产品
编 号：F754356
分子式：C22H21N5O3
分子量：403.43
分子式：C22H21N5O3
分子量：403.43
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CAS No: 2648799-49-7
产品详情
生物活性：
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).
体内研究：
FLT3/D835Y-IN-1 (10 mg/kg, IP, daily, 6 days per week) significantly suppresses tumor growth and exhibits potent antitumor activity against MOLM14-ITD/D835Y cells.FLT3/D835Y-IN-1 (10 mg/kg, IV or Orally, single) displays extremely low AUC and high clearance.Pharmacokinetic Parameters of FLT3/D835Y-IN-1 in ICR mice.Parameters13a
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
Animal Model:NOD/SCID mice (6 weeks, male, nine mice per group)
Dosage:10 mg/kg
Administration:IP, daily, 6 days per week, from day 7 to day 29
Result:Significantly suppressed tumor growth.
Animal Model:ICR mice (7–8 weeks, male)
Dosage:10 mg/kg, dissolved in a solution (10% DMSO, 40% PEG400, and 50% PBS)
Administration:IV or Orally, single (Pharmacokinetic Analysis)
Result:Displayed extremely low AUC and high clearance.
体外研究：
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.FLT3/D835Y-IN-1 (3-30 nM, 16 h) significantly inhibit FLT3, AKT, ERK, and STAT5 pathways.
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).
体内研究：
FLT3/D835Y-IN-1 (10 mg/kg, IP, daily, 6 days per week) significantly suppresses tumor growth and exhibits potent antitumor activity against MOLM14-ITD/D835Y cells.FLT3/D835Y-IN-1 (10 mg/kg, IV or Orally, single) displays extremely low AUC and high clearance.Pharmacokinetic Parameters of FLT3/D835Y-IN-1 in ICR mice.Parameters13a
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
Animal Model:NOD/SCID mice (6 weeks, male, nine mice per group)
Dosage:10 mg/kg
Administration:IP, daily, 6 days per week, from day 7 to day 29
Result:Significantly suppressed tumor growth.
Animal Model:ICR mice (7–8 weeks, male)
Dosage:10 mg/kg, dissolved in a solution (10% DMSO, 40% PEG400, and 50% PBS)
Administration:IV or Orally, single (Pharmacokinetic Analysis)
Result:Displayed extremely low AUC and high clearance.
体外研究：
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.FLT3/D835Y-IN-1 (3-30 nM, 16 h) significantly inhibit FLT3, AKT, ERK, and STAT5 pathways.
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