1. Cell Cycle/DNA Damage Cytoskeleton
  2. Microtubule/Tubulin
  3. KGP591

KGP591 是一种微管蛋白聚合抑制剂 (IC50 0.57µM)。KGP591 诱导 MDA-MB-231 细胞显著的 G2/M 停滞并抑制细胞迁移,破坏微管结构和细胞形态。KGP591 在原位肾癌模型 (RENCA) 中显示抗肿瘤活性。

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KGP591 Chemical Structure

KGP591 Chemical Structure

CAS No. : 3018962-69-8

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

KGP591 is a tubulin polymerization inhibitor (IC50 0.57 µM). KGP591 induces significant G2/M stagnation, inhibits cell migration, disrupts microtubule structure and cell morphology in MDA-MB-231 cells. KGP591 shows antitumor activity in orthotopic model of kidney cancer (RENCA)[1].

体外研究
(In Vitro)

KGP591 (100 nM, 72 h) 在 MDA-MB-231 细胞中具有抑制细胞迁移和增殖的作用[1]>。
KGP591 (100 nM, 30 min) 在 MDA-MB-231 细胞中有微管破坏作用[1]
KGP591 (200 nM, 48 h) 在 MDA-MB-231 细胞中有 G2/M 细胞周期停滞作用[1]

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

Cell Migration Assay [1]

Cell Line: MDA-MB-231 cells
Concentration: 100 nM
Incubation Time: 72 h
Result: Decreased in wound width in cells and remained largely open.

Cell Cycle Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 200 nM
Incubation Time: 48 h
Result: Had an arrest of MDA-MB-231 cells at G2/M of the cell cycle.
体内研究
(In Vivo)

KGP591 的磷酸盐前药 KGP618 (150 mg/kg, 皮下注射, 24 h) 在 RENCA-luc xenograft BALB/c 小鼠模型中具有肿瘤选择性血管破坏剂 (vascular disrupting agents, VDA) 疗效[1]

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

Animal Model: RENCA-luc xenograft in BALB/c mice[1]
Dosage: 150 mg/kg
Administration: Subcutaneous Injection
Result: Caused significant reduction of Bio-Layer Interferometry (BLI) signal occurred within 2.5 h.
Showed necrosis and severe hemorrhage in RENCA tumor tissue.
分子量

403.43

Formula

C24H21NO5

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.

溶解性数据
  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验:

以下溶解方案源自文献,仅供参考,建议您先取少量样品进行尝试。

  • 方案 一

    Tubulin polymerization was evaluated in 0.25 mL reaction mixtures (final volume) containing 1 mg/mL (10 μM) purified bovine brain tubulin, 0.8 M monosodium glutamate (pH 6.6), 4% (v/v) DMSO, 0.1 mM GTP.

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献
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.

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产品名称:
KGP591
目录号:
HY-155249
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