/kidney/heart/lung/spleen damage (histopathological examination) [1]
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| References | |
| Additional Infomation |
It has been reported that Caudatin has been found in Araujia sericifera, and there is relevant data.
1. Caudatin is a C21 steroidal glycoside from Araujia species (traditional use: anti-inflammatory/anti-tumor)[1] 2. Mechanism: inhibits the VEGF-VEGFR2-AKT/FAK axis, thereby inhibiting endothelial cell function (angiogenesis)[1] 3. Significance: It has good safety and is a potential anti-angiogenic/anti-tumor lead compound[1] |
| Molecular Formula |
C28H42O7
|
|---|---|
| Molecular Weight |
490.6289
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| Exact Mass |
490.293
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| CAS # |
38395-02-7
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| PubChem CID |
21633059
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
617.9±55.0 °C at 760 mmHg
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| Flash Point |
197.5±25.0 °C
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| Vapour Pressure |
0.0±4.1 mmHg at 25°C
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| Index of Refraction |
1.584
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| LogP |
4.37
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
35
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| Complexity |
984
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| Defined Atom Stereocenter Count |
8
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| SMILES |
CC(C)/C(=C/C(=O)O[C@@H]1C[C@@H]2[C@]3(CC[C@@H](CC3=CC[C@]2([C@@]4([C@]1([C@@](CC4)(C(=O)C)O)C)O)O)O)C)/C
|
| InChi Key |
VWLXIXALPNYWFH-UXGQNDOZSA-N
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| InChi Code |
InChI=1S/C28H42O7/c1-16(2)17(3)13-23(31)35-22-15-21-24(5)9-8-20(30)14-19(24)7-10-27(21,33)28(34)12-11-26(32,18(4)29)25(22,28)6/h7,13,16,20-22,30,32-34H,8-12,14-15H2,1-6H3/b17-13+/t20-,21+,22+,24-,25+,26+,27-,28+/m0/s1
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| Chemical Name |
[(3S,8S,9R,10R,12R,13S,14R,17S)-17-acetyl-3,8,14,17-tetrahydroxy-10,13-dimethyl-1,2,3,4,7,9,11,12,15,16-decahydrocyclopenta[a]phenanthren-12-yl] (E)-3,4-dimethylpent-2-enoate
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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: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 (~101.91 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (10.19 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 50.0 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: ≥ 5 mg/mL (10.19 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 50.0 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. View More
Solubility in Formulation 3: ≥ 5 mg/mL (10.19 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 | 2.0382 mL | 10.1910 mL | 20.3820 mL | |
| 5 mM | 0.4076 mL | 2.0382 mL | 4.0764 mL | |
| 10 mM | 0.2038 mL | 1.0191 mL | 2.0382 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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