| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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| Targets |
PLK2 0.31 μM (IC50) PLK1 >10 μM (IC50) PLK3 >10 μM (IC50) PLK4 >10 μM (IC50)
|
|---|---|
| ln Vitro |
With IC50 values greater than 10 μM, ON1231320 (compound 7ao) exhibits no inhibitory effect against PLK1, PLK3, or PLK4 [1]. In human tumor cells, ON1231320 (0–5 μM; 24 hours) triggers programmed cell death [1]. 16 tumor cell lines (IC50=0.035-0.2 μM) are inhibited by ON1231320 (DU145, MCF-7, BT474, SK-OV-3, MIA-PaCa-2, SK-MEL-28, A549, U87, COLO -205, HELA, H1975, RAJI, U205, K562, GRANTA-519)[1]. Tubulin polymerization is not substantially inhibited by ON1231320 [1]. Human fibroblasts that are normal are unaffected by ON1231320 [2].
|
| ln Vivo |
ON1231320 (compound 7ao; 75 mg/kg; intraperitoneal injection; given every other day, or Q2D) for 20 days. tumour development was markedly suppressed[1].
|
| Cell Assay |
Apoptosis Analysis[1]
Cell Types: U2OS cells Tested Concentrations: 0-5 µM Incubation Duration: 24 hrs (hours) Experimental Results: Increased the activity of Caspases 3/7 in a dose-dependent manner. Induced apoptosis. |
| Animal Protocol |
Animal/Disease Models: 6-8 week old NCR nu/nu female mice with MDAMB-231 triple negative breast cancer cells[1]
Doses: 75 mg/kg Route of Administration: IP; alternate days (Q2D) for 20 days Experimental Results: Resulted in significant inhibition of tumor growth (86.5%) |
| References |
| Molecular Formula |
C22H15F2N5O3S
|
|---|---|
| Molecular Weight |
467.448009729385
|
| Exact Mass |
467.086
|
| CAS # |
1312471-39-8
|
| PubChem CID |
67240318
|
| Appearance |
Light yellow to green yellow solid powder
|
| LogP |
3.3
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
4
|
| Heavy Atom Count |
33
|
| Complexity |
897
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
S(C1C=CC(=CC=1F)F)(C1=CC2=CN=C(NC3C=CC4=C(C=CN4)C=3)N=C2N(C)C1=O)(=O)=O
|
| InChi Key |
ZEHBZHZMQSHZFI-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C22H15F2N5O3S/c1-29-20-13(9-19(21(29)30)33(31,32)18-5-2-14(23)10-16(18)24)11-26-22(28-20)27-15-3-4-17-12(8-15)6-7-25-17/h2-11,25H,1H3,(H,26,27,28)
|
| Chemical Name |
6-(2,4-difluorophenyl)sulfonyl-2-(1H-indol-5-ylamino)-8-methylpyrido[2,3-d]pyrimidin-7-one
|
| HS Tariff Code |
2934.99.9001
|
| 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: 50 mg/mL (106.96 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (5.35 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1393 mL | 10.6963 mL | 21.3927 mL | |
| 5 mM | 0.4279 mL | 2.1393 mL | 4.2785 mL | |
| 10 mM | 0.2139 mL | 1.0696 mL | 2.1393 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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