2. Protein Tyrosine Kinase/RTK PI3K/Akt/mTOR MAPK/ERK Pathway Stem Cell/Wnt
  3. VEGFR FGFR FLT3 PDGFR RET Akt ERK c-Kit
  4. VEGFR2-IN-84

VEGFR2-IN-84 是一种基于萘环骨架、口服有效的、多靶点酪氨酸激酶抑制剂。VEGFR2-IN-84 能够以亚纳摩尔级别的亲和力抑制 VEGFR2，并广泛靶向 Kit、FGFR、PDGFR 及 Ret 等激酶。VEGFR2-IN-84 通过竞争性结合 ATP 结合口袋，阻断 VEGFR2 及其下游 AKT/ERK 信号通路的磷酸化，从而显著抑制内皮细胞增殖、迁移及肿瘤血管生成。VEGFR2-IN-84 对肝癌、肺癌、肾癌等多种实体瘤具有广谱抗增殖活性，且对正常细胞毒性较弱，效力优于 Lenvatinib (HY-10981)。VEGFR2-IN-84 具有良好的药代动力学特征和较高的安全性 (LD50>2000 mg/kg)，可用于多种恶性肿瘤的相关研究。

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VEGFR2-IN-84

VEGFR2-IN-84 Chemical Structure

CAS No. : 861877-12-5

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VEGFR2-IN-84 相关抗体

Top Publications Citing Use of Products

查看 VEGFR 亚型特异性产品:

查看所有亚型
VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

查看 PDGFR 亚型特异性产品:

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PDGFR PDGFRβ PDGFRα

查看 Akt 亚型特异性产品:

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Akt Akt1 Akt2 Akt3

查看 ERK 亚型特异性产品:

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ERK ERK1 ERK2 ERK5 ERK8

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

VEGFR2-IN-84 is an orally active, multi-targeted tyrosine kinase inhibitor based on a naphthalene ring scaffold. VEGFR2-IN-84 inhibits VEGFR2 with sub-nanomolar affinity and broadly targets kinases including Kit, FGFR, PDGFR, and Ret. By competitively binding to the ATP-binding pocket, VEGFR2-IN-84 blocks the phosphorylation of VEGFR2 and its downstream AKT/ERK signaling pathway, thereby significantly inhibiting endothelial cell proliferation, migration, and tumor angiogenesis. VEGFR2-IN-84 exhibits broad-spectrum antiproliferative activity against various solid tumors such as liver cancer, lung cancer, and renal cancer, shows weak toxicity to normal cells, and has superior potency to Lenvatinib (HY-10981). VEGFR2-IN-84 possesses favorable pharmacokinetic properties and high safety (LD50>2000 mg/kg), and can be used in related studies of various malignant tumors[1].\n
IC50 & Target

VEGFR2

0.303 nM (EC50)

PDGFRα

0.742 nM (EC50)

PDGFRβ

2.12 nM (EC50)

Flt-4

1.35 nM (EC50)

FGFR1

195 nM (EC50)

FGFR2

4.43 nM (EC50)

FGFR3

28.7 nM (EC50)

Flt-1

1.61 nM (EC50)

体外研究
(In Vitro)

VEGFR2-IN-84 (E20) (4.92 nM；96 h) 显著抑制 VEGF 诱导的 HUVEC 细胞增殖，活性约为 Lenvatinib (HY-10981) 的 10 倍[1]。
VEGFR2-IN-84 (10-1000 nM；48 h) 剂量依赖性地抑制 HUVEC、A549 和 HepG2 细胞中 VEGFR2 及其下游 AKT、ERK 的磷酸化，且活性优于 Lenvatinib[1]。
VEGFR2-IN-84 (8.53-14.1 μM；72 h) 对正常细胞 LO2、HEK293T 和 BEAS-2B 的抑制活性较弱，显示出良好的肿瘤细胞选择性[1]。

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

VEGFR2-IN-84 相关抗体:

Cell Proliferation Assay[1]

Cell Line: Human umbilical vein endothelial cells (HUVECs)
Concentration: IC50
Incubation Time: 96 h
Result: Significantly inhibited hVEGF-165 (20 ng/mL)-induced proliferation of HUVECs with an IC50 value of 4.92 nM, which was over 10-fold more potent than lenvatinib (IC50=51.2 nM).

Western Blot Analysis[1]

Cell Line: HUVECs, A549 cells, HepG2 cells
Concentration: 10 nM, 1000 nM
Incubation Time: 48 h
Result: Dose-dependently suppressed hVEGF-165 (50 ng/mL)-induced phosphorylation of VEGFR2 (Tyr1175), AKT (Ser473), and ERK1/2 (Thr202/Tyr204) in HUVECs.
Significantly reduced p-VEGFR2 and p-ERK levels.
Dose-dependently inhibited the phosphorylation of VEGFR2, AKT, and ERK in A549 and HepG2 cells, and exhibited more potent inhibitory effects than lenvatinib at the same concentrations.
体内研究
(In Vivo)

VEGFR2-IN-84 (E20) (50 mg/kg；灌胃；每日一次；21 天) 在雄性 BALB/c 裸鼠 HepG2 肝癌异种移植模型中，显著抑制肿瘤生长，优于同剂量 Lenvatinib (HY-10981)，且无明显体重下降[1]。
VEGFR2-IN-84 (30-60 mg/kg；灌胃；每日一次；20-30 天) 在雄性 BALB/c 裸鼠 A549 肺癌、786-O 肾细胞癌、8305C 甲状腺癌异种移植模型中，分别剂量依赖性抑制肿瘤生长，均优于同剂量 Lenvatinib[1]。
VEGFR2-IN-84 (2 mg/kg；尾静脉注射；单次；24 h) 在健康 ICR 小鼠中具有中等消除半衰期 (T1/2=5.05 h) 和血浆暴露量 (AUC0-∞=1970 ng・h/mL)[1]。

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

Animal Model: Male BALB/c nude mice (4-5 weeks old, 15-17 g), HepG2 hepatocellular carcinoma subcutaneous xenograft model[1]
Dosage: 50 mg/kg
Administration: Intragastric (p.o.) administration, once daily (qd)
Result: Significantly inhibited the growth of HepG2 xenografts with a tumor growth inhibition (TGI) rate of 94.3%, which was superior to lenvatinib (TGI=83.6%) at the same dose.
No significant body weight loss or overt signs of toxicity were observed throughout the experimental period.
Animal Model: Male BALB/c nude mice (4-5 weeks old, 15-17 g), A549 non-small cell lung cancer subcutaneous xenograft model[1]
Dosage: 30 mg/kg or 60 mg/kg
Administration: Intragastric (p.o.) administration, once daily (qd)
Result: Exhibited dose-dependent antitumor activity.
At 30 mg/kg, the TGI rate was 76.9%, which was superior to lenvatinib (TGI=61.3%) at the same dose.
At 60 mg/kg, achieved a TGI rate of 95.7%, significantly outperforming lenvatinib (TGI=84.6%).
No significant body weight loss was observed.
分子量

470.50

Formula

C25H18N4O4S
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

VEGFR2-IN-84 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:

VEGFR2-IN-84861877-12-5VEGFRFGFRFLT3PDGFRRETAktERKc-KitVascular endothelial growth factor receptorFibroblast growth factor receptorCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3Platelet-derived growth factor receptorPKBProtein kinase BExtracellular signal regulated kinasesSCFRCD117VEGFR2FGFR2KitPDGFRαFlt4RetFlt1PDGFRβAKTFGFR3Inhibitorinhibitorinhibit

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