2. Protein Tyrosine Kinase/RTK
  3. FLT3
  4. 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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TTT 3002 Chemical Structure

TTT 3002 Chemical Structure

CAS No. : 871037-95-5

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TTT 3002 Related Antibodies

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Description

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[1].

In Vitro

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.

TTT 3002 Related Antibodies

Western Blot Analysis[1]

Cell Line: Molm14 and MV4-11 cells
Concentration: 0, 0.25, 0.5, 1, 2 nM
Incubation Time: 1 h
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.

Cell Cycle Analysis[1]

Cell Line: Molm14 and MV4-11 cells
Concentration: 0, 1, 2, 5, 10 nM
Incubation Time: 24 h
Result: Showed cell cycle arrest followed by marked induction of apoptosis, along with concurrent activation of caspase 3 and poly ADP ribose polymerase cleavage.
In Vivo

TTT 3002 (6 mg/kg, Oral gavage, twice per day, for 2 to 4 weeks) is effective in vivo in several mouse tumor models of FLT3/ITD-associated AML (acute myeloid leukemia) with minimal toxicity[1].
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.

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]
Dosage: 6 mg/kg
Administration: Oral gavage, twice per day, for 2 to 4 weeks
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).
Animal Model: Leukemic engrafted mice (female, age 6 to 8 weeks)[1]
Dosage: 6 mg/kg
Administration: Oral gavage, single (Pharmacokinetic Analysis)
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.
Molecular Weight

465.50

Formula

C27H23N5O3
CAS No.
SMILES

C[C@]12N3C4=C(C5=CC=CC=C35)C(CNC6=O)=C6C7=C4N(C8=CC=CC=C87)[C@](C[C@]2(N)C(NC)=O)([H])O1
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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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TTT 3002 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:

TTT 3002871037-95-5TTT3002TTT-3002FLT3Cluster of differentiation antigen 135CD135Fms like tyrosine kinase 3internal tandem duplicationITDMolm14MV4-11 cellsFLT3/ITDFLT3/PMand FLT3/WT cellInhibitorinhibitorinhibit

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