2. PI3K/Akt/mTOR
  3. mTOR PI3K
  4. LASSBio-2337

LASSBio-2337 是一种双重泛 PI3K/mTOR 抑制剂，能够功能性地调控 mTOR 及所有 PI3K 亚型，其对 mTOR 的 IC50 值为 5.8 μM。LASSBio-2337 在急性淋巴细胞白血病、慢性粒细胞白血病及乳腺癌细胞（包括多药耐药株）中表现出显著的细胞毒作用，同时对非肿瘤性人外周血单个核细胞无杀伤活性，显示出良好的选择性。LASSBio-2337 存在不溶于水、在大鼠肝微粒体中代谢稳定性较低以及仅具中等 PAMPA-GIT 通透性等理化局限，但 LASSBio-2337 是研究白血病和乳腺癌的重要工具分子。

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LASSBio-2337

LASSBio-2337 Chemical Structure

1.  客户无需承担相应的运输费用。

2.  同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户。

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Customer Review

LASSBio-2337 相关抗体

Top Publications Citing Use of Products

查看 mTOR 亚型特异性产品:

查看所有亚型
mTOR mTORC1 mTORC2

查看 PI3K 亚型特异性产品:

查看所有亚型
PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

LASSBio-2337 is a dual pan-PI3K/mTOR inhibitor with an mTOR IC50 of 5.8 μM.LASSBio-2337 functionally modulates mTOR and all PI3K isoforms.LASSBio-2337 acts as a cytotoxic agent in leukemia cells, including multidrug-resistant populations.LASSBio-2337 spares nontumor human peripheral blood mononuclear cells.LASSBio-2337 displays moderate PAMPA-GIT permeability.LASSBio-2337 shows low metabolic stability in rat liver microsomes.LASSBio-2337 is aqueous insoluble.LASSBio-2337 can be used for the research of acute lymphoblastic leukemia, chronic myelogenous leukemia, breast cancer[1].

体外研究
(In Vitro)

LASSBio-2337 (4 h; 24 h) 在 pH 7.4 的水性缓冲液中不溶，孵育 4 h 和 24 h 后的溶解度低于 1 μM[1]。
LASSBio-2337 (0.003-100 μM; 72 h) 对 CCRF-CEM 急性淋巴细胞白血病细胞、MOLT-4 急性淋巴细胞白血病细胞、MCF7 乳腺癌细胞、K562 慢性粒细胞白血病细胞、Lucena 慢性粒细胞、hPBMCs 都具有细胞毒性[1]。
LASSBio-2337 具有中等胃肠道通透性，在 PAMPA-GIT 实验中的预测吸收分数为 48.40%，渗透系数为 1.74 × 10-6 cm/s[1]。
LASSBio-2337 (10 μM; 0, 15, 30, 45, 60 min) 在大鼠肝微粒体中代谢稳定性较低，在 NADPH 再生系统存在下的半衰期为 34.3 min，提示其通过氧化代谢途径清除[1]。

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

LASSBio-2337 相关抗体:

Cell Cytotoxicity Assay[1]

Cell Line: CCRF-CEM acute lymphoblastic leukemia cells (PTEN-mutated), MOLT-4 acute lymphoblastic leukemia cells (PTEN and PIK3R1-mutated), MCF7 breast carcinoma cells (PIK3CA-mutated)
Concentration: 0.003-100 μM
Incubation Time: 72 h
Result: Demonstrated a CC50 of 4.37 (3.45-5.53) μM against CCRF-CEM cells, with a maximum cytotoxic effect (Emax) of 91.1%.
Demonstrated a CC50 of 8.05 (3.80-17.06) μM against MOLT-4 cells, with a maximum cytotoxic effect (Emax) of 99.1%.
Demonstrated a CC50 of 39.69 (24.72-63.71) μM against MCF7 cells, with a maximum cytotoxic effect (Emax) of 62.8%.

Cell Cytotoxicity Assay[1]

Cell Line: K562 chronic myelogenous leukemia cells (P53/CDKN2A-mutated), Lucena multidrug-resistant chronic myelogenous leukemia cells (P-glycoprotein-expressing MDR phenotype), Human peripheral blood mononuclear cells (hPBMCs, nontumor cells)
Concentration: 0.003-100 μM
Incubation Time: 72 h
Result: Demonstrated a CC50 of 9.44 (5.02-17.75) μM, with a maximum cytotoxic effect (Emax) of 93.6%.
Demonstrated a CC50 of 9.33 (5.48-15.90) μM against Lucena multidrug-resistant chronic myelogenous leukemia cells, with a maximum cytotoxic effect (Emax) of 93.5%.
Reduced hPBMC viability by only 33% at the highest tested concentration (50 μM), and did not decrease viability by ≥50% at any tested concentration.
分子量

356.42

Formula

C18H24N6O2
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

LASSBio-2337 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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:

LASSBio-2337LASSBio2337LASSBio 2337mTORPI3KMammalian target of RapamycinPhosphoinositide 3-kinaserat liver microsomesCCRF-CEM cellshuman peripheral blood mononuclear cellsleukemia cellschronic myelogenous leukemiaMOLT-4 cellsPI3K isoformsbreast canceracute lymphoblastic leukemiaInhibitorinhibitorinhibit

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