| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| ln Vitro |
FMK-MEA is a water-soluble derivative of FMK. FMK-MEA therapy reduces RSK2 kinase activity in several highly aggressive human cancer cell lines, including 212LN, M4e, A549, and SKBR3. Treatment with the RSK-specific inhibitor FMK-MEA dramatically reduced RSK2 activity, as measured by Ser-386 phosphorylation and consequent A549 cell invasiveness [1].
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| ln Vivo |
In highly metastatic M4e cell xenograft nude mice, therapy with FMK-MEA (80 mg/kg/day intraperitoneally) for 16 days greatly reduced LN metastasis. The size and rate of primary tumor proliferation are unaffected by FMK-MEA therapy [1].
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| References | |
| Additional Infomation |
1-[4-amino-7-[3-(2-methoxyethylamino)propyl]-5-(4-methylphenyl)-6-pyrrolo[2,3-d]pyrimidinyl]-2-fluoroethyl ketone is a member of the pyrrole class of compounds.
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| Molecular Formula |
C21H26FN5O2
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|---|---|
| Molecular Weight |
399.461847782135
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| Exact Mass |
399.207
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| CAS # |
1414811-15-6
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| Related CAS # |
CMK;821794-90-5;FMK;821794-92-7
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| PubChem CID |
56965963
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| Appearance |
Brown to reddish brown solid powder
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| LogP |
2.4
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
29
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| Complexity |
517
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| Defined Atom Stereocenter Count |
0
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| SMILES |
FCC(C1=C(C2=CC=C(C)C=C2)C3=C(N)N=CN=C3N1CCCNCCOC)=O
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| InChi Key |
UPTQGXMIZXGVSC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H26FN5O2/c1-14-4-6-15(7-5-14)17-18-20(23)25-13-26-21(18)27(19(17)16(28)12-22)10-3-8-24-9-11-29-2/h4-7,13,24H,3,8-12H2,1-2H3,(H2,23,25,26)
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| Chemical Name |
1-[4-amino-7-[3-(2-methoxyethylamino)propyl]-5-(4-methylphenyl)pyrrolo[2,3-d]pyrimidin-6-yl]-2-fluoroethanone
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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 Note: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| 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 (~250.3 mM; with ultrasonication)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.26 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 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 DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and 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 (6.26 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 DMSO stock solution (25.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. 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. Solubility in Formulation 3: ≥ 2.5 mg/mL (6.26 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 DMSO stock solution (25.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5034 mL | 12.5169 mL | 25.0338 mL | |
| 5 mM | 0.5007 mL | 2.5034 mL | 5.0068 mL | |
| 10 mM | 0.2503 mL | 1.2517 mL | 2.5034 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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