2. Protein Tyrosine Kinase/RTK
  3. FLT3
  4. 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。

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FLT3-IN-15 Chemical Structure

FLT3-IN-15 Chemical Structure

CAS No. : 2435562-99-3

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FLT3-IN-15 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

FLT3-IN-15 相关抗体:

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

MCE 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

443.90

Formula

C22H23ClFN5O2
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.
纯度 & 产品资料
参考文献

FLT3-IN-15 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

FLT3-IN-152435562-99-3FLT3Cluster of differentiation antigen 135CD135Fms like tyrosine kinase 3Acute myeloid leukemiaOrally activeAnti-proliferativeMOLM14MV4-11Inhibitorinhibitorinhibit

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