2. Cell Cycle/DNA Damage Membrane Transporter/Ion Channel Apoptosis
  3. PERK P-glycoprotein Apoptosis
  4. BRAFV600E/ABL2-IN-2

BRAFV600E/ABL2-IN-2 是一种双重 BRAFV600E 和 ABL2 激酶抑制剂，对人源 BRAFV600E 的 IC50 为 0.088 μM，对人源 ABL2 的 IC50 为 0.3 μM。BRAFV600E/ABL2-IN-2 可降低黑色素瘤细胞中下游 ERK1/2 和 CrkL 的磷酸化水平。BRAFV600E/ABL2-IN-2 可降低黑色素瘤细胞中 P-糖蛋白 (P-glycoprotein) 的表达。BRAFV600E/ABL2-IN-2 可诱导黑色素瘤细胞发生 G1 期细胞周期阻滞以及凋亡 (Apoptosis)。BRAFV600E/ABL2-IN-2 可用于黑色素瘤的相关研究。

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BRAFV600E/ABL2-IN-2

BRAFV600E/ABL2-IN-2 Chemical Structure

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BRAFV600E/ABL2-IN-2 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

BRAFV600E/ABL2-IN-2 is a dual BRAFV600E and ABL2 kinase inhibitor, with an IC50 of 0.088 μM against human BRAFV600E and an IC50 of 0.3 μM against human ABL2. BRAFV600E/ABL2-IN-2 reduces the phosphorylation levels of downstream ERK1/2 and CrkL in melanoma cells. BRAFV600E/ABL2-IN-2 decreases the expression of P-glycoprotein (P-glycoprotein) in melanoma cells. BRAFV600E/ABL2-IN-2 induces G1 cell cycle arrest and apoptosis (Apoptosis) in melanoma cells. BRAFV600E/ABL2-IN-2 is applicable to relevant research on melanoma[1].

体外研究
(In Vitro)

BRAFV600E/ABL2-IN-2 (Compound 8h) (0.01-100 μM; 48 h) 可抑制 NCI-60 细胞组中癌细胞系的增殖，对 SK-MEL-5 黑色素瘤细胞的抑制活性最强 (GI50 = 0.54 μM)[1]。
BRAFV600E/ABL2-IN-2 (10 μM) 可强效抑制 BRAFWT、PI3K 和 VEGFR2 激酶，对 FGFR1、CDK4 和 CDK6 激酶具有中等抑制活性[1]。
BRAFV600E/ABL2-IN-2 (72 h) 在 SK-MEL-5 黑色素瘤细胞中可将 P-糖蛋白的表达下调 67.38%[1]。
BRAFV600E/ABL2-IN-2 可抑制亲本和维莫非尼耐药性 A375 黑色素瘤细胞的增殖，对 A375 细胞的 IC50 为 12.3 μM，对 A375-R 细胞的 IC50 为 20.1 μM，对人正常 WI-38 肺成纤维细胞表现出低细胞毒性，其 IC50 为 28.78 μM[1]。
BRAFV600E/ABL2-IN-2 可在对 Vemurafenib (HY-12057) 耐药的 A375-R 黑色素瘤细胞中抑制 ABL2 介导的 p-CrkL 以及 BRAFV600E 介导的 p-ERK1/2 信号通路，且不会改变总蛋白水平[1]。
BRAFV600E/ABL2-IN-2 (0.54 μM) 可诱导 SK-MEL-5 黑色素瘤细胞发生 G1 期细胞周期阻滞，减少其向 S 期和 G2/M 期的进程[1]。
BRAFV600E/ABL2-IN-2 (0.54 μM; 24 h) 可在 SK-MEL-5 黑色素瘤细胞中诱导显著的早期和晚期细胞凋亡，总凋亡率达 45.28%[1]。

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

BRAFV600E/ABL2-IN-2 相关抗体:

Cell Proliferation Assay[1]

Cell Line: NCI-60 cancer cell line panel, SK-MEL-5 melanoma cells, HT29 colon cancer cells
Concentration: 100, 10, 1, 0.1, and 0.01 μM
Incubation Time: 48 h
Result: Exhibited a GI50 range of 0.54-28.18 μM across the NCI-60 panel.
Showed the highest potency against SK-MEL-5 melanoma cells with a GI50 of 0.54 μM.
Showed cytostatic activity against SK-MEL-5 (TGI = 19.95 μM) and HT29 colon cancer cells (TGI = 26.30 μM).

Apoptosis Analysis[1]

Cell Line: SK-MEL-5 melanoma cells
Concentration: 0.54 μM
Incubation Time: 24 h
Result: Induced total apoptosis in 45.28% of cells, with 25.61% early apoptotic (Annexin V-positive, PI-negative) and 13.89% late apoptotic (Annexin V-positive, PI-positive) cells, compared to 2.12% total apoptosis in untreated control cells.
分子量

559.86

Formula

C24H20BrClN4O3S
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

BRAFV600E/ABL2-IN-2 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

BRAFV600E/ABL2-IN-2PERKP-glycoproteinApoptosisProtein kinase R-like endoplasmic reticulum kinasePKR-like endoplasmic reticulum kinaseP-gpPgpMultidrug resistance protein 1MDR1ATP-binding cassette sub-family B member 1ABCB1Cluster of differentiation 243CD243BRAFV600E and ABL2 kinase inhibitormelanomaSK-MEL-5 melanoma cellsA375 cellsA375-R cellsWI-38 lung fibroblastsInhibitorinhibitorinhibit

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