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

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].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
MCF7 GI50
320 nM
Compound: KGP591
Cytotoxicity against human MCF7 cells assessed as cell growth inhibition incubated for 96 hrs by SRB assay
Cytotoxicity against human MCF7 cells assessed as cell growth inhibition incubated for 96 hrs by SRB assay
[PMID: 37984295]
MDA-MB-231 GI50
102 nM
Compound: KGP591
Cytotoxicity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 96 hrs by SRB assay
Cytotoxicity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 96 hrs by SRB assay
[PMID: 37984295]
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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