2. Metabolic Enzyme/Protease GPCR/G Protein MAPK/ERK Pathway TGF-beta/Smad Apoptosis
  3. Farnesyl Transferase Ras TGF-β Receptor Apoptosis
  4. L-744832

L-744832 是一种法尼基转移酶 (Farnesyl Transferase) 抑制剂。L-744,832 能有效抑制 H-Ras 和 N-Ras 的法尼基化，但对 K-Ras 的处理影响较小。L-744,832 不仅通过抑制 Ras 法尼基化直接靶向致癌通路，更通过表观遗传重编程恢复 TGF-β 信号，从而增强放疗敏感性。L-744832 可诱导细胞周期阻滞并诱导细胞凋亡 (apoptosis)。L-744832 可用于胰腺癌等 Ras 驱动型肿瘤的联合治疗研究。

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L-744832

L-744832 Chemical Structure

CAS No. : 160141-09-3

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L-744832 相关抗体

Top Publications Citing Use of Products

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K-Ras H-Ras N-Ras Ras

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ALK1 ALK2 ALK3 ALK4 ALK5 ALK6 ALK7 TGFβR2 ACVR2A ACVR2B

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

L-744832 is a farnesyl transferase inhibitor. L-744832 effectively inhibits the farnesylation of H-Ras and N-Ras, but has little effect on K-Ras treatment. L-744832 not only directly targets the oncogenic pathway by inhibiting Ras farnesylation, but also enhances radiosensitivity by restoring TGF-β signaling through epigenetic reprogramming. L-744832 can induce cell cycle arrest and apoptosis. L-744832 can be used in combination therapy studies for Ras-driven tumors such as pancreatic cancer[1][2].

IC50 & Target[1]

H-Ras

 

NRAS rG4

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
DU-145 IC50
78 μM
Compound: L-744832
Anticancer activity against hormone-resistant human DU145 cells assessed as cell proliferation after 72 hrs by MTT assay
Anticancer activity against hormone-resistant human DU145 cells assessed as cell proliferation after 72 hrs by MTT assay
[PMID: 21299244]
PC-3 IC50
75 μM
Compound: L-744832
Anticancer activity against hormone-resistant human PC3 cells assessed as cell proliferation after 72 hrs by MTT assay
Anticancer activity against hormone-resistant human PC3 cells assessed as cell proliferation after 72 hrs by MTT assay
[PMID: 21299244]
体外研究
(In Vitro)

L-744832 (0.1-50 μM, 24-72 h) 在 Panc-1、Capan-2、BxPC-3、AsPC-1 和 CFPAC-1 细胞中表现出显著不同的敏感性，IC50 值分别为 1.3、2.1、12.3、14.3 和 > 50 μM[1]。
L-744832 (0.1-50 μM, 72 h) 可使敏感细胞系 (Panc-1、Capan-2、BxPC-3 和 AsPC-1) 阻滞于细胞周期的 G2/M 期，且阻滞发生在 G2/M 检查点下游的有丝分裂起始阶段[1]。
L-744832 (10 μM, 24-72 h) 可诱导上述五种细胞凋亡，且放疗联合治疗可显著提高 MIA PaCa-2 细胞的凋亡率，而 BxPC-3 细胞则未观察到此效应[1][2]。
L-744832 (0.1-10 μM) 与电离辐射联用可增强人胰腺癌细胞的细胞毒性[1]。
L-744832 (5-10 μM) 可有效抑制 H-Ras 和 N-Ras 的法尼基化，且 MIA PaCa-2 细胞比 BxPC-3 细胞更敏感[2]。
L-744832 (5-10 μM，3-6 h) 可通过调节 DNMT1 恢复 TGF-β II 型受体 (RII) 的表达，从而重建 TGF-β 的抑癌功能[2]。

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

L-744832 相关抗体:

Cell Cycle Analysis[2]

Cell Line: Panc-1, Capan-2, BxPC-3, AsPC-1 and CFPAC-1 cells
Concentration: 0.1, 0.5, 1, 10, 25 and 50 μM
Incubation Time: 72 h
Result: Dose-dependent increased in G2/M phase accumulation and the proportion of G2/M phase cells in Panc-1 cells increased nearly threefold.

Apoptosis Analysis[2]

Cell Line: Panc-1, Capan-2, BxPC-3, AsPC-1 and CFPAC-1 cells
Concentration: 10 μM
Incubation Time: 72 h
Result: Showed chromatin condensation and nuclear fragmentation.
Increased the apoptotic index in each group, and this occurred in both wild-type p53 (Capan-2) cells and mutant p53 (Panc-1) cells.

Western Blot Analysis[2]

Cell Line: Panc-1, Capan-2, BxPC-3, AsPC-1 and CFPAC-1 cells
Concentration: 10 μM
Incubation Time: 72 h
Result: Significantly increased the activity of Cyclin B1/Cdc2 kinase.

RT-PCR[1]

Cell Line: MIA PaCa-2 cells
Concentration: 10 μM
Incubation Time: 3 and 6 h
Result: Activated the RII promoter to increase its mRNA levels.
Reduced the mRNA levels of DNMT1.

Western Blot Analysis[1]

Cell Line: MIA PaCa-2 cells
Concentration: 10 μM
Incubation Time: 3 and 6 h
Result: Activated the RII promoter to increase its protein levels.
Reduced the protein levels of DNMT1.
分子量

559.78

Formula

C26H45N3O6S2
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

L-744832 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:

L-744832160141-09-3L744832L 744832Farnesyl TransferaseRasTGF-β ReceptorApoptosisFtaseTransforming growth factor beta receptorspancreatic cancerTGF-b signalingradio-sensitizationfarnesyltransferase inhibitor (FTI)DNA methyltransferaseTGF-b type II receptor (TGF-bRII)Inhibitorinhibitorinhibit

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