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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 |
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是否有货 |
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| 100 mg |
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询价 |
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| 250 mg |
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询价 |
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| 500 mg |
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询价 |
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* 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].
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IC50 & Target |
IC50: 0.87 nM (FLT3), 0.32 nM (FLT3/D835Y)[1]
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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: |
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| 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. |
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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].
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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) |
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158.7 ± 98.7 |
| VSS (L/kg) |
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127891 ± 104764 |
| Cmax (ng/mL) |
36.5 ± 24.3 |
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| Tmax (min) |
390.0 ± 366.0 |
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| Xu, 24h (%) |
0.001 ± 0.0 |
0.002 ± 0.002 |
| GI24h (%) |
0.05 ± 0.05 |
0.24 ± 0.02 |
| F (%) |
42.9 |
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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%. |
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| 分子量 |
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| Formula |
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| CAS 号 |
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis.
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| 参考文献 |
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[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.
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