| 生物活性 | FLT3/D835Y-IN-1 (compound 13a) is a orally active, potent and selectiveFLT3andFLT3/D835Yinhibitor, withIC50values 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)[1]. |
| IC50& TargetFLT3/D835Y | |
体外研究
(In Vitro) | 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].
Cell Proliferation Assay | Cell Line: | Ba/F3-FLT3-ITD, Ba/F3-FLT3-ITD/D835Y, and Ba/F3-FLT3-ITD-F691L cell lines, AML cells[1] | | Concentration: | 100 nM | | Incubation Time: | 3 h | | Result: | Inhibited Ba/F3-FLT3-ITD, Ba/F3-FLT3-ITD/D835Y, Ba/F3-FLT3-ITD-F691L, MV4-11, MOLM14, and MOLM14-ITD/D835Y proliferation, withGI50values of 0.59, 0.73, 5.54, 1.30, 6.20, and 4.58 nM, respectively. |
Western Blot Analysis | Cell Line: | MOLM14-ITD/D835Y and MOLM14-ITD/F691L cells[1]. | | Concentration: | 3, 10, and 30 nM | | Incubation Time: | 16 h | | Result: | Significantly inhibited the FLT3, AKT, ERK, and STAT5 pathways at lower dosages. |
|
体内研究
(In Vivo) | 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[1].
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 |
| Animal Model: | NOD/SCID mice (6 weeks, male, nine mice per group)[1] | | 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)[1] | | 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. |
|
| 分子量 | |
| Formula | |
| CAS 号 | |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
