| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| Other Sizes |
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| ln Vitro |
The viability of HCT116 and SW620 cells is decreased by ASR-490 (0-1.6 µM; 24 hours, 48 hours) at 24 hours (IC50 = 750 nM in HCT116 cells, IC50 = 1.2 µM in SW620 cells) and 48 hours (in HCT116 cells, IC50 = 850 nM in SW620 cells) [1]. ASR-490 (750 nM in HCT116 cells, 1.2 µM in SW620 cells, 24 hours) inhibits colorectal cancer cells and exhibits apoptotic cell death and induction of pro-apoptotic markers Bax and cleaved PARP expression [1]. Notch1 overexpression is eliminated by ASR-490 (HCT116 cells; 750 nM over 24 hours, 600 nM over 48 hours), which also prevents HCT/Notch1 transfectants from growing [1].
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|---|---|
| ln Vivo |
ASR-490 (5 mg/kg; i.p.; three times per week for 4 weeks) suppresses control (pCMV/HCT116) and Notch1/HCT116 tumor growth in xenograft mice [1].
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| Cell Assay |
Cell viability assay [1]
Cell Types: HCT116, SW620 Cell Tested Concentrations: 0-1.6 µM Incubation Duration: 24 hrs (hours), 48 hrs (hours) Experimental Results: The viability of HCT116 and SW620 cells diminished within 24 hrs (hours) (IC50 =750 nM in HCT116 cells, IC50 = 1.2 µM in SW620 cells) and 48 hrs (hours) (IC50 = 600 nM in HCT116 cells, IC50 = 850 nM in SW620 cells). Apoptosis analysis[1] Cell Types: HCT116, SW620 Cell Tested Concentrations: 750 nM in HCT116 cells, 1.2 µM in SW620 cells Incubation Duration: 24 hrs (hours) Experimental Results: Shows apoptotic cell death and upregulation of pro-apoptotic markers Bax and cleavage PARP expression and inhibitory capacity in colorectal cancer cells. Cell proliferation experiment [1] Cell Types: HCT116 cell Tested Concentrations: 750 nM in 24 h, 600 nM in 48 h Incubation Duration: 24 h, 48 h Experimental Results: Overcome Notch1 overexpression and inhibit the growth of HCT/Notch1 transfectants. |
| Animal Protocol |
Animal/Disease Models: 6- to 8weeks old BALB/c athymic nude mice (nu/nu) (pCMV/HCT116 and Notch1/HCT116 (C4) xenografts) [1].
Doses: 5 mg/kg Route of Administration: intraperitoneal (ip) injection three times per week for 4 weeks Experimental Results: Inhibition of Notch1/HCT116 tumor growth in control (pCMV/HCT116) and xenograft mice. |
| References |
| Molecular Formula |
C34H41NO7
|
|---|---|
| Molecular Weight |
575.691850423813
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| Exact Mass |
575.288
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| CAS # |
2690312-67-3
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| PubChem CID |
156831801
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| Appearance |
White to light yellow solid powder
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| LogP |
5.3
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| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
42
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| Complexity |
1240
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| Defined Atom Stereocenter Count |
11
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| SMILES |
C[C@]12C(C=C[C@@H]([C@@]31O[C@]3([H])C[C@@]1([H])[C@]3([H])CC[C@@]([H])([C@]3(CC[C@]21[H])C)[C@@H]([C@]1([H])OC(C(=C(C1)C)CO)=O)C)OC(C1N=CC=CC=1)=O)=O
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| InChi Key |
VLOZRPFAQLWDLI-RJMVMCCISA-N
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| InChi Code |
InChI=1S/C34H41NO7/c1-18-15-26(40-30(38)21(18)17-36)19(2)22-8-9-23-20-16-29-34(42-29)28(41-31(39)25-7-5-6-14-35-25)11-10-27(37)33(34,4)24(20)12-13-32(22,23)3/h5-7,10-11,14,19-20,22-24,26,28-29,36H,8-9,12-13,15-17H2,1-4H3/t19-,20-,22+,23-,24-,26+,28-,29+,32+,33-,34+/m0/s1
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| Chemical Name |
[(1S,2R,6S,7S,9R,11S,12S,15R,16S)-15-[(1S)-1-[(2R)-5-(hydroxymethyl)-4-methyl-6-oxo-2,3-dihydropyran-2-yl]ethyl]-2,16-dimethyl-3-oxo-8-oxapentacyclo[9.7.0.02,7.07,9.012,16]octadec-4-en-6-yl] pyridine-2-carboxylate
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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 |
| 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 (~43.43 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.34 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 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 (4.34 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 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.34 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 | 1.7370 mL | 8.6852 mL | 17.3705 mL | |
| 5 mM | 0.3474 mL | 1.7370 mL | 3.4741 mL | |
| 10 mM | 0.1737 mL | 0.8685 mL | 1.7370 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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