上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。
FLT3-IN-15
FLT3-IN-15 是一种有效且具有口服活性的 FLT3 抑制剂,对 FLT3 和 FLT3/D835Y 的 IC50 分别为 0.87 nM 和 0.32 nM。FLT3-IN-15 可用于研究急性髓系白血病。
FLT3-IN-15 Chemical Structure
CAS No. : 2435562-99-3
规格 |
|
是否有货 |
|
100 mg |
|
询价 |
|
250 mg |
|
询价 |
|
500 mg |
|
询价 |
|
* Please select Quantity before adding items.
生物活性 |
FLT3-IN-15 is a highly potent and orally active FLT3 inhibitor with IC50s of 0.87 nM and 0.32 nM for FLT3 and FLT3/D835Y, respectively. FLT3-IN-15 can be used for researching acute myeloid leukemia[1].
|
IC50 & Target |
IC50: 0.87 nM (FLT3), 0.32 nM (FLT3/D835Y)[1]
|
体外研究 (In Vitro) |
FLT3-IN-15 (compound 36) (0-100 nM) exhibits anti-proliferative activities against MOLM14 cell lines[1]. FLT3-IN-15 (0-1 μM; 72 hours) shows extremely more sensitive against MV4-11 cells than K562 cell line, and displayed good safety profiles against other cancer cell lines[1]. FLT3-IN-15 (0.01-1 μM; 4 hours) shows strongly blockage of the phosphorylation of STAT5 and Erk1/2 in MV4-11 cells[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Proliferation Assay
Cell Line: |
MOLM14 wild type cells, MOLM14-ITD cells, MOLM14-ITD-D835Y cells, MOLM14-ITD-F691L cells[1] |
Concentration: |
0-100 nM |
Incubation Time: |
|
Result: |
Exhibited anti-proliferative activities against MOLM14 cell lines, with GI50s of 4.88 ± 0.67 nM, 1.85 ± 0.06 nM, 1.87 ± 0.36 nM and 3.27 ± 0.99 nM in MOLM14 wild type cells, MOLM14-ITD cells, MOLM14-ITD-D835Y cells and MOLM14-ITD-F691L cells, respectively. |
Cell Proliferation Assay
Cell Line: |
MV4-11, K562, A549, HepG2, MDA-MB-231, HCT-116, PC3 and SK-OV-3[1] |
Concentration: |
0-1 μM |
Incubation Time: |
72 hours |
Result: |
Showed extremely more sensitive against MV4-11 cells (GI50 = 1 nM) than K562 cell line, and displayed good safety profiles against other cancer cell lines. |
Western Blot Analysis
Cell Line: |
MV4-11[1] |
Concentration: |
10 nM, 100 nM and 1 μM |
Incubation Time: |
4 hours |
Result: |
Showed strongly blockage of the phosphorylation of STAT5 and Erk1/2. |
|
体内研究 (In Vivo) |
FLT3-IN-15 (20 mg/kg; PO; daily, for 21 days) results in the rapid and complete remission of tumors in all mice[1]. FLT3-IN-15 (2000 mg/kg; PO; single) causes one female mouse died at day 6, and the LD50 value is calculated as 4,950 mg/kg in female mice[1]. FLT3-IN-15 (10 μM) shows 21.4% inhibition of hERG ligand binding[1]. FLT3-IN-15 (10 mg/kg; PO and IV; single) exhibits an AUClast of 25.0 μg·min/mL, a Cmax of 36.5 ng/mL, and a remarkable increase in the oral bioavailability of 42.6%[1]. Pharmacokinetic Parameters of FLT3-IN-15 in male ICR mice[1].
|
PO (10 mg/kg) |
IV (10 mg/kg) |
AUClast (μg·min/mL) |
25.0 ± 11.6 |
58.5 ± 57.4 |
AUCinf (μg·min/mL) |
62.1 ± 58.6 |
103.4 ± 95.3 |
MRT (hr) |
2811.3 ± 2713.0 |
1257.1 ± 1084.1 |
T1/2 (hr) |
1775.7 ± 1901.0 |
1099.2 ± 945.8 |
CL (mL/min/kg) |
|
158.7 ± 98.7 |
VSS (L/kg) |
|
127891 ± 104764 |
Cmax (ng/mL) |
36.5 ± 24.3 |
|
Tmax (min) |
390.0 ± 366.0 |
|
Xu, 24h (%) |
0.001 ± 0.0 |
0.002 ± 0.002 |
GI24h (%) |
0.05 ± 0.05 |
0.24 ± 0.02 |
F (%) |
42.9 |
|
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model: |
BALB/c nu/nu (injected with MV4-11)[1] |
Dosage: |
20 mg/kg |
Administration: |
PO; daily, for 21 days |
Result: |
Resulted in the rapid and complete remission of tumors in all mice, and no weight loss or any other signs of toxicity during the administration period. |
Animal Model: |
Female ICR mice[1] |
Dosage: |
2000 mg/kg |
Administration: |
PO; single |
Result: |
Caused one female mouse of the 2,000 mg/kg group died at day 6 and the approximate lethal dose (ALD) is determined over 2,000 mg/kg in male mice and 2,000 mg/kg in female mice, respectively; the LD50 value was calculated as 4,950 mg/kg in female mice. |
Animal Model: |
Male ICR mice[1] |
Dosage: |
10 mg/kg |
Administration: |
PO and IV; single (Pharmacokinetics Analysis) |
Result: |
Exhibited an AUClast of 25.0 μg·min/mL, a Cmax of 36.5 ng/mL, and a remarkable increase in the oral bioavailability of 42.6%. |
|
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.
|
参考文献 |
-
[1]. Jeong P, Moon Y, Lee JH, et al. Discovery of orally active indirubin-3′-oxime derivatives as potent type 1 FLT3 inhibitors for acute myeloid leukemia. Eur J Med Chem. 2020;195:112205.
|
所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务