2. Protein Tyrosine Kinase/RTK Stem Cell/Wnt JAK/STAT Signaling PI3K/Akt/mTOR MAPK/ERK Pathway Apoptosis
  3. FLT3 STAT Akt ERK Apoptosis
  4. FYJ-195

FYJ-195 is a potent orally active FLT3 inhibitor targeting FLT3 and its variants FLT3-ITD, FLT3-F691L, FLT3-D835V, FLT3-D835Y. FYJ-195 blocks FLT3 autophosphorylation and downstream STAT5, AKT, ERK signaling pathways, and induces apoptosis. FYJ-195 induces tumor regression in mouse acute myeloid leukemia (AML) xenograft models. FYJ-195 can be used for the research of AML.

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FYJ-195

FYJ-195 Chemical Structure

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Description

FYJ-195 is a potent orally active FLT3 inhibitor targeting FLT3 and its variants FLT3-ITD, FLT3-F691L, FLT3-D835V, FLT3-D835Y. FYJ-195 blocks FLT3 autophosphorylation and downstream STAT5, AKT, ERK signaling pathways, and induces apoptosis. FYJ-195 induces tumor regression in mouse acute myeloid leukemia (AML) xenograft models. FYJ-195 can be used for the research of AML[1].

In Vitro

FYJ-195 potently inhibits FLT3-WT, FLT3-ITD, and drug-resistant FLT3 variants (F691L, D835Y) with IC50 values ≤2.03 nM, while also showing inhibitory activity against a limited subset of other kinases including KDR and JAK1[1].
FYJ-195 potently inhibits the proliferation of FLT3-ITD-driven MOLM-13 and MV4-11 AML cells with IC50 values of 0.80 nM and 0.22 nM, respectively, while showing minimal activity against FLT3-WT, non-FLT3-dependent cancer cells, and normal cells, indicating high on-target selectivity[1].
FYJ-195 potently inhibits the proliferation of BaF3 cells transformed with FLT3-ITD and drug-resistant FLT3 mutations (N676D, D835V, D835Y, F691L) with IC50 values ranging from 0.41 nM to 9.09 nM[1].
FYJ-195 (0.1-100 nM; 24 h) dose-dependently arrests MOLM-13 and MV4-11 AML cells in the G0-G1 phase[1].
FYJ-195 (0.1-100 nM; 24-48 h) dose-dependently induces apoptosis in MOLM-13 and MV4-11 AML cells[1].
FYJ-195 (0.1-100 nM; 2-12 h) dose-dependently inhibits the FLT3-STAT5/AKT/ERK signaling pathway in FLT3-ITD-driven AML cells and FLT3 mutant-transformed BaF3 cells (including drug-resistant F691L and D835V variants), with no effect on signaling in FLT3-independent K562 cells[1].

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

FYJ-195 Related Antibodies

Cell Cycle Analysis[1]

Cell Line: MOLM-13, MV4-11 cells
Concentration: 0.1; 1; 10; 100 nM
Incubation Time: 24 h
Result: Increased the percentage of G0-G1 phase cells in MOLM-13 from 49.7% (vehicle) to 56.0% (0.1 nM), 63.6% (1 nM), 79.4% (10 nM), and 89.6% (100 nM).
Increased the percentage of G0-G1 phase cells in MV4-11 from 53.2% (vehicle) to 54.5% (0.1 nM), 72.9% (1 nM), 85.7% (10 nM), and 92.4% (100 nM).

Apoptosis Analysis[1]

Cell Line: MOLM-13, MV4-11 cells
Concentration: 0.1; 1; 10; 100 nM
Incubation Time: 24; 48 h
Result: Induced apoptosis rates in MOLM-13 of 4.39% (0.1 nM), 9.71% (1 nM), 15.32% (10 nM), and 26.2% (100 nM) after 24 h, and 5.48% (0.1 nM), 14.62% (1 nM), 36.1% (10 nM), and 60.6% (100 nM) after 48 h.
Induced apoptosis rates in MV4-11 of 5.56% (0.1 nM), 13.34% (1 nM), 20.64% (10 nM), and 25.8% (100 nM) after 24 h, and 9.13% (0.1 nM), 19.53% (1 nM), 51.66% (10 nM), and 65.43% (100 nM) after 48 h.

Western Blot Analysis[1]

Cell Line: MOLM-13, MV4-11 cells, BaF3-FLT3-ITD-F691L, BaF3-FLT3-ITD-D835V cells, FLT3-independent K562 cells
Concentration: 0.1; 0.3; 1; 3; 10; 30; 100 nM
Incubation Time: 2 h (MOLM-13/MV4-11); 12 h (BaF3/K562)
Result: Dose-dependently reduced phosphorylation of FLT3, STAT5, AKT, and ERK in MOLM-13 and MV4-11 cells, with near-complete inhibition observed at 10 nM to 30 nM.
Dose-dependently suppressed p-FLT3 and p-STAT5 in BaF3-FLT3-ITD-F691L and BaF3-FLT3-ITD-D835V cells, with complete inhibition at 100 nM (a concentration where quizartinib showed no significant activity).
Had no effect on phosphorylation of FLT3, STAT5, ERK, or AKT in K562 cells.
Parmacokinetics
Species Dose Route AUC0-t AUC0-∞ C0 T1/2 Vz CL MRT0-t MRT0-∞ Cmax Tmax Vz/F CL/F F
Mice[1] 1 mg/kg i.v. 66.9 ng·h/mL 69.4 ng·h/mL 347 ng/mL 0.539 h 11.3 L/kg 14.6 L/h/kg 0.323 h 0.412 h / / / / /
Mice[1] 10 mg/kg p.o. 23.6 ng·h/mL 24.8 ng·h/mL / 0.359 h / / 0.547 h 0.631 h 28.3 ng/mL 0.250 h 246 L/kg 535 L/h/kg 3.58 %
In Vivo

FYJ-195 (10-50 mg/kg; i.v.; daily; 14 days) induces dose-dependent tumor regression in mouse MV4-11 AML xenograft models[1].
FYJ-195 (10-50 mg/kg; i.p.; daily; 9 days) achieves robust tumor growth suppression in FLT3F691L-resistant mosue AML xenograft model[1].

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

Animal Model: NOD/SCID mice (male, 4-5 weeks old) subcutaneously injected with MV4-11 cells[1]
Dosage: 10; 25; 50 mg/kg
Administration: i.v.; daily; 14 days
Result: Induced tumor growth inhibition (TGI) of 125%, 128%, and 130% at 10, 25, and 50 mg/kg, respectively.
Achieved tumor weight inhibition rates (IR) of 90.6%, 97.6%, and 98.7% at 10, 25, and 50 mg/kg, respectively.
Reduced Ki-67 positive cells in a dose-dependent manner in tumor tissues.
Increased TUNEL-positive apoptotic cells in a dose-dependent manner in tumor tissues.
Abrogated p-STAT5 in tumor tissues.
Caused no significant body weight loss or organ pathology across doses.
Animal Model: BALB/c nude (female, 4−6 weeks old) subcutaneously injected with BaF3-FLT3-ITD-F691L cells[1]
Dosage: 10; 50 mg/kg
Administration: i.p.; daily; 9 days
Result: Induced tumor growth inhibition (TGI) of 21.3% at 10 mg/kg and 68.6% at 50 mg/kg.
Achieved tumor weight inhibition rates (IR) of 18% at 10 mg/kg and 61% at 50 mg/kg.
Caused no significant body weight loss in treated mice.
Molecular Weight

525.53

Formula

C26H26F3N7O2
SMILES

NC1=NOC2=C1C(C3=CC=C(C=C3)NC(NC4=CC(C(F)(F)F)=C(C=C4)CN5CCN(CC5)C)=O)=CC=N2
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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FYJ-195 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

FYJ-195FYJ195FYJ 195FLT3STATAktERKApoptosisCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3PKBProtein kinase BExtracellular signal regulated kinasesFLT3-D835YFLT3-ITDacute myeloid leukemiaSTAT5FLT3-F691LAKTFLT3-D835VMOLM-13Inhibitorinhibitorinhibit

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