| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| ln Vitro |
In a dose-dependent manner, crotonoside (0-200 μM) specifically reduces the survival of AML cell lines MV4-11, MOLM-13 (with FLT3-ITD mutant), and KG-1 (without FLT3-ITD mutant). IC50 Their respective values are 11.6 μM, 12.7 μM, and 17.2 μM [1]. Crotonin (0-100 μM; 7 hours) suppresses the phosphorylation of Akt/mTOR, FLT3 Erk1/2, and STAT5, with the highest concentration of 12.5 μM showing a concentration-dependent strong inhibition [1]. A dose-dependent rise in the proportion of cells in the G0/G1 phase and a dose-dependent decrease in the percentage of cells in the G2/M and S phases are observed when using crotonin (0-100 μM; 12 hours) [1]. The number of apoptotic MV4-11 cells varies concentration-dependently with crotonoside (0-100 μM; 24 hours), pro-caspase-3 levels drop with dose, and caspase-3 precursor levels increase with dose. Cleaved caspase-3 fragment levels [1].
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|---|---|
| ln Vivo |
In comparison to vehicle treatment, crotonin (intraperitoneal and intravenous injection; 70 mg/kg, 35 mg/kg; once daily) generated considerable anticancer activity and reduced the growth of xenograft tumors [1].
|
| Cell Assay |
Cell Viability Assay [1]
Cell Types: AML cell lines MV4-11, MOLM-13 and KG-1 Cell Tested Concentrations: 0-200 μM Incubation Duration: 72 hrs (hours) Experimental Results: Inhibited AML cell growth than other cell lines tested. Western Blot Analysis[1] Cell Types: MV4-11 Cell Tested Concentrations: 0 μM, 12.5 μM, 25 μM, 50 μM Incubation Duration: 7 hrs (hours) Experimental Results: Inhibition of AML cell growth compared to other cell lines tested. Cell cycle analysis [1] Cell Types: MV4-11 Cell Tested Concentrations: 0 μM, 12.5 μM, 25 μM, 50 μM Incubation Duration: 12 hrs (hours) Experimental Results: Induced cell cycle arrest at G0/G1. Apoptosis analysis [1] Cell Types: MV4-11 Cell Tested Concentrations: 0 μM, 12.5 μM, 25 μM, 50 μM Incubation Duration: 24 hrs (hours) Experimental Results: Induced apoptosis of MV4-11 cells. |
| Animal Protocol |
Animal/Disease Models: MV4-11 cells NOD-SCID (severe combined immunodeficient) mouse [1]
Doses: 70 mg/kg, 35 mg/kg Route of Administration: intraperitoneal (ip) injection, intravenous (iv) (iv)injection; 70 mg/kg, 35 mg/kg; one time/day Experimental Results: Produced significant AML tumor inhibition rate of 93.5% at 70 mg/kg. |
| References | |
| Additional Infomation |
Crotonoside is a purine nucleoside.
Crotonoside has been reported in Croton tiglium with data available. |
| Molecular Formula |
C10H13N5O5
|
|---|---|
| Molecular Weight |
283.2407
|
| Exact Mass |
283.091
|
| CAS # |
1818-71-9
|
| PubChem CID |
65085
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| Appearance |
White to off-white solid powder
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| Density |
2.3±0.1 g/cm3
|
| Boiling Point |
831ºC at 760 mmHg
|
| Flash Point |
456.4ºC
|
| Vapour Pressure |
2.83E-29mmHg at 25°C
|
| Index of Refraction |
1.955
|
| LogP |
-3.42
|
| Hydrogen Bond Donor Count |
5
|
| Hydrogen Bond Acceptor Count |
7
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
20
|
| Complexity |
544
|
| Defined Atom Stereocenter Count |
4
|
| SMILES |
C1=NC2=C(NC(=O)N=C2N1[C@H]3[C@@H]([C@@H]([C@H](O3)CO)O)O)N
|
| InChi Key |
MIKUYHXYGGJMLM-UUOKFMHZSA-N
|
| InChi Code |
InChI=1S/C10H13N5O5/c11-7-4-8(14-10(19)13-7)15(2-12-4)9-6(18)5(17)3(1-16)20-9/h2-3,5-6,9,16-18H,1H2,(H3,11,13,14,19)/t3-,5-,6-,9-/m1/s1
|
| Chemical Name |
6-amino-9-[(2R,3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-1H-purin-2-one
|
| 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 |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~25 mg/mL (~88.26 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.34 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 (7.34 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 (7.34 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 | 3.5306 mL | 17.6529 mL | 35.3057 mL | |
| 5 mM | 0.7061 mL | 3.5306 mL | 7.0611 mL | |
| 10 mM | 0.3531 mL | 1.7653 mL | 3.5306 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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