| 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 |
SIK1 SIK2 SIK3
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|---|---|
| ln Vitro |
MRIA9 (5 μM) MRIA9 causes significant apoptosis, which makes SKOV3 cells more susceptible to paclitaxel treatment[1]. In HeLa cells, MRIA9 (5 μM) combined with paclitaxel (2 nM) greatly increases cell death[1]. MRIA9 significantly impairs centrosome function, misplaces the spindles during mitosis in ovarian cancer cell lines, stops the centrosome from disjunction in the late G2 phase, and makes patient-derived 3D-spheroids and ovarian cancer cells more sensitive to paclitaxel treatment[2].
|
| ln Vivo |
High oral bioavailability (F = 75-80%) is demonstrated by MRIA9[1].
|
| Cell Assay |
Cell Viability Assay[1]
Cell Types: SKOV3 cells. Tested Concentrations: 0.5-5 μM (1 nM paclitaxel). Incubation Duration: 9 days. Experimental Results: Inhibited cell growth. |
| References |
| Molecular Formula |
C24H22CLFN6O3
|
|---|---|
| Molecular Weight |
496.92
|
| Exact Mass |
496.142
|
| CAS # |
2750707-05-0
|
| PubChem CID |
162642759
|
| Appearance |
White to off-white solid powder
|
| LogP |
2.2
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
9
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
35
|
| Complexity |
784
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C([C@H]1OC[C@@H](CO1)N)N1C(C(C2C=CC(C3N=CC=CC=3F)=CC=2Cl)=CC2=CN=C(N=C12)NC)=O
|
| InChi Key |
QKNBRNSGPNCARD-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C24H22ClFN6O3/c1-28-24-30-9-14-7-17(16-5-4-13(8-18(16)25)21-19(26)3-2-6-29-21)23(33)32(22(14)31-24)10-20-34-11-15(27)12-35-20/h2-9,15,20H,10-12,27H2,1H3,(H,28,30,31)
|
| Chemical Name |
8-[(5-amino-1,3-dioxan-2-yl)methyl]-6-[2-chloro-4-(3-fluoropyridin-2-yl)phenyl]-2-(methylamino)pyrido[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 : 66.67 mg/mL (134.17 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 5 mg/mL (10.06 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
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 corn oil and mix evenly. Solubility in Formulation 2: ≥ 4.5 mg/mL (9.06 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 45.0 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 | 2.0124 mL | 10.0620 mL | 20.1240 mL | |
| 5 mM | 0.4025 mL | 2.0124 mL | 4.0248 mL | |
| 10 mM | 0.2012 mL | 1.0062 mL | 2.0124 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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