TTT 3002
TTT 3002 is a potent and orally active FLT3 inhibitor. TTT 3002 potently inhibits FLT3 phosphorylation by activating mutations at residue D835, with an IC50 of 0.2 nM. TTT 3002 can be used for AML (acute myeloid leukemia) research.
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- No. CAS: 871037-95-5
- Fòrmula: C27H23N5O3
- Peso molecular:465.50
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MV4-11 | IC50 |
<0.25 nM
Compound: TTT-3002
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Antiproliferative activity against human MV4-11 cells assessed as reduction in cell proliferation measured after 24 hrs by MTT assay
Antiproliferative activity against human MV4-11 cells assessed as reduction in cell proliferation measured after 24 hrs by MTT assay
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[PMID: 32659083] |
TTT 3002 downregulates FLT3 phosphorylation (pFLT3) in Molm14 and MV4-11 cells[1].
TTT 3002 induces cell cycle arrest followed by marked induction of apoptosis[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Molm14 and MV4-11 cells
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Concentration:0, 0.25, 0.5, 1, 2 nM
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Incubation Time:1 h
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Result:Downregulated FLT3 phosphorylation (pFLT3) in Molm14 and MV4-11 cells in a dose-dependent manner. The IC50 for FLT3 phosphorylation in both cell lines was six- to seven fold lower for TTT 3002 compared with Quizartinib (HY-13001) at 0.2 vs 1.3 nM, respectively.
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Cell Line:Molm14 and MV4-11 cells
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Concentration:0, 1, 2, 5, 10 nM
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Incubation Time:24 h
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Result:Showed cell cycle arrest followed by marked induction of apoptosis, along with concurrent activation of caspase 3 and poly ADP ribose polymerase cleavage.
TTT 3002 (6 mg/kg, Oral gavage, single) is rapidly absorbed with a biphasic maximum serum concentration (Cmax) followed by a monoexponential decay[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/C mice (female, age 6 to 8 weeks, received Ba/F3-ITD Luc+ cells by tail vein injection on day 0)[1]
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Dosage:6 mg/kg
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Administration:Oral gavage, twice per day, for 2 to 4 weeks
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Result:Showed no significant changes in animal weight and was sufficient to eliminate the presence of Ba/F3-ITD Luc+ cells by day 17 (10 days of treatment).
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Animal Model:Leukemic engrafted mice (female, age 6 to 8 weeks)[1]
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Dosage:6 mg/kg
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Administration:Oral gavage, single (Pharmacokinetic Analysis)
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Result:After oral administration, TTT 3002 was rapidly absorbed with a biphasic maximum serum concentration (Cmax) followed by a monoexponential decay. The Cmax and area under the concentration-time curve from time 0 to infinity (AUC0→∞) were 613 nM and 3127 nM⋅h, respectively. The half-life, apparent volume of distribution, and apparent clearance were 3.6 hours, 21 L/kg, and 4.1 L/h per kilogram, respectively.
Chemical Information
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No. CAS 871037-95-5
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Peso molecular 465.50
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Fòrmula C27H23N5O3
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SMILES
C[C@]12N3C4=C(C5=CC=CC=C53)C(CNC6=O)=C6C7=C4N([C@](C[C@]2(N)C(NC)=O)([H])O1)C8=CC=CC=C78
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
TTT 3002 Related Classifications
HY-111249 Related Classifications
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