FLT3-IN-32
FLT3-IN-32 is a potent and orally active FLT3 inhibitor. FLT3-IN-32 shows high selectivity for FLT3 and efficiently inhibits FLT3-activating mutations and induces apoptosis. FLT3-IN-32 shows good tolerability in non-tumor bearing mice. FLT3-IN-32 demonstrates outstanding anti-tumor efficacy in MV4-11 bearing NOD/SCID mice, prolonging the survival noticeably. FLT3-IN-32 can be used for the research of acute myeloid leukemia.
For research use only. We do not sell to patients.
- CAS No.: 3047195-48-9
- Formula: C28H29N5O5
- Molecular Weight:515.56
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
FLT3-IN-32 (Compound 29c) (0.3-218.7 nM, 72 h) effectively inhibits the proliferation in four different Ba/F3 cell lines expressing mutant FLT3 isoforms[1].
FLT3-IN-32 shows promising (1 μM-1 M) selectivity and safety toward FLT3-ITD-positive cells[1].
FLT3-IN-32 (100-500 nM, 48 h) induces apoptosis in four different Ba/F3 cell lines expressing mutant FLT3 isoforms[1].
FLT3-IN-32 (1-50 nM, 4 h) decreases the levels of phosphorylation of FLT3 and its downstream signaling molecules (STAT5, MAPK)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Ba/F3 pMIY FLT3-ITD (NPOS), Ba/F3 pMIY FLT3 D835Y, Ba/F3 pMIY FLT3 NPOS D835Y, Ba/F3 pMIY FLT3 NPOS N 676K cells
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Concentration:0.3-218.7 nM
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Incubation Time:72 h
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Result:Showed effectively inhibition with IC50 values of 0.29 nM, 0.77 nM, 11.69 nM and 2.07nM, respectively.
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Cell Line:Ba/F3 pMIY FLT3-ITD (NPOS), Ba/F3 pMIY FLT3 D835Y, Ba/F3 pMIY FLT3 NPOS D835Y, Ba/F3 pMIY FLT3 NPOS N 676K cells
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Concentration:5, 20, 100,and 500 nM
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Incubation Time:48 h
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Result:Showed highly potent in inducing apoptotsis in FLT3 D835Y cells (54.11 %) and FLT3 NPOS N676K cells (38.43 %) at 100 nM.
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Cell Line:Ba/F3 pMIY FLT3-ITD (NPOS) cells
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Concentration:1, 5, 10, 20, and 50 nM
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Incubation Time:4 h
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Result:Decreased the levels of phosphorylation of FLT3 and its downstream signaling molecules including STAT5, MAPK and to a lesser extent also AKT in a concentration-dependent manner.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MV4-11 CDX (cell-line derived xenograft) model in non-tumor bearing NOD/SCID mice (female, 8-9 weeks)[1]
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Dosage:50 mg/kg
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Administration:Oral administration, daily for 5 days
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Result:Showed less relative body weight loss compared to Quizartinib (HY-13001) and comparable with Midostaurin (HY-10230).
Showed similarly inhibitive activity as Quizartinib (HY-13001) and much more active than Midostaurin (HY-10230).
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Animal Model:Non-tumor bearing NOD/SCID mice (female, 6-8 weeks)[1]
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Dosage:20, 50, 75 mg/kg
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Administration:Oral administration, Intraperitoneal injection (20, 50 mg/kg), 15 days
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Result:Showed good tolerability.
Chemical Information
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CAS No. 3047195-48-9
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Molecular Weight 515.56
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Formula C28H29N5O5
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SMILES
O=C(NC1=CC=C(OC(C(C(N2)=CC3=C2C=CC(O)=C3CN(C)C)=O)=C4)C4=C1)NC5=NOC(C(C)(C)C)=C5
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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)
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