FLT3-IN-43
FLT3-IN-43 is an orally active inhibitor of tubulin and FLT3 kinase, with an IC50 of 3.6 μM against tubulin and an IC50 of 58.6 nM against human FLT3 kinase. FLT3-IN-43 binds to the colchicine-binding site on tubulin to inhibit microtubule polymerization. FLT3-IN-43 suppresses FLT3 kinase activity. FLT3-IN-43 disrupts the cellular microtubule network. Tubulin-IN-69 induces cell cycle arrest. Tubulin-IN-69 induces tumor cell apoptosis. FLT3-IN-43 is used for research on acute myeloid leukemia and solid tumors including colorectal cancer, lung adenocarcinoma, and breast cancer.
For research use only. We do not sell to patients.
- Formula: C20H20N4O3
- Molecular Weight:364.40
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[1]|
tubulin 3.6 μM (IC50) |
FLT3 58.6 nM (IC50) |
Cellular Effect
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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | IC50 |
0.015 μM
|
Antiproliferative activity against human HCT116 colorectal carcinoma cells assessed by MTT assay after 72 h incubation.
Antiproliferative activity against human HCT116 colorectal carcinoma cells assessed by MTT assay after 72 h incubation.
|
42571759 |
| A549 | IC50 |
0.021 μM
|
Antiproliferative activity against human A549 lung adenocarcinoma cells assessed by MTT assay after 72 h incubation.
Antiproliferative activity against human A549 lung adenocarcinoma cells assessed by MTT assay after 72 h incubation.
|
42571759 |
| MDA-MB-231 | IC50 |
0.025 μM
|
Antiproliferative activity against human MDA-MB-231 breast carcinoma cells assessed by MTT assay after 72 h incubation.
Antiproliferative activity against human MDA-MB-231 breast carcinoma cells assessed by MTT assay after 72 h incubation.
|
42571759 |
| MOLM-13 | IC50 |
3.3 nM
|
Antiproliferative activity against FLT3-ITD mutant MOLM-13 leukemia cells assessed by MTT assay after 72 h incubation.
Antiproliferative activity against FLT3-ITD mutant MOLM-13 leukemia cells assessed by MTT assay after 72 h incubation.
|
42571759 |
| MV4-11 | IC50 |
6.3 nM
|
Antiproliferative activity against FLT3-ITD mutant MV4-11 leukemia cells assessed by MTT assay after 72 h incubation.
Antiproliferative activity against FLT3-ITD mutant MV4-11 leukemia cells assessed by MTT assay after 72 h incubation.
|
42571759 |
| HL-60 | IC50 |
9.9 nM
|
Antiproliferative activity against FLT3 wild-type HL60 leukemia cells assessed by MTT assay after 72 h incubation.
Antiproliferative activity against FLT3 wild-type HL60 leukemia cells assessed by MTT assay after 72 h incubation.
|
42571759 |
In Vitro
FLT3-IN-43 (compound 6h) (15-25 nM; 72 h) exhibits nanomolar antiproliferative potency against HCT116, A549, and MDA-MB-231 human solid tumor cell lines, with IC50 values ranging from 15 nM to 25 nM[1].
FLT3-IN-43 (72 h) exhibits exceptionally potent antiproliferative activity against FLT3-driven leukemia cell lines, with no observable toxicity to normal human PBMC at concentrations up to 10 μM[1].
FLT3-IN-43 potently inhibits in vitro tubulin polymerization with an IC50 of 3.6 μM[1].
FLT3-IN-43 (1-10 μM; 2 h, 1.5 h) specifically occupies the colchicine binding site on tubulin in HCT116 cells[1].
FLT3-IN-43 (15-30 nM; 24 h) disrupts the cellular microtubule network of HCT116 cells in a concentration-dependent manner, inducing perinuclear contraction of microtubule structures[1].
FLT3-IN-43 40 min) is a potent, highly selective FLT3 kinase inhibitor with an IC50 of 58.6 nM, showing minimal inhibitory activity against the off-target homologous kinases c-KIT, PDGFRα, and PDGFRβ[1].
FLT3-IN-43 (15-60 nM; 8 h) effectively inhibits the FLT3 signaling pathway in MOLM-13 cells through concentration-dependent reduction of phosphorylated FLT3 and phosphorylated STAT5 protein levels[1].
FLT3-IN-43 (5-15 nM; 12-24 h) produces a sequential, time-dependent dual phase arrest phenotype in MOLM-13 cells, with early 12 h G2/M arrest characteristic of tubulin inhibition, transitioning to 24 h G0/G1 arrest characteristic of FLT3 kinase inhibition[1].
FLT3-IN-43 (5-30 nM; 24 h) induces robust, concentration-dependent apoptosis in MOLM-13 leukemia cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT116 human colorectal carcinoma cells
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Concentration:15 nM; 30 nM
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Incubation Time:24 h
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Result:Resulted in partial collapse of the microtubule network with residual microtubule structures visible around cell nuclei at 15 nM.
Caused further disruption, with only sparse residual perinuclear microtubule structures remaining at 30 nM, producing a microtubule reorganization pattern identical to that observed with 30 nM colchicine.
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Cell Line:FLT3-ITD mutant MOLM-13 human acute myeloid leukemia cells
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Concentration:15 nM; 30 nM; 60 nM
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Incubation Time:8 h
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Result:Suppressed FLT3 phosphorylation and downstream STAT5 phosphorylation in MOLM-13 cells in a clear dose-dependent manner, an effect not observed for the pure tubulin inhibitor colchicine.
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Cell Line:FLT3-ITD mutant MOLM-13 human acute myeloid leukemia cells
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Concentration:5 nM; 10 nM; 15 nM
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Incubation Time:12 h; 24 h
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Result:Increased the proportion of MOLM-13 cells arrested at the G2/M phase from 14.83% in untreated control cells to 41.50% after 12 h of treatment.
Increased the proportion of cells arrested at the G0/G1 phase from 56.96% in untreated control cells to 77.00% after 24 h of treatment.
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Cell Line:FLT3-ITD mutant MOLM-13 human acute myeloid leukemia cells
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Concentration:5 nM; 15 nM; 30 nM
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Incubation Time:24 h
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Result:Increased the percentage of apoptotic MOLM-13 cells in a concentration-dependent manner, raising the apoptosis rate from 1.62% in vehicle control cells to 3.29% at 5 nM, 30.78% at 15 nM, and 49.06% at 30 nM.
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude mice (4-week-old female)[1]
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Dosage:15 mg/kg; 30 mg/kg
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Administration:p.o.; once daily; 21 consecutive days
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Result:Achieved 63% inhibition of tumor growth at 30 mg/kg dose relative to the vehicle control group.
Showed no notable body weight loss in any treatment group relative to the control.
Revealed no significant pathological lesions or notable organ toxicity in H&E stained histopathological sections of heart, liver, and kidney tissues under the experimental conditions.
Chemical Information
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Molecular Weight 364.40
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Formula C20H20N4O3
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SMILES
COC1=C(OC)C(OC)=CC(NC2=NNC(C3=CC=CC4=C3C=CN4)=C2)=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)