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| Targets |
FN-1501 targets FLT3 (FMS-like tyrosine kinase 3) and cyclin-dependent kinases (CDKs) CDK2, CDK4, and CDK6. FLT3 is a receptor tyrosine kinase frequently mutated in acute myeloid leukemia (AML). CDKs are key regulators of the cell cycle. By simultaneously inhibiting these targets, FN-1501 blocks cell cycle progression and survival signals in cancer cells.
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| ln Vitro |
FN-1501 is a strong FLT3 and CDK paradigm, with IC50 values for CDK2/cyclin A, CDK4/cyclin D1, CDK6/cyclin D1, and FLT3 being 2.47 ± 0.21, 0.85 ± 0.28, 1.96 ± 0.08, and 0.28 ± FN, respectively. With GI50 values of 0.37±0.04, 0.05±0.01, 2.84±0.25, and 0.09±0.04, respectively, -1501 has potent inhibitory activity against a range of tumor cells, including MGC803, RS4 11, MCF-7, HCT-116, and NCI-H82. 0.11 ± 0.02 nM[1].
In vitro, FN-1501 is a highly potent inhibitor of its targets, with IC50 values in the low nanomolar range. It shows potent antiproliferative effects against cancer cell lines. It also exhibits little cytotoxicity against normal lymphocyte cells, with an LD50 of 185.67 mg/kg in ICR mice. These results confirm its potent antitumor activity and favorable selectivity. |
| ln Vivo |
FN-1501 exhibits strong anti-tumor efficacy, virtually minimal cytotoxicity to the healthy oral cavity, and a lethal dose-range of 185.67 mg/kg in ICR mice. The growth of MV4-11 cell xenograft tumors is rotationally inhibited by FN-1501 (15.30, or 40 mg/kg/d, iv) [1].
In vivo, FN-1501 has demonstrated antitumor activity in preclinical models. It has been studied in xenograft models, where it inhibits tumor growth. Its antitumor activity, combined with its low toxicity to normal cells, makes it a promising candidate for cancer therapy. |
| Enzyme Assay |
In vitro enzyme assays for FN-1501 measure its inhibition of CDK2/cyclin A, CDK4/cyclin D1, CDK6/cyclin D1, and FLT3 kinase activities. The compound is incubated with each kinase and a peptide substrate in the presence of ATP. The IC50 values are determined from dose-response curves.
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| Cell Assay |
In vitro cell-based assays for FN-1501 assess its antiproliferative effects on cancer cell lines. Cells are treated with varying concentrations of the compound, and cell viability is measured (e.g., MTT assay). Its effects on cell cycle progression and apoptosis are analyzed by flow cytometry. Its cytotoxicity on normal lymphocytes is also assessed.
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| Animal Protocol |
In vivo animal experiments for FN-1501 have been conducted in mouse xenograft models. Tumor-bearing mice are treated with FN-1501, and tumor growth inhibition is monitored. The LD50 of 185.67 mg/kg in ICR mice has been reported.
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| ADME/Pharmacokinetics |
FN-1501 has a molecular weight of 431.49 and a molecular formula of C22H25N9O. It is a solid compound typically stored at -20°C. Its purity is ≥98%. It is soluble in DMSO.
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| Toxicity/Toxicokinetics |
FN-1501 has low toxicity on normal lymphocyte cells (LD50: 185.67 mg/kg in ICR mice). As a potent kinase inhibitor, its toxicity profile is being evaluated in preclinical studies. Standard safety precautions should be taken when handling this compound.
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| References | |
| Additional Infomation |
FN-1501, a CDK2/4/6/FLT3 inhibitor, is a small-molecule multi-kinase inhibitor that inhibits cyclin-dependent kinase (CDK) isoforms 2 (CDK2), 4 (CDK4), and 6 (CDK6), as well as FMS-associated tyrosine kinases 3 (FLT3, FLK2, STK1), exhibiting potential antitumor activity. After intravenous injection, FN-1501 binds to and inhibits the activity of CDK2, CDK4, CDK6, and FLT3. This may induce apoptosis and inhibit cancer cell proliferation, particularly in cancer cells overexpressing these kinases. CDKs are serine/threonine kinases involved in cell cycle regulation and cell proliferation. FLT3 is a class III tyrosine kinase receptor that is overexpressed or mutated in various cancers.
FN-1501 is a potent inhibitor of FLT3 and CDK2/4/6, with IC50 values in the low nanomolar range. It has potent antitumor activity and little cytotoxicity on normal cells. FN-1501 disrupts cell cycle progression and induces apoptosis by targeting key regulators of cell division and survival. It is a research compound with potential applications in cancer therapy. |
| Molecular Formula |
C22H25N9O
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| Molecular Weight |
431.493602514267
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| Exact Mass |
431.218
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| CAS # |
1429515-59-2
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| PubChem CID |
72195175
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| Appearance |
White to off-white solid powder
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| LogP |
2.2
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
32
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| Complexity |
621
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(C1=C(C=NN1)NC1=C2C=CNC2=NC=N1)NC1C=CC(=CC=1)CN1CCN(C)CC1
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| InChi Key |
VXLAKHWYGRKCGI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H25N9O/c1-30-8-10-31(11-9-30)13-15-2-4-16(5-3-15)27-22(32)19-18(12-26-29-19)28-21-17-6-7-23-20(17)24-14-25-21/h2-7,12,14H,8-11,13H2,1H3,(H,26,29)(H,27,32)(H2,23,24,25,28)
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| Chemical Name |
N-[4-[(4-methylpiperazin-1-yl)methyl]phenyl]-4-(7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-1H-pyrazole-5-carboxamide
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| Synonyms |
FN1501; FN 1501; FN-1501
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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 |
| 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 : ≥ 50 mg/mL (~115.88 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.79 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 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 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to 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 (5.79 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 ultrasonication. 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 | 2.3176 mL | 11.5878 mL | 23.1755 mL | |
| 5 mM | 0.4635 mL | 2.3176 mL | 4.6351 mL | |
| 10 mM | 0.2318 mL | 1.1588 mL | 2.3176 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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