FN-1501
Based on 2 publication(s) in Google Scholar
FN-1501 is a potent inhibitor of FLT3 and CDK, with IC50s of 2.47, 0.85, 1.96, and 0.28 nM for CDK2/cyclin A, CDK4/cyclin D1, CDK6/cyclin D1 and FLT3, respectively. FN-1501 has anticancer activity.
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- Pureté: 98.72%
- CAS No.: 1429515-59-2
- Formule: C22H25N9O
- Masse moléculaire:431.49
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) FN-1501
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Activité biologique
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Cdk4/cyclin D1 0.85 nM (IC50) |
CDK6/cyclinD1 1.96 nM (IC50) |
cdk2/cyclin A 2.47 nM (IC50) |
FLT3 0.28 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BaF3 | IC50 |
0.008 μM
Compound: FN-1501
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Antiproliferative activity against mouse BaF3 cells harboring FLT3 ITD/D835V mutant assessed as inhibition of cell growth incubated for 72 hrs
Antiproliferative activity against mouse BaF3 cells harboring FLT3 ITD/D835V mutant assessed as inhibition of cell growth incubated for 72 hrs
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[PMID: 37163951] |
| BaF3 | IC50 |
0.038 μM
Compound: FN-1501
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Antiproliferative activity against mouse BaF3 cells harboring FLT3 ITD mutant assessed as inhibition of cell growth incubated for 72 hrs
Antiproliferative activity against mouse BaF3 cells harboring FLT3 ITD mutant assessed as inhibition of cell growth incubated for 72 hrs
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[PMID: 37163951] |
| BaF3 | IC50 |
0.039 μM
Compound: FN-1501
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Antiproliferative activity against mouse BaF3 cells harboring FLT3 D835V mutant assessed as inhibition of cell growth incubated for 72 hrs
Antiproliferative activity against mouse BaF3 cells harboring FLT3 D835V mutant assessed as inhibition of cell growth incubated for 72 hrs
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[PMID: 37163951] |
| BaF3 | IC50 |
0.056 μM
Compound: FN-1501
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Antiproliferative activity against mouse BaF3 cells harboring FLT3 ITD/F691L mutant assessed as inhibition of cell growth incubated for 72 hrs
Antiproliferative activity against mouse BaF3 cells harboring FLT3 ITD/F691L mutant assessed as inhibition of cell growth incubated for 72 hrs
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[PMID: 37163951] |
| BaF3 | IC50 |
0.073 μM
Compound: FN-1501
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Antiproliferative activity against mouse BaF3 cells harboring FLT3 ITD/N676D mutant assessed as inhibition of cell growth incubated for 72 hrs
Antiproliferative activity against mouse BaF3 cells harboring FLT3 ITD/N676D mutant assessed as inhibition of cell growth incubated for 72 hrs
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[PMID: 37163951] |
| BaF3 | IC50 |
0.155 μM
Compound: FN-1501
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Cytotoxicity against mouse BaF3 cells assessed as inhibition of cell growth incubated for 72 hrs
Cytotoxicity against mouse BaF3 cells assessed as inhibition of cell growth incubated for 72 hrs
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[PMID: 37163951] |
| BaF3 | IC50 |
7.65 nM
Compound: 4; FN.1501
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Antiproliferative activity against mouse BaF3 cells harboring FLT3-ITD-F691L mutant assessed as reduction in cell viability incubated for 72 hrs by CellTiterGlo luminescent assay
Antiproliferative activity against mouse BaF3 cells harboring FLT3-ITD-F691L mutant assessed as reduction in cell viability incubated for 72 hrs by CellTiterGlo luminescent assay
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[PMID: 34550682] |
| BT-474 | IC50 |
23939 nM
Compound: CICAMPA-07
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Cytotoxicity against human BT-474 cells incubated for 48 hrs by CCK-8 reagent microplate reader assay
Cytotoxicity against human BT-474 cells incubated for 48 hrs by CCK-8 reagent microplate reader assay
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[PMID: 36827953] |
| HCT-116 | GI50 |
0.09 μM
Compound: 50; FN-1501
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Growth inhibition of human HCT116 cells after 72 hrs by CellTiter-Glo assay
Growth inhibition of human HCT116 cells after 72 hrs by CellTiter-Glo assay
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[PMID: 29357250] |
| HL-60 | IC50 |
770.1 nM
Compound: FN-1501
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Antiproliferative activity against human HL-60 cells expressing low level wild type FLT3 assessed as inhibition of cell growth
Antiproliferative activity against human HL-60 cells expressing low level wild type FLT3 assessed as inhibition of cell growth
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[PMID: 37163951] |
| HL-60 | IC50 |
89.33 nM
Compound: FN-1501
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Antiproliferative activity against human HL-60 cells measured after 1 to 3 days by CCK-8 assay
Antiproliferative activity against human HL-60 cells measured after 1 to 3 days by CCK-8 assay
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[PMID: 38878515] |
| K562 | IC50 |
795.1 nM
Compound: FN-1501
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Antiproliferative activity against human K562 cells deficit of oncogenic FLT3 assessed as inhibition of cell growth
Antiproliferative activity against human K562 cells deficit of oncogenic FLT3 assessed as inhibition of cell growth
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[PMID: 37163951] |
| Lymphocyte | IC50 |
0.492 μM
Compound: 50; FN-1501
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Cytotoxicity against human lymphocytes assessed as decrease in cell viability after 72 hrs by MTT assay
Cytotoxicity against human lymphocytes assessed as decrease in cell viability after 72 hrs by MTT assay
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[PMID: 29357250] |
| MCF7 | GI50 |
2.84 μM
Compound: 50; FN-1501
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Growth inhibition of human MCF7 cells after 72 hrs by CellTiter-Glo assay
Growth inhibition of human MCF7 cells after 72 hrs by CellTiter-Glo assay
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[PMID: 29357250] |
| MGC-803 | GI50 |
0.37 μM
Compound: 50; FN-1501
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Growth inhibition of human MGC803 cells after 72 hrs by CellTiter-Glo assay
Growth inhibition of human MGC803 cells after 72 hrs by CellTiter-Glo assay
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[PMID: 29357250] |
| MOLM-13 | IC50 |
5.4 nM
Compound: FN-1501
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Antiproliferative activity against human MOLM-13 cells harboring FLT3 ITD mutant assessed as inhibition of cell growth
Antiproliferative activity against human MOLM-13 cells harboring FLT3 ITD mutant assessed as inhibition of cell growth
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[PMID: 37163951] |
| MV4-11 | IC50 |
0.004 μM
Compound: 3; FN-1501
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Synergistic antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability after 72 hrs in presence vorinostat by CellTiterGlo assay
Synergistic antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability after 72 hrs in presence vorinostat by CellTiterGlo assay
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[PMID: 37659198] |
| MV4-11 | IC50 |
0.007 μM
Compound: 3; FN-1501
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Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability after 72 hrs by CellTiterGlo assay
Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability after 72 hrs by CellTiterGlo assay
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[PMID: 37659198] |
| MV4-11 | IC50 |
0.007 μM
Compound: FN-1501
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Antiproliferative activity against human MV4-11 cells harboring FLT3 ITD mutant assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo luminescent assay
Antiproliferative activity against human MV4-11 cells harboring FLT3 ITD mutant assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo luminescent assay
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[PMID: 37163951] |
| MV4-11 | IC50 |
0.008 μM
Compound: 50; FN-1501
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Growth inhibition of human MV4-11 cells after 72 hrs by CellTiter-Glo assay
Growth inhibition of human MV4-11 cells after 72 hrs by CellTiter-Glo assay
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[PMID: 29357250] |
| MV4-11 | IC50 |
6.38 nM
Compound: 4; FN.1501
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Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 72 hrs by CellTiterGlo luminescent assay
Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 72 hrs by CellTiterGlo luminescent assay
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[PMID: 34550682] |
| MV4-11 | IC50 |
7.02 nM
Compound: 3; FN-1501
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Antiproliferative activity against human MV4-11 cells expressing FLT3 ITD mutant assessed as inhibition of cell viability incubated for 72 hrs by Cell Titer Glo assay
Antiproliferative activity against human MV4-11 cells expressing FLT3 ITD mutant assessed as inhibition of cell viability incubated for 72 hrs by Cell Titer Glo assay
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[PMID: 38387337] |
| NCI-H82 | GI50 |
0.11 μM
Compound: 50; FN-1501
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Growth inhibition of human NCI-H82 cells after 72 hrs by CellTiter-Glo assay
Growth inhibition of human NCI-H82 cells after 72 hrs by CellTiter-Glo assay
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[PMID: 29357250] |
| NCI-H929 | IC50 |
0.58 μM
Compound: 55
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Cytotoxicity against human NCI-H929 cells assessed as reduction in cell viability measured after 96 hrs by CellTiter-Glo luminescent assay
Cytotoxicity against human NCI-H929 cells assessed as reduction in cell viability measured after 96 hrs by CellTiter-Glo luminescent assay
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[PMID: 38071792] |
| PBMC | IC50 |
126.3 nM
Compound: FN-1501
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Cytotoxicity against human PBMC cells assessed as inhibition of cell growth
Cytotoxicity against human PBMC cells assessed as inhibition of cell growth
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[PMID: 37163951] |
| PC-3 | IC50 |
0.69 μM
Compound: FN-1501
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Antiproliferative activity against AR-negative human PC3 cells assessed as reduction in cell viability after 5 days by CCK8 assay
Antiproliferative activity against AR-negative human PC3 cells assessed as reduction in cell viability after 5 days by CCK8 assay
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[PMID: 31846828] |
| RPMI-8226 | IC50 |
3.17 μM
Compound: 55
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Cytotoxicity against human RPMI-8226 cells assessed as reduction in cell viability measured after 96 hrs by CellTiter-Glo luminescent assay
Cytotoxicity against human RPMI-8226 cells assessed as reduction in cell viability measured after 96 hrs by CellTiter-Glo luminescent assay
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[PMID: 38071792] |
| RS4-11 | GI50 |
0.05 μM
Compound: 50; FN-1501
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Growth inhibition of human RS4:11 cells after 72 hrs by CellTiter-Glo assay
Growth inhibition of human RS4:11 cells after 72 hrs by CellTiter-Glo assay
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[PMID: 29357250] |
| U-266 | IC50 |
0.78 μM
Compound: 55
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Cytotoxicity against human U-266 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
Cytotoxicity against human U-266 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
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[PMID: 38071792] |
FN-1501 is a potent inhibitor of FLT3 and CDK, with IC50s of 2.47 ± 0.21, 0.85 ± 0.28, 1.96 ± 0.08 and 0.28 ± 0.01 nM for CDK2/cyclin A, CDK4/cyclin D1, CDK6/cyclin D1 and FLT3, respectively. FN-1501 shows potent inhibitory activity against several tumor cells, such as MGC803, RS4 11, MCF-7, HCT-116, and NCI-H82, with GI50s of 0.37 ± 0.04, 0.05 ± 0.01, 2.84 ± 0.25, 0.09 ± 0.04, 0.11 ± 0.02 nM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1429515-59-2
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Appearance Solid
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Masse moléculaire 431.49
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Formule C22H25N9O
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Color White to off-white
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SMILES
O=C(C1=NNC=C1NC2=NC=NC3=C2C=CN3)NC4=CC=C(CN5CCN(C)CC5)C=C4
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Synonyms
LT-171-861
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
Solvant et solubilité
DMSO : ≥ 50 mg/mL (115.88 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.79 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (5.79 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocole
The activity of the CDKs and FLT3 are assayed in reaction buffer (20 mM HEPES pH 7.5, 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, 1% DMSO) at room temperature at a final ATP concentration of 10 mM. Then FLT3, dissolved in 100% DMSO at the indicated doses, are delivered into the kinase reaction mixture by acoustic technology and incubated for 20 min at room temperature. After 10 μM [γ-33P] ATP (specific activity 10 Ci/μL) is added to initiate the reaction, the reactions are carried out at 25°C for 120 min. The kinase activities are detected by the filterbinding method. IC50 values and curve fits are obtained by Prism[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
The human AML cell line MV4-11 is cultured in IMDM media with 10% FBS and supplemented with 2% l-glutamine and 1% penicillin/streptomycin. The MV4-11 cell line is maintained in culture media at 37°C with 5% CO2. The effects of FN-1501 on MV4-11 proliferation are performed. Cells are cultured in 96-well culture plates (10 000 cells/well). FN-1501 at various concentrations is added to the plates. Cell proliferation is determined after treatment with FN-1501 for 72 h. Cell viability is measured using the CellTiter-Glo assay, and luminescence is measured in a multilabel reader. Data are normalized to control groups (DMSO) and represented as the means of three independent measurements with standard errors of <20%. IC50 values are calculated using Prism 5.0[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[1]
Six-week-old female nu/nu mice are housed in a specific pathogen-free facility. Prior to implantation, cells are harvested during exponential growth. Five million MV4-11 cells in PBS are formulated as a 1:1 mixture with a Matrigel and injected into the subcutaneous space on the right flank of each nu/nu mouse. Daily intravenous injections are initiated when MV4-11 tumors have reached sizes of 100-200 mm3. The animals are then randomized into treatment groups of 8 mice each for the efficacy studies and dosed with FN-1501 (0, 15, 30, or 40 (mg/kg)/d) or cytarabine (50 (mg/kg)/d). The compounds (FN-1501, etc.) are dissolved in a solution of PEG400 (25%), ethanol (3.7%), glucose (5%), and acetic acid/sodium acetate buffer (pH 4.5, 7.5%). Tumor growth is measured every 3 days using Vernier calipers for the duration of the treatment. The volume is calculated as follows: tumor volume = a × b2/2, where a is the long diameter, and b is the short diameter. The percentage of tumor-growth inhibition (GI) is calculated as follows: GI = 100% × {1 - [(tumor volumefinal - tumor volumeinitial for the compound-treated group)/(tumor volumefinal - tumor volumeinitial for the vehicle-treated group)]}. The percent tumor regression (PTR) is calculated as follows: PTR = 100% × (tumor volumeinitial - tumor volumefinal)/(tumor volumeinitial)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (281 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Wang Y, et al. Discovery of 4-((7H-Pyrrolo[2,3-d]pyrimidin-4-yl)amino)-N-(4-((4-methylpiperazin-1-yl)methyl)phenyl)-1H-pyrazole-3-carboxamide (FN-1501), an FLT3- and CDK-Kinase Inhibitor with Potentially High Efficiency against Acute Myelocytic Leukemia. J Med Chem. 2018 Feb 22;61(4):1499-1518. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3176 mL | 11.5878 mL | 23.1755 mL | 57.9388 mL |
| 5 mM | 0.4635 mL | 2.3176 mL | 4.6351 mL | 11.5878 mL | |
| 10 mM | 0.2318 mL | 1.1588 mL | 2.3176 mL | 5.7939 mL | |
| 15 mM | 0.1545 mL | 0.7725 mL | 1.5450 mL | 3.8626 mL | |
| 20 mM | 0.1159 mL | 0.5794 mL | 1.1588 mL | 2.8969 mL | |
| 25 mM | 0.0927 mL | 0.4635 mL | 0.9270 mL | 2.3176 mL | |
| 30 mM | 0.0773 mL | 0.3863 mL | 0.7725 mL | 1.9313 mL | |
| 40 mM | 0.0579 mL | 0.2897 mL | 0.5794 mL | 1.4485 mL | |
| 50 mM | 0.0464 mL | 0.2318 mL | 0.4635 mL | 1.1588 mL | |
| 60 mM | 0.0386 mL | 0.1931 mL | 0.3863 mL | 0.9656 mL | |
| 80 mM | 0.0290 mL | 0.1448 mL | 0.2897 mL | 0.7242 mL | |
| 100 mM | 0.0232 mL | 0.1159 mL | 0.2318 mL | 0.5794 mL |
FN-1501 Related Classifications
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