2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  3. EGFR VEGFR
  4. EGFR/VEGFR2-IN-12

EGFR/VEGFR2-IN-12 (compound 11a) 是一种双重 EGFR/VEGFR2 抑制剂，对人源 EGFR 的 IC50 值分别为 64 nM，对人源 VEGFR2 的 IC50 为 74 nM。EGFR/VEGFR2-IN-12 可抑制 EGFR 和 VEGFR2 的磷酸化，诱导细胞周期阻滞于 G1/S 期，激活凋亡通路，促进 PARP-1 剪切，且具有低微摩尔级的抗增殖活性，对癌细胞的选择性远高于正常细胞。EGFR/VEGFR2-IN-12 可用于癌症相关研究。

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EGFR/VEGFR2-IN-12

EGFR/VEGFR2-IN-12 Chemical Structure

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EGFR/VEGFR2-IN-12 相关抗体

Top Publications Citing Use of Products

查看 EGFR 亚型特异性产品:

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EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

EGFR/VEGFR2-IN-12 (compound 11a) is a dual EGFR/VEGFR2 inhibitor, with an IC50 value of 64 nM against human EGFR and an IC50 value of 74 nM against human VEGFR2. EGFR/VEGFR2-IN-12 inhibits the phosphorylation of EGFR and VEGFR2, induces cell cycle arrest at the G1/S phase, activates apoptotic pathways, promotes PARP-1 cleavage, exhibits low micromolar antiproliferative activity, and shows much higher selectivity for cancer cells than normal cells. EGFR/VEGFR2-IN-12 is applicable for cancer-related research[1].

IC50 & Target

VEGFR2

 

体外研究
(In Vitro)

EGFR/VEGFR2-IN-12 (compound 11a) (10 μM; 48 h) 在 10 μM 浓度下对完整的 NCI-60 人类肿瘤细胞株组表现出强效广谱抗增殖活性，平均 GI%为 115%，且在肺癌、结肠癌、中枢神经系统肿瘤、黑色素瘤、卵巢癌、肾癌、前列腺癌和乳腺癌细胞株中均展现出优异活性[1]。
EGFR/VEGFR2-IN-12 (11a) (48 h) 在五剂量 NCI-60 筛选试验中，对黑色素瘤和肺癌细胞系表现出稳定的抗增殖活性[1]。
EGFR/VEGFR2-IN-12 (11a) (96 h) 可强效抑制 HepG-2、HCT-116 和 MCF-7 癌细胞的增殖，其 IC50 值分别为 8.26 μM、2.73 μM 和 6.72 μM；同时该化合物对正常 WI-38 和 MCF-10A 细胞的细胞毒性较低，因此具有高选择指数[1]。
EGFR/VEGFR2-IN-12 (11a)(30-40 min) 是野生型 EGFR TK (IC50 = 64 nM) 和 VEGFR-2 (IC50 = 74 nM) 的强效双重抑制剂，同时还能抑制具有临床相关性的 EGFR 突变体，包括 L858R (IC50 = 90 nM)、T790M (IC50 = 241 nM) 和 C797S (IC50 = 649 nM)[1]。
EGFR/VEGFR2-IN-12 (11a) 可抑制 EGFR 和 VEGFR-2 的磷酸化并诱导 PARP1 剪切，表明其可在 MDA-MB-231 乳腺癌细胞中抑制致癌信号通路并激活细胞凋亡[1]。
EGFR/VEGFR2-IN-12 (11a) (2.73 μM) 可在其 IC50 浓度处理下诱导 HCT-116 结肠癌细胞发生 G0/G1 期和 S 期细胞周期阻滞[1]。
EGFR/VEGFR2-IN-12 (11a) (2.73 μM) 在其 IC50 浓度处理时可显著诱导 HCT-116 结肠癌细胞发生早期和晚期凋亡，其中早期凋亡细胞占比 19.91%，晚期凋亡细胞占比 23.65%[1]。
EGFR/VEGFR2-IN-12 (11a) 可通过上调促凋亡蛋白 BAX、caspase-3、caspase-7 和 caspase-9，同时下调抗凋亡蛋白 BCL-2，促进 MDA-MB-231 乳腺癌细胞凋亡[1]。
EGFR/VEGFR2-IN-12 (11a) 可通过关键的氢键、卤键和疏水相互作用，与 EGFR TK (结合亲和力 = -15.35 kcal/mol) 和 VEGFR-2 (结合亲和力 = -14.21 kcal/mol) 的活性位点形成稳定的高亲和力相互作用，这为其双重抑制活性提供了支持[1]。
EGFR/VEGFR2-IN-12 (11a) (100 ns) 可在 100 ns 的分子动力学模拟全程与 EGFR TK 和 VEGFR-2 形成稳定复合物，维持稳定的蛋白主链 RMSD 值，该值与结合状态良好、构象保守的激酶结构一致[1]。

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

EGFR/VEGFR2-IN-12 相关抗体:

Cell Proliferation Assay[1]

Cell Line: NCI-60 human tumor cell line panel
Concentration: 10 μM
Incubation Time: 48 h
Result: Exhibited excellent broad-spectrum antiproliferative activity across all tested non-small cell lung cancer cell lines, with GI% values ranging from 94% to 164%.
Showed outstanding activity against colon cancer cell lines HCT-116, SW-620, and HT29, with GI% values of 181%, 122%, and 95% respectively.
Demonstrated anticancer activity against CNS cancer cell lines with GI% values ranging from 91% to 176%, and remarkable activity against melanoma cell lines LOX IMVI and MALME-3 M with GI% values of 162% and 141% respectively.
Showed significant broad-spectrum activity against all ovarian cancer cell lines (OVCAR-3, OVCAR-4, OVCAR-5, OVCAR-8, NCI/ADR-RES, SK-OV-3) with GI% values of 187%, 169%, 109%, 128%, 140%, and 149% respectively.
Exhibited activity against renal cancer cell lines with GI% values ranging from 115% to 181%, significant activity against prostate cancer cell line DU-145 with a GI% of 107%, and remarkable broad-spectrum activity against breast cancer cell lines MCF-7, MDA-MB-231/ATCC, T-47D, and MDA-MB-468 with GI% values of 85%, 159%, 104%, and 117% respectively.
Had a mean GI% of 115%.
体内研究
(In Vivo)

EGFR/VEGFR2-IN-12 (compound 11a) 100-2000 mg/kg；口服；单次给药) 在大鼠中表现出较低的急性口服毒性，计算得出的 LD50 约为 1300 mg/kg[1]。

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

552.04

Formula

C31H22ClN3O3S
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

EGFR/VEGFR2-IN-12 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

EGFR/VEGFR2-IN-12EGFRVEGFREpidermal growth factor receptorErbB-1HER1Vascular endothelial growth factor receptorPARP-1 cleavageHepG-2human VEGFR2human EGFRapoptotic pathwaysNCI-60 human tumor cell line panelVEGFR2G1/S phase cell cycle arrestC797SInhibitorinhibitorinhibit

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