FLT3/D835Y-IN-1
FLT3/D835Y-IN-1 (compound 13a) is a orally active, potent and selective FLT3 and FLT3/D835Y inhibitor, with IC50 values of 0.26 nM and 0.18 nM, respectively. FLT3/D835Y-IN-1 also blocks tumor growth, has anticancer efficacy, and can be used to research for AML (acute myeloid leukemia).
For research use only. We do not sell to patients.
- CAS No.: 2648799-49-7
- Formula: C22H21N5O3
- Molecular Weight:403.43
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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
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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FLT3/D835Y 0.18 nM (IC50) |
FLT3/D835Y-IN-1 (compound 13a) (100 nM, 3 h) potently inhibits Ba/F3-FLT3-ITD, Ba/F3-FLT3-ITD/D835Y, Ba/F3-FLT3-ITD-F691L cell lines, and AML cells proliferation[1].
FLT3/D835Y-IN-1 (3-30 nM, 16 h) significantly inhibit FLT3, AKT, ERK, and STAT5 pathways[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-FLT3-ITD, Ba/F3-FLT3-ITD/D835Y, and Ba/F3-FLT3-ITD-F691L cell lines, AML cells[1]
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Concentration:100 nM
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Incubation Time:3 h
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Result:Inhibited Ba/F3-FLT3-ITD, Ba/F3-FLT3-ITD/D835Y, Ba/F3-FLT3-ITD-F691L, MV4-11, MOLM14, and MOLM14-ITD/D835Y proliferation, with GI50 values of 0.59, 0.73, 5.54, 1.30, 6.20, and 4.58 nM, respectively.
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Cell Line:MOLM14-ITD/D835Y and MOLM14-ITD/F691L cells[1].
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Concentration:3, 10, and 30 nM
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Incubation Time:16 h
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Result:Significantly inhibited the FLT3, AKT, ERK, and STAT5 pathways at lower dosages.
FLT3/D835Y-IN-1 (10 mg/kg, IV or Orally, single) displays extremely low AUC and high clearance[1].
Pharmacokinetic Parameters of FLT3/D835Y-IN-1 in ICR mice[1].
| Parameters | 13a |
| AUClast (ng*h/mL) | 1360 ± 110 |
| CL (L/h/kg) | 6.96 ± 0.66 |
| Vss (L/kg) | 14.8 ± 0.7 |
| T1/2 (h) | 1.5 ± 0.1 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NOD/SCID mice (6 weeks, male, nine mice per group)[1]
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Dosage:10 mg/kg
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Administration:IP, daily, 6 days per week, from day 7 to day 29
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Result:Significantly suppressed tumor growth.
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Animal Model:ICR mice (7–8 weeks, male)[1]
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Dosage:10 mg/kg, dissolved in a solution (10% DMSO, 40% PEG400, and 50% PBS)
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Administration:IV or Orally, single (Pharmacokinetic Analysis)
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Result:Displayed extremely low AUC and high clearance.
Chemical Information
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CAS No. 2648799-49-7
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Molecular Weight 403.43
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Formula C22H21N5O3
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SMILES
O=C1NC2=C(C=CC=C2)/C1=C3NC4=C(C=CC=C4)C/3=N\OCC(N5CCNCC5)=O
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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/D835Y-IN-1 Related Classifications
HY-143434 Related Classifications
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