| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| Targets |
Aurora A 28 nM (DC50) Aurora A 99 nM (Kd) Aurora A 193 nM (EC50) Cereblon
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|---|---|
| ln Vitro |
JB170 (1 μM; 24-72 hours; MV4-11 cells) decreases the survival of cancer cells via mediating the depletion of Aurora-A [1]. AURORA-A levels are lowered by JB170 (0.01-10 μM; 6 hours; MV4-11 cells) [1]. JB170 (0.5 μM; 12 hours; MV4-11 cells) inhibits or slows the advancement of the S phase [1]. JB170 (0.5 μM; 0-72 hours; MV4-11 cells) exclusively targets AURORA-A to trigger apoptosis[1]. JB170 (0.1 μM; 0-9 hours; IMR5 cells) exhibits a quick AURORA-A depletion. In comparison to AURORA-A, JB170 (0~1 μM; 6 hours; MV4-11 cells) was significantly diminished in the mutants. In MV4-11 cells, JB170 (0.1 μM; 18 hours) does not cause AURORA-A activation. JB170 (0~1 μM; 24 hours; IMR5 cells) significantly eliminates the depletion of AURORA-AT217D. JB170 (1 μM; 4 days; IMR5 cells) mediates the reduction of Aurora-A, which prevents the survival of cancer cells. By lowering AURORA-A mRNA levels, JB170 (IMR5 cells) lowers AURORA-A levels [1].
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: MV4-11 cells Tested Concentrations: 1 µM Incubation Duration: 24-72 hrs (hours) Experimental Results: After 72 hrs (hours), the number of viable cells was 32% of control levels. Western Blot Analysis[1] Cell Types: MV4-11 cells Tested Concentrations: 0.01~10 μM Incubation Duration: 6 hrs (hours) Experimental Results: Substantial degradation was observed at 100 nM and 1 µM. Apoptosis Analysis[1] Cell Types: MV4-11 cells Tested Concentrations: 0.5 µM Incubation Duration: 0~72 hrs (hours) Experimental Results: Apoptosis was exclusively caused by targeting AURORA-A. Cell Cycle Analysis[1] Cell Types: MV4-11 cells Tested Concentrations: 0.5 µM Incubation Duration: 12 hrs (hours) Experimental Results: Delayed or arrested S-phase progression. |
| References |
[1]. Adhikari B, et al. PROTAC-mediated degradation reveals a non-catalytic function of AURORA-A kinase. Nat Chem Biol. 2020;16(11):1179-1188.
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| Molecular Formula |
C48H44CLFN8O11
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|---|---|
| Molecular Weight |
963.36
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| CAS # |
2705844-82-0
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| SMILES |
C(NCCOCCOCCNC(COC1=CC=CC2=C1C(=O)N(C1CCC(=O)NC1=O)C2=O)=O)(=O)C1=CC=C(NC2=NC=C3C(=N2)C2=CC=C(Cl)C=C2C(C2=C(OC)C=CC=C2F)=NC3)C=C1OC
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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 : 100 mg/mL (103.80 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (2.60 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 | 1.0380 mL | 5.1902 mL | 10.3803 mL | |
| 5 mM | 0.2076 mL | 1.0380 mL | 2.0761 mL | |
| 10 mM | 0.1038 mL | 0.5190 mL | 1.0380 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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