FLT3-ITD-IN-4
FLT3-ITD-IN-4 is an orally active FLT3-ITD inhibitor. FLT3-ITD-IN-4 targets FLT3-ITD with an IC50 of 1.1 nM, blocking autophosphorylation and downstream STAT, AKT, and ERK signaling. FLT3-ITD-IN-4 shows weaker inhibition of wild-type FLT3, with PDGFRβ as the primary off-target, demonstrating selectivity across a broad kinase panel. FLT3-ITD-IN-4 induces cell cycle arrest, apoptosis, and DNA damage response. FLT3-ITD-IN-4 can be used for research on acute myeloid leukemia.
For research use only. We do not sell to patients.
- Formula: C27H23F3N6O5
- Molecular Weight:568.50
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
FLT3-ITD 1.1 nM (IC50) |
Akt |
STAT |
ERK |
PDGFRβ |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MOLM-13 | IC50 |
1.6 nM
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Antiproliferative activity against human MOLM-13 cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.
Antiproliferative activity against human MOLM-13 cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.
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42685470 |
| MOLM-14 | IC50 |
3.3 nM
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Antiproliferative activity against human MOLM-14 cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.
Antiproliferative activity against human MOLM-14 cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.
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42685470 |
| MV4-11 | IC50 |
2.9 nM
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Antiproliferative activity against human MV4-11 cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.
Antiproliferative activity against human MV4-11 cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.
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42685470 |
| Jurkat | IC50 |
1765 nM
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Antiproliferative activity against human Jurkat cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.
Antiproliferative activity against human Jurkat cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.
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42685470 |
| HL-60 | IC50 |
994 nM
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Antiproliferative activity against human HL-60 cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.
Antiproliferative activity against human HL-60 cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.
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42685470 |
| PBMC | IC50 |
>10000 nM
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Cytotoxicity against normal human PBMCs assessed as viability reduction incubated 72 hrs by CCK-8 assay.
Cytotoxicity against normal human PBMCs assessed as viability reduction incubated 72 hrs by CCK-8 assay.
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42685470 |
| HCT-116 | IC50 |
97541 nM
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Antiproliferative activity against human HCT-116 cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.
Antiproliferative activity against human HCT-116 cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.
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42685470 |
| T47D | IC50 |
7937 nM
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Antiproliferative activity against human T47D cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.
Antiproliferative activity against human T47D cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.
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42685470 |
| HCC827 | IC50 |
2309 nM
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Antiproliferative activity against human HCC827 cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.
Antiproliferative activity against human HCC827 cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.
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42685470 |
| A549 | IC50 |
3792 nM
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Antiproliferative activity against human A549 cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.
Antiproliferative activity against human A549 cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.
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42685470 |
| PC-9 | IC50 |
5440 nM
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Antiproliferative activity against human PC-9 cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.
Antiproliferative activity against human PC-9 cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.
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42685470 |
In Vitro
FLT3-ITD-IN-4 (0.5-100 nM; 2 h) suppresses FLT3 autophosphorylation and downstream STAT5, AKT, and ERK signaling in MOLM-13 cells, with marked p-FLT3 reduction at 5 nM and near-complete suppression at 10 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MOLM-13 cells
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Concentration:0.5, 1, 5, 10, 50, 100 nM
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Incubation Time:2 h
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Result:Concentration-dependent reduction in FLT3 autophosphorylation was observed.
p-FLT3 levels were markedly diminished at concentrations as low as 5 nM.
Phosphorylation of downstream effectors p-STAT5, p-AKT, and p-ERK was attenuated.
FLT3 phosphorylation and downstream signaling were near-completely suppressed at 10 nM.
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Cell Line:MOLM-13 cells
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Concentration:3, 10, 30, 100 nM
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Incubation Time:24 h for cell cycle analysis; 48 h for apoptosis analysis
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Result:G1 phase was 61.4% at 3 nM.
G1 phase was 73.7% at 10 nM.
G1 phase was 78.5%, S phase was 6.1%, and G2/M phase was 0.05% at 30 nM.
Sub-G1 was 14.6% at 30 nM.
G1 phase was 86.7%, S phase was 13.6%, and G2/M phase was 0.9% at 100 nM.
Total apoptotic rates were 14.0% at 3 nM, 25.1% at 10 nM, 57.5% at 30 nM, and 80.7% at 100 nM.
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 (male; 4-6 weeks old)[1]
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Dosage:2.5 mg/kg; 10 mg/kg
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Administration:p.o.; once daily; 21 consecutive days
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Result:In the MV4-11 xenograft model, FLT3-ITD-IN-4 (18p) at 2.5 mg/kg produced a final tumor volume reduction of approximately 45% compared with vehicle (TGI = 45%).
At 10 mg/kg, FLT3-ITD-IN-4 (18p) achieved a tumor growth inhibition rate of approximately 80% (TGI = 80%).
Chemical Information
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Molecular Weight 568.50
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Formula C27H23F3N6O5
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SMILES
O=C(NC1=CC(OC2=CC=C(C=C2F)NC(C3=C(NC(N3C4=CC(F)=C(F)C=C4)=O)C)=O)=CC=N1)N5CC(C5)OC
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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)
FLT3-ITD-IN-4 Related Classifications
HY-189673 Related Classifications
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