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PCLX-001

产品编号 T63788 CAS 1215011-08-7

PCLX-001 is a small-molecule compound that acts as an orally active inhibitor of N-myristoyltransferase (NMT), specifically targeting NMT1 and NMT2 with IC50 values of 5 nM and 8 nM, respectively. This compound demonstrates anti-tumor effects and effectively inhibits the early signaling of B-cell receptor (BCR). Consequently, PCLX-001 is a valuable tool for researching B-cell malignancies [1] [2].

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PCLX-001, CAS 1215011-08-7

规格	价格/CNY	货期
1 mg	￥ 1,650	现货
5 mg	￥ 3,970	现货
10 mg	￥ 6,430	现货
25 mg	￥ 11,300	现货
50 mg	￥ 15,300	现货
100 mg	￥ 19,800	现货
500 mg	￥ 39,600	现货
1 mL * 10 mM (in DMSO)	￥ 5,130	现货

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生物活性

化学信息

存储 & 溶解度

参考文献

产品描述	PCLX-001 is a small-molecule compound that acts as an orally active inhibitor of N-myristoyltransferase (NMT), specifically targeting NMT1 and NMT2 with IC50 values of 5 nM and 8 nM, respectively. This compound demonstrates anti-tumor effects and effectively inhibits the early signaling of B-cell receptor (BCR). Consequently, PCLX-001 is a valuable tool for researching B-cell malignancies [1] [2].
靶点活性	NMT2:8 nM, NMT1:5 nM
体外活性	We discovered a marked sensitivity of hematological cancer cell lines, including B-cell lymphomas, to the potent pan-NMT inhibitor PCLX-001. PCLX-001 treatment impacts the global myristoylation of lymphoma cell proteins and inhibits early B-cell receptor (BCR) signaling events critical for survival. In addition to abrogating myristoylation of Src family kinases, PCLX-001 also promotes their degradation and, unexpectedly, that of numerous non-myristoylated BCR effectors including c-Myc, NFκB and P-ERK, leading to cancer cell death in vitro and in xenograft models.[2]
体内活性	Treatment of cultured breast cancer cells with PCLX-001 reduced cell viability in vitro. Daily oral administration of PCLX-001 to immunodeficient mice bearing human MDA-MB-231 breast cancer xenografts produced significant dose-dependent tumor growth inhibition in vivo.[4]

分子量	537.51
分子式	C24H30Cl2N6O2S
CAS No.	1215011-08-7

存储

store at low temperature,keep away from direct sunlight　|　Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 5.38 mg/mL (10 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.8604 mL	9.3022 mL	18.6043 mL	46.5108 mL
	5 mM	0.3721 mL	1.8604 mL	3.7209 mL	9.3022 mL
	10 mM	0.186 mL	0.9302 mL	1.8604 mL	4.6511 mL

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参考文献

1. Weickert M, et al. Initial characterization and toxicology of an nmt inhibitor in development for hematologic malignancies. Blood. 2019;134: 3362. 2. Beauchamp E, et al. Targeting N-myristoylation for therapy of B-cell lymphomas. Nat Commun. 2020;11(1):5348. 3. Sangha R, et al. Novel, First-in-Human, Oral PCLX-001 Treatment in a Patient with Relapsed Diffuse Large B-Cell Lymphoma. Curr Oncol. 2022;29(3):1939-1946. 4. Mackey JR, et al. N-myristoyltransferase proteins in breast cancer: prognostic relevance and validation as a new drug target. Breast Cancer Res Treat. 2021;186(1):79-87.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

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第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

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