| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
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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].
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| 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].
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| References | |
| Additional Infomation |
CDK2/4/6/FLT3 Inhibitor FN-1501 is a small molecule multi-kinase inhibitor of cyclin-dependent kinase (CDK) subtypes 2 (CDK2), 4 (CDK4), and 6 (CDK6) and FMS-related tyrosine kinase 3 (FLT3, FLK2, STK1), with potential antineoplastic activity. Upon intravenous administration, CDK2/4/6/FLT3 inhibitor FN-1501 binds to and inhibits CDK2, CDK4, and CDK6, as well as FLT3. This may induce apoptosis and inhibit tumor cell proliferation in cancer cells that overexpress these kinases. CDKs are serine/threonine kinases that assist in cell cycle regulation and cellular proliferation. FLT3, a class III tyrosine kinase receptor, is overexpressed or mutated in many cancer types.
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| 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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