2. Protein Tyrosine Kinase/RTK Apoptosis
  3. FLT3 Apoptosis
  4. FLT3-IN-14

FLT3-IN-14 is a potent FLT3 inhibitor with IC50s of 5.6 nM and 1.4 nM for FLT3-WT and FLT3-ITD. FLT3-IN-14 reduces the phosphorylation of FLT3 (Y591), induces cell cycle arrest at G1 phase and apoptosis. FLT3-IN-14 significantly reduces the tumor growth in an MV4-11 xenograft mouse model.

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FLT3-IN-14 Chemical Structure

FLT3-IN-14 Chemical Structure

CAS No. : 2620551-45-1

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FLT3-IN-14 Related Antibodies

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Description

FLT3-IN-14 is a potent FLT3 inhibitor with IC50s of 5.6 nM and 1.4 nM for FLT3-WT and FLT3-ITD. FLT3-IN-14 reduces the phosphorylation of FLT3 (Y591), induces cell cycle arrest at G1 phase and apoptosis. FLT3-IN-14 significantly reduces the tumor growth in an MV4-11 xenograft mouse model[1].

IC50 & Target

IC50: 1.4 nM (FLT-ITD), 5.6 nM (FLT3-WT)[1]
In Vitro

FLT3-IN-14 (compound 9c) (0-10 μM; 24 hours) inhibits the proliferation of tested twelve haematological cell lines with IC50s of 0.011-1.582 μM[1].
FLT3-IN-14 (0-10 μM; 72 hours) exhibits low toxicity, with GI50 greater than 10 μM, in resting lymphocytes[1].
FLT3-IN-14 (1-50 nM; 24 and 48 hours) accumulates annexin-V positive cells in a concentration and time-dependent manner[1].
FLT3-IN-14 (25-100 nM; 24 and 48 hours) induces a significant G1 arrest in both cell lines[1].
FLT3-IN-14 (1-50 nM; 24 hours) induces the dephosphorylation of FLT3[1].

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

FLT3-IN-14 Related Antibodies

Cell Proliferation Assay

Cell Line: MOLT-4 , HL-60, KG-1, KG-1a, MOLM-13, MV4-11, NOMO-1, OCI-AML2, PL-21, THP-1, K-562, KCL-22[1]
Concentration: 0-10 μM
Incubation Time: 24 hours
Result: Inhibited the proliferation of these twelve haematological cell lines with IC50s of 0.011-1.582 μM.

Cell Cytotoxicity Assay

Cell Line: PBL[1]
Concentration: 0-10 μM
Incubation Time: 72 hours
Result: Exhibited low toxicity, with GI50 greater than 10 μM, in resting lymphocytes.

Apoptosis Analysis

Cell Line: MV4-11[1]
Concentration: 1, 10 and 50 nM
Incubation Time: 24 and 48 hours
Result: Accumulated annexin-V positive cells in a concentration and time-dependent manner.

Cell Cycle Analysis

Cell Line: MOLM-13 and MV-14[1]
Concentration: 25, 50, 75 and 100 nM
Incubation Time: 24 and 48 hours
Result: Induced a significant G1 arrest in both cell lines.

Western Blot Analysis

Cell Line: MV-14[1]
Concentration: 1, 10 and 50 nM
Incubation Time: 24 hours
Result: Induced the dephosphorylation of FLT3.
In Vivo

FLT3-IN-14 (1.0 and 3.0 mg/kg; IP; daily for 28 days) significantly reduces tumor growth in a dose-dependent manner without sign of toxicity[1].

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

Animal Model: NOD/SCID female mice (subcutaneously implanted MV4-11)[1]
Dosage: 1.0 and 3.0 mg/kg
Administration: IP; daily for 28 days
Result: Significantly reduced tumor growth by 44.1% and 55.2% at 1 and 3 mg/kg, respectively.
Molecular Weight

472.56

Formula

C25H24N6O2S
CAS No.
SMILES

CC(C)(C1=CC(NC(NC2=CC=C(C=C2)C3=CN4C5=C(SC4=N3)CCC6=CNC=C65)=O)=NO1)C
Shipping

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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FLT3-IN-14 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:

FLT3-IN-142620551-45-1FLT3ApoptosisCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3Acute myeloid leukemiaPhosphorylationCell cytotoxicityMOLM-13MV-14NOD/SCID female miceInhibitorinhibitorinhibit

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