2. Apoptosis Protein Tyrosine Kinase/RTK
  3. Apoptosis Necroptosis FGFR VEGFR PDGFR
  4. FGFR1/VEGFR2-IN-2

FGFR1/VEGFR2-IN-2 (compound 6 ) 是一种 VEGFR2/FGFR1 双重抑制剂，对 VEGFR2 和 FGFR1 的 IC50 值分别为 0.025 µM 和 0.026 µM，对 EGFR 和 PDGFR-β 的 IC50 值为 0.106 μM 和 0.077 µM。FGFR1/VEGFR2-IN-2 对 NCI-60 细胞系表现出显著抗癌活性 (GI=60.38%)，在 T-47D 细胞株中 IC50 为 8.51 µM，具有抗迁移作用，使细胞停滞于 G1 期并促进凋亡和坏死; 对 MCF-7 细胞株 IC50 超过 100 µM，对 MDA-MB-231 的 IC50 为 69.17 µM，对正常细胞无毒性。

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FGFR1/VEGFR2-IN-2 Chemical Structure

FGFR1/VEGFR2-IN-2 Chemical Structure

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FGFR1/VEGFR2-IN-2 相关抗体

Top Publications Citing Use of Products

查看 FGFR 亚型特异性产品:

查看所有亚型
FGFR FGFR1 FGFR2 FGFR3 FGFR4 FGF21

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

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

FGFR1/VEGFR2-IN-2 (compound 6l) is a VEGFR2/FGFR1 dual inhibitor. The IC50 values for VEGFR2 and FGFR1 are 0.025 µM and 0.026 µM respectively, and for EGFR and PDGFR-β, the IC50 values are 0.106 µM and 0.077 µM. FGFR1/VEGFR2-IN-2 showes significant anti-cancer activity (GI=60.38%) on NCI-60 cell line, with an IC50 of 8.51 µM in T-47D cell line and anti-migration. FGFR1/VEGFR2-IN-2 acts to arrest cells in the G1 phase and promote apoptosis and necrosis; the IC50 for MCF-7 cell line exceeds 100 µM, and the IC50 for MDA-MB-231 is 69.17 µM, non-toxic to normal cells[1].

IC50 & Target

FGFR1

0.026 μM (IC50)

VEGFR2

0.025 μM (IC50)

PDGFRβ

0.077 μM (IC50)

FGFR

0.106 μM (IC50)

体外研究
(In Vitro)

FGFR1/VEGFR2-IN-2 (10 μM) 具有抗肿瘤增殖活性，平均 GI 为 60.38%[1]。
FGFR1/VEGFR2-IN-2 对乳腺癌细胞系 T-47D，MCF-7 和 MDA-MB-231 有较好的细胞毒性，对正常细胞 Vero 没有影响[1]。
FGFR1/VEGFR2-IN-2 (10，20 μM) 将 T-47D 细胞阻滞在 G1 期[1]。
FGFR1/VEGFR2-IN-2 (2.12，4.25 μM) 促进 T-47D 细胞早期和晚期细胞凋亡，促进细胞坏死[1]。
FGFR1/VEGFR2-IN-2 (3.7-4.8 μM) 促进细胞坏死，提高了 BAX 和 Caspase-3 的表达，降低了 BCL-2 的表达[1]。
FGFR1/VEGFR2-IN-2 (6 μM；24，48 h) 在 T-47D 中有抗迁移作用[1]。

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

FGFR1/VEGFR2-IN-2 相关抗体:

Cell Cytotoxicity Assay[1]

Cell Line: T-47D, MCF-7, MDA-MB-231, Vero
Concentration: 10 μM
Incubation Time:
Result: Had no cytotoxicity to Vero cells and the IC50 for T-47D was 8.51 μM, the IC50 for MCF-7 was greater than 100 μM, and the IC50 for MDA-MB-231 was 69.17 μM.

Cell Proliferation Assay[1]

Cell Line: NCI-60
Concentration: 10 μM
Incubation Time:
Result: Inhibited lung cancer (NCI-H460), colon cancer (HCC-2998), central nervous system cancer (SF-295), melanoma (UACC-62), ovarian cancer (OVCAR-5), kidney cancer (UO-31), and breast cancer (MDA-MB-231), GI were 89.11%, 81.73%, 82.33%, 97.59%, 81.63%, 87.08% and 82.85%.

Cell Cycle Analysis[1]

Cell Line: T-47D
Concentration: 10, 20 μM
Incubation Time:
Result: Increased the number of T-47D cells in the G1 phase from 60.81% to 72.62%.

Cell Migration Assay [1]

Cell Line: T-47D
Concentration: 6.0 μM
Incubation Time: 0, 24, 48 h
Result: Increased the wound healing rate from 25.2% to 19.8% after 24 hours and from 42.2% to 31.2% after 48 hours.

Apoptosis Analysis[1]

Cell Line: T-47D
Concentration: 2.12, 4.25 μM
Incubation Time:
Result: Increased the early apoptosis rate of T-47D cells by 25% and 20% at 2.12 and 4.25 μM, and the late apoptosis rate by 10% and 16%. At 2.12 μM, the apoptosis rate increased by 8%, and at 4.25 μM, the apoptosis rate increased by 16%. At 2.12 and 4.25 μM, the necrotic cells increased from 5% to 12%.

RT-PCR[1]

Cell Line: T-47D
Concentration: 1/2 × IC50 (T-47D), IC50=8.5 μM
Incubation Time:
Result: Increased the expression level of BAX by 5.82 times, decreased the expression level of BCL-2 by 0.243 times, and increased the expression level of Caspase-3 by 8.2 times.
分子量

469.86

Formula

C21H15ClF3NO4S
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

FGFR1/VEGFR2-IN-2 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:

FGFR1/VEGFR2-IN-2ApoptosisNecroptosisFGFRVEGFRPDGFRFibroblast growth factor receptorVascular endothelial growth factor receptorPlatelet-derived growth factor receptorT-47DMCF-7MDA-MB-231VeroBreast cancerInhibitorinhibitorinhibit

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