2. Protein Tyrosine Kinase/RTK Stem Cell/Wnt JAK/STAT Signaling PI3K/Akt/mTOR MAPK/ERK Pathway Apoptosis Epigenetics Cell Cycle/DNA Damage
  3. FLT3 STAT Akt ERK Caspase PARP Bcl-2 Family Apoptosis
  4. FLC-8

FLC-8 是一种具有口服活性的 FLT3 抑制剂，对人源 FLT3-WT、FLT3-G697R 和 FLT3-N676D 的 IC50 值分别为 10.2 nM、11.6 nM 和 24.10 nM。FLC-8 抑制 FLT3 自磷酸化以及下游 STAT5、AKT 和 ERK 信号通路，并诱导急性髓系白血病 (AML) 细胞凋亡 (apoptosis)。FLC‑8 在 MV4‑11 异种移植模型中展现强效抗肿瘤活性。FLC-8 可用于急性髓系白血病的研究。

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FLC-8

FLC-8 Chemical Structure

CAS No. : 3100242-36-9

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FLC-8 相关抗体

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STAT3 STAT5 STAT6 STAT1

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PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3 Bad

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

FLC-8 is an orally active FLT3 inhibitor with IC50 values of 10.2 nM, 11.6 nM and 24.10 nM against human FLT3-WT, FLT3-G697R and FLT3-N676D, respectively. FLC-8 inhibits FLT3 autophosphorylation and downstream STAT5, AKT and ERK signaling pathways, and induces apoptosis in acute myeloid leukemia (AML) cells. FLC-8 exhibits potent antitumor activity in the MV4-11 xenograft model. FLC-8 can be used for the research of acute myeloid leukemia[1].

IC50 & Target[1]

STAT5

 

ERK

 

Akt

 

Caspase 3

 

PARP

 

Bcl-2

 

Bax

 

bad

 

体外研究
(In Vitro)

FLC-8 (给药 3.5 小时) 可强效抑制 FLT3-WT 激酶活性，其 IC50 为 10.2 nM[1]。
FLC-8 (50 μM; 24 h) 可共价结合于 FLT3 激酶结构域的 Cys807 残基[1]。
FLC-8 (72 h) 能有效抑制 MV4-11 和 MOLM-13 细胞增殖，IC50 值分别为 0.28 nM 和 2.45 nM[1]。

FLC-8 (72 h) 可强效抑制 BaF3-FLT3ITD、BaF3-FLT3ITD-G697R 和 BaF3-FLT3ITD-N676D 细胞的增殖，对应的 IC50 值分别为 3.10 nM、11.6 nM 和 24.10 nM，而对其他 FLT3 突变型 BaF3 细胞系的活性则有所降低[1]。
FLC-8 (1 μM) 表现出狭窄的激酶组抑制谱，其 S10 评分为 0.096，在 1 μM 浓度下可强效抑制 FLT3-WT、FLT3-ITD、PDGFRα、NCOA4-RET 和 RET L730I[1]。
FLC-8 (0.1-100 nM; 24 h) 可在孵育 24 h 后诱导 MV4-11 和 MOLM-13 急性髓系白血病 (AML) 细胞呈剂量依赖性 G0-G1 期阻滞[1]。
FLC-8 (0.1-100 nM; 24-72 h) 可在 24、48 和 72 h 内诱导 MV4-11 和 MOLM-13 急性髓系白血病 (AML) 细胞发生剂量依赖性凋亡[1]。
FLC-8 (0.1-30 nM) 通过激活内源性凋亡通路诱导 MV4-11 细胞发生凋亡，具体表现为促凋亡基因/蛋白表达上调、抗凋亡 BCL-2 表达下调、caspase-3 和 PARP 的剪切，以及经 TUNEL 染色检测到的 DNA 片段化[1]。
FLC-8 (0.1-30 nM; 12 h) 可在 MV4-11 细胞中以剂量依赖的方式抑制 FLT3 自磷酸化及其下游 STAT5、AKT 和 ERK 的磷酸化[1]。

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

FLC-8 相关抗体:

Cell Cycle Analysis[1]

Cell Line: MV4-11 and MOLM-13 AML cells
Concentration: 0.1, 1, 10, 100 nM
Incubation Time: 24 h
Result: Induced dose-dependent G0-G1 phase arrest in both cell lines.
Increased the G0-G1 population in MOLM-13 cells to 86.4% (from 52.0% in control) at 100 nM.
Increased the G0-G1 population in MV4-11 cells to 48.9%, 57.5%, 80.1%, and 87.0% at 0.1, 1, 10, and 100 nM respectively.

Apoptosis Analysis[1]

Cell Line: MV4-11 and MOLM-13 AML cells
Concentration: 0.1, 1, 10, 100 nM
Incubation Time: 24, 48, 72 h
Result: Induced dose-dependent apoptosis in both cell lines.
In MOLM-13 cells, apoptosis rates were 7.91-21.60% (24 h), 3.89-45.52% (48 h), and 3.69-73.90% (72 h).
In MV4-11 cells, apoptosis rates were 7.69-19.11% (24 h), 13.33-46.9% (48 h), and 7.61-71.20% (72 h).
Exceeded 70% apoptosis rates in both cell lines at 100 nM and 72 h.

Western Blot Analysis[1]

Cell Line: MV4-11 AML cells
Concentration: 0.1, 0.3, 1.0, 3.0, 10, 30 nM
Incubation Time: 12 h
Result: Potently inhibited FLT3 autophosphorylation in a dose-dependent manner, with significant suppression at 10 nM.
Reduced phosphorylation levels of STAT5, AKT, and ERK in a concentration-dependent fashion.
Exhibited superior inhibition of FLT3-mediated signaling at 30 nM compared to quizartinib.
药代动力学
(Parmacokinetics)
Species Dose Route T1/2 C0 AUC0-t AUC0-∞ MRT0-t MRT0-∞ CL Tmax Cmax F
Mice[1] 1 mg/kg i.v. 0.2 h 629.0 ng/mL 106.5 ng·h/mL 112.0 ng·h/mL 0.1 h 0.2 h 9.0 L/h/kg / / /
Mice[1] 10 mg/kg p.o. 0.6 h / 109.9 ng·h/mL 125.4 ng·h/mL 0.7 h 0.9 h / 0.3 h 120.4 ng/mL 10.3 %
体内研究
(In Vivo)

FLC-8 (腹腔注射；每日一次；连续 14 天；10-50 mg/kg) 对 MV4-11 急性髓系白血病 (AML)异种移植物展现出强效的、剂量依赖性抗肿瘤活性，在 50 mg/kg 剂量下实现 178% 的最大肿瘤生长抑制率，且安全性良好[1]。
FLC-8 (10-50 mg/kg；口服、腹腔注射；每日一次；连续 14 天) 对 BaF3-FLT3-ITD-G697R AML 异种移植瘤表现出温和的、剂量依赖性抗肿瘤活性，在 50 mg/kg 口服剂量下达到最高疗效 (TGI = 32%)[1]。
FLC-8 (1-10 μM; immersion; 24 hours) 在转基因斑马鱼中表现出良好的造血安全性，在高达 10 μM 的浓度下对中性粒细胞生成无显著抑制作用[1]。

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

Animal Model: NOD/SCID (female, 4-5 weeks old, 18-20 g, subcutaneous inoculation of MV4-11 FLT3-ITD-expressing cells)[1]
Dosage: 10 mg/kg; 25 mg/kg; 50 mg/kg
Administration: i.p.; daily; 14 days
Result: Elicited dose-dependent tumor growth inhibition with TGI values of 136%, 163%, and 178% at 10, 25, and 50 mg/kg, respectively.
Achieved inhibitory rates (IR) based on final tumor weight of 25.0%, 48.2%, and 78.6% at 10, 25, and 50 mg/kg, respectively.
Induced dose-dependent tumor cell necrosis, reduced Ki67 staining, increased TUNEL staining, and reduced phosphorylated STAT5 in tumor tissues.
Animal Model: Balb/c nude (female, 6-8 weeks old, 18-20 g, subcutaneous inoculation of BaF3-FLT3-ITD-G697R cells)[1]
Dosage: 10 mg/kg (p.o.); 50 mg/kg (p.o.); 10 mg/kg (i.p.)
Administration: p.o. (daily; 14 days); i.p. (daily; 14 days)
Result: Produced minimal tumor growth inhibition (TGI = 2%) with a tumor weight inhibitory rate of 13.4% at oral 10 mg/kg.
Improved efficacy to a TGI of 32% with a tumor weight inhibitory rate of 30.7% at oral 50 mg/kg.
Resulted in a TGI of 11% with a tumor weight inhibitory rate of 8.5% at intraperitoneal 10 mg/kg.
Animal Model: Eze-Rinka (3−4 months old)[1]
Dosage: 1 μM; 10 μM
Administration: immersion; 24 hours
Result: Did not significantly reduce neutrophil counts at either concentration when compared to the vehicle control group.
分子量

496.44

Formula

C24H19F3N6O3
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

FLC-8 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • 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:

FLC-83100242-36-9FLC8FLC 8FLT3STATAktERKCaspasePARPBcl-2 FamilyApoptosisCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3PKBProtein kinase BExtracellular signal regulated kinasespoly ADP ribose polymerase AKTAML cellsSTAT5acute myeloid leukemiaMV4-11Cys807FLT3-N676DFLT3-G697RFLT3-WTInhibitorinhibitorinhibit

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