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]
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HepG2 GI50
1.1 μM
Compound: 36
Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition by WST assay
Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition by WST assay
[PMID: 32272419]
K562 GI50
0.437 μM
Compound: 36
Antiproliferative activity against human K562 cells assessed as cell growth inhibition by WST assay
Antiproliferative activity against human K562 cells assessed as cell growth inhibition by WST assay
[PMID: 32272419]
MOLM-14 GI50
1.85 nM
Compound: 36
Antiproliferative activity against human MOLM14 cells harboring ITD mutant assessed as cell growth inhibition by MTT assay
Antiproliferative activity against human MOLM14 cells harboring ITD mutant assessed as cell growth inhibition by MTT assay
[PMID: 32272419]
MOLM-14 GI50
1.87 nM
Compound: 36
Antiproliferative activity against human MOLM14 cells harboring ITD/D835Y mutant assessed as cell growth inhibition by MTT assay
Antiproliferative activity against human MOLM14 cells harboring ITD/D835Y mutant assessed as cell growth inhibition by MTT assay
[PMID: 32272419]
MOLM-14 GI50
3.27 nM
Compound: 36
Antiproliferative activity against human MOLM14 cells harboring ITD/F691L mutant assessed as cell growth inhibition by MTT assay
Antiproliferative activity against human MOLM14 cells harboring ITD/F691L mutant assessed as cell growth inhibition by MTT assay
[PMID: 32272419]
MOLM-14 GI50
4.88 nM
Compound: 36
Antiproliferative activity against wild type human MOLM14 cells assessed as cell growth inhibition by MTT assay
Antiproliferative activity against wild type human MOLM14 cells assessed as cell growth inhibition by MTT assay
[PMID: 32272419]
MV4-11 GI50
1 nM
Compound: 36
Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition after 72 hrs by WST assay
Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition after 72 hrs by WST assay
[PMID: 32272419]
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

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  • 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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