1. Cell Cycle/DNA Damage
    Protein Tyrosine Kinase/RTK
  2. CDK
    FLT3
  3. FN-1501

FN-1501 

Cat. No.: HY-111361 Purity: 98.41%
Handling Instructions

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.

For research use only. We do not sell to patients.

FN-1501 Chemical Structure

FN-1501 Chemical Structure

CAS No. : 1429515-59-2

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 275 In-stock
Estimated Time of Arrival: December 31
5 mg USD 250 In-stock
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10 mg USD 450 In-stock
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50 mg USD 1400 In-stock
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100 mg USD 2100 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

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.

IC50 & Target[1]

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)

In Vitro

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].

In Vivo

FN-1501 exhibits potent antitumor activity, and shows little cytotoxicity on normal lymphocyte cells, with LD50 of 185.67 mg/kg in ICR mice. FN-1501 (15. 30, or 40 mg/kg/d, i.v.) dose-dependently and significantly suppresses the growth of tumor in MV4-11-cell-inoculated-xenograft mice[1].

Clinical Trial
Molecular Weight

431.49

Formula

C₂₂H₂₅N₉O

CAS No.

1429515-59-2

SMILES

O=C(C1=NNC=C1NC2=NC=NC3=C2C=CN3)NC4=CC=C(CN5CCN(C)CC5)C=C4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 50 mg/mL (115.88 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
References
Kinase Assay
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

FN-1501FN1501FN 1501CDKFLT3Cyclin dependent kinaseCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3Inhibitorinhibitorinhibit

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FN-1501
Cat. No.:
HY-111361
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