2. Cell Cycle/DNA Damage Cytoskeleton Metabolic Enzyme/Protease
  3. Microtubule/Tubulin Prolyl Endopeptidase (PREP)
  4. Tasidotin

Tasidotin (ILX651 free base) 是一种微管蛋白抑制剂和竞争性脯氨酰寡肽酶 (Prolyl Endopeptidase (PREP)) 抑制剂，对牛微管蛋白的 IC50 为 10 μM。Tasidotin 在非人灵长类动物中表现出较高的脑脊液穿透性。Tasidotin 可拮抗微管组装并诱导延长的组装延迟期，进而抑制有丝分裂和细胞增殖，对癌细胞发挥细胞毒性和溶瘤作用。Tasidotin 在细胞内可代谢为多肽和脯氨酸，并在体内被脯氨酰寡肽酶介导和代谢。Tasidotin 可应用于伯基特淋巴瘤、乳腺癌、白血病、黑色素瘤、中枢神经系统恶性肿瘤及各类实体瘤的相关研究。

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Tasidotin

Tasidotin Chemical Structure

CAS No. : 192658-64-3

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。

规格 是否有货
50 mg   询价  
100 mg   询价  
250 mg   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of Tasidotin:

Tasidotin 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Tasidotin (ILX651 free base) is a tubulin inhibitor and competitive Prolyl Endopeptidase (PREP) inhibitor, with an IC50 of 10 μM against bovine tubulin. Tasidotin exhibits high cerebrospinal fluid penetration in non-human primates. Tasidotin antagonizes microtubule assembly and induces an extended assembly lag phase, thereby inhibiting mitosis and cell proliferation, and exerts cytotoxic and oncolytic effects on cancer cells. Tasidotin is metabolized into polypeptides and proline inside cells, and its in vivo metabolism is mediated by prolyl endopeptidase. Tasidotin can be applied in research related to Burkitt's lymphoma, breast cancer, leukemia, melanoma, central nervous system malignancies and various solid tumors[1][2][3].

体外研究
(In Vitro)

Tasidotin 可抑制 Burkitt 淋巴瘤 CA46 细胞的生长，其 IC50 为 100 nM[1]。
Tasidotin 可抑制 MCF-7 人乳腺癌细胞的生长，其 IC50 为 150 nM[1]。
Tasidotin (2-300 nM; 70 nM) 可在体外强效抑制多种肿瘤细胞系的增殖，其 IC50 值范围为 2 至 300 nM；在约 70 nM 的浓度下，它可通过影响微管动力学来抑制有丝分裂与细胞增殖[2]。

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

Tasidotin 相关抗体:

Cell Proliferation Assay[1]

Cell Line: Burkitt lymphoma CA46 suspension cells
Concentration: Multiple unspecified concentrations
Incubation Time: 48 h
Result: Inhibited the growth of CA46 cells with an IC50 of 100 nM.
Was substantially less cytotoxic than dolastatin 15 and dolastatin 10, but more cytotoxic than its metabolite P5.

Cell Proliferation Assay[1]

Cell Line: MCF-7 human breast carcinoma monolayer cells
Concentration: Multiple unspecified concentrations
Incubation Time: 48 h
Result: Inhibited the growth of MCF-7 cells with an IC50 of 150 nM.
Was substantially less cytotoxic than dolastatin 15, cemadotin, and dolastatin 10, but more cytotoxic than its metabolite P5.
药代动力学
(Parmacokinetics)
Species Dose Route AUC0-∞ (Plasma) T1/2 (Plasma) CLplasma
Rhesus monkey[2] 0.75 mg/kg i.v. 30 μM·min 27 min 44 mL/min/kg
体内研究
(In Vivo)

Tasidotin (0.75 mg/kg；静脉注射；单次给药；输注 30 分钟) 在健康成年雄性恒河猴体内可实现高脑脊液穿透性，其脑脊液与血浆的 AUC0-t 平均比值为 1.1，且给药后数小时内脑脊液中的药物浓度可达到与抗增殖活性相关的水平[2]。

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

Animal Model: Macaca mulatta (adult male, 11.4-15.9 kg)[2]
Dosage: 0.75 mg/kg
Administration: i.v.; single dose; 30 minutes infusion
Result: Achieved a mean CSF:plasma AUC ratio of 1.1.
Had a mean plasma AUC of 30 μM min, mean plasma half-life of 27 min, and mean plasma clearance of 44 mL/min/kg.
Had a mean CSF AUC of 28 μM min, with a mean CSF half-life of 96 min.
Reached peak CSF concentrations ranging from 53 to 272 nM, exceeding 70 nM for 2.5-3.5 hours in three of four animals.
Was well tolerated with no significant clinical or laboratory toxicity.
分子量

606.85

Formula

C32H58N6O5
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

Tasidotin 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:

Tasidotin192658-64-3ILX651ILX 651ILX-651Microtubule/TubulinProlyl Endopeptidase (PREP)prolyl oligopeptidasePOPBurkitt lymphoma CA46 cellsmicrotubule assemblybovine tubulinnonhuman primatesMCF-7 human breast carcinoma cellsCCRF-CEM human leukemia cellsMDA-MB-435 human breast carcinoma cellsHS 578-T human breast carcinoma cellsFlavobacterium meningosepticumInhibitorinhibitorinhibit

您最近查看的产品:

Your information is safe with us. * Required Fields.

   产品名称：

  

* 需求量：

* 客户姓名：

 

* Email：

* 电话：

 

* 公司或机构名称：

   留言给我们：

Bulk Inquiry

Inquiry Information

产品名称：
Tasidotin
目录号：
HY-106021
需求量：

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

   产品名称：

  

* Lot #：

* 客户姓名：

 

* Email：

   电话：

 

* 部门：

* 公司或机构名称：

 

   留言给我们：

Request for HNMR Report

We have received your request and will respond to you as soon as possible.

嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z