2. Protein Tyrosine Kinase/RTK
  3. Syk FLT3
  4. Mivavotinib

Mivavotinib  (Synonyms: TAK-659; CB-659)

目录号: HY-100867
产品使用指南 技术支持

TAK-659 是一种高效选择性、可逆的，口服有效的 SYK/FLT3 双抑制剂，对 SYK 和 FLT3 作用的 IC50 值分别为 3.2 nM、4.6 nM。TAK-659 能诱导肿瘤细胞死亡而不作用于非肿瘤细胞，具有研究慢性淋巴细胞白血病 (CLL) 的潜力。

在相同的摩尔浓度下，化合物盐形式与游离形式有相同的生物活性，但盐形式 Mivavotinib monohydrochloride 通常具有更好的水溶性和稳定性。

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

我们将采用定制合成服务的方式为您快速提供所需产品和技术服务

Mivavotinib Chemical Structure

Mivavotinib Chemical Structure

CAS No. : 1312691-33-0

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.

Mivavotinib 的其他形式现货产品:

Customer Review

Other Forms of Mivavotinib:

Mivavotinib 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

TAK-659 is a highly potent, selective, reversible and orally available dual inhibitor of spleen tyrosine kinase (SYK) and fms related tyrosine kinase 3 (FLT3), with an IC50 of 3.2 nM and 4.6 nM for SYK and FLT3, respectively. TAK-659 induces cell death in tumor cells but not in nontumor cells, and with potential for the treatment of chronic lymphocytic leukemia (CLL)[1][2][3][4].

IC50 & Target

IC50: 3.2 nM (Syk), 4.6 nM (FLT3)[1]
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
Hepatocyte EC50
> 10 μM
Compound: 3b; TAK-659
Cytotoxicity against human hepatocytes assessed as decrease in cell viability after 72 to 96 hrs by MTS assay
Cytotoxicity against human hepatocytes assessed as decrease in cell viability after 72 to 96 hrs by MTS assay
[PMID: 27839918]
MOLM-13 EC50
0.11 μM
Compound: 3b; TAK-659
Cytotoxicity against FLT3-ITD dependent human MOLM13 cells assessed as decrease in cell viability after 72 to 96 hrs by MTS assay
Cytotoxicity against FLT3-ITD dependent human MOLM13 cells assessed as decrease in cell viability after 72 to 96 hrs by MTS assay
[PMID: 27839918]
MV4-11 EC50
0.018 μM
Compound: 3b; TAK-659
Cytotoxicity against FLT3-ITD dependent human MV411 cells assessed as decrease in cell viability after 72 to 96 hrs by MTS assay
Cytotoxicity against FLT3-ITD dependent human MV411 cells assessed as decrease in cell viability after 72 to 96 hrs by MTS assay
[PMID: 27839918]
Ramos EC50
9.8 nM
Compound: 3b; TAK-659
Inhibition of SYK in TgM-stimulated human Ramos cells expressing RA1/GFP-tagged BLNK assessed as reduction in RA1/GFP-tagged BLNK phosphorylation preincubated for 1 hr followed by IgM stimulation for 20 mins by TR-FRET assay
Inhibition of SYK in TgM-stimulated human Ramos cells expressing RA1/GFP-tagged BLNK assessed as reduction in RA1/GFP-tagged BLNK phosphorylation preincubated for 1 hr followed by IgM stimulation for 20 mins by TR-FRET assay
[PMID: 27839918]
RS4-11 EC50
1.4 μM
Compound: 3b; TAK-659
Cytotoxicity against human RS4:11 cells harboring wild type FLT3 assessed as decrease in cell viability after 72 to 96 hrs by MTS assay
Cytotoxicity against human RS4:11 cells harboring wild type FLT3 assessed as decrease in cell viability after 72 to 96 hrs by MTS assay
[PMID: 27839918]
Sf9 IC50
135 nM
Compound: 3b; TAK-659
Inhibition of human N-terminal 6His-tagged VEGFR2 (807 to 1171 residues) expressed in Sf9 insect cells using 5-carboxyfluorescein(FAM)-EEPLYWSFPAKKK-NH2 as substrate after 1 hr in presence of ATP by electrophoretic mobility shift assay
Inhibition of human N-terminal 6His-tagged VEGFR2 (807 to 1171 residues) expressed in Sf9 insect cells using 5-carboxyfluorescein(FAM)-EEPLYWSFPAKKK-NH2 as substrate after 1 hr in presence of ATP by electrophoretic mobility shift assay
[PMID: 27839918]
Sf9 IC50
3.2 nM
Compound: 3b; TAK-659
Inhibition of human C-terminal 6His-tagged SYK (356 to 635 residues) expressed in Sf9 insect cells using 5-carboxyfluorescein(FAM)-EEPLYWSFPAKKK-NH2 as substrate after 1 hr in presence of ATP by electrophoretic mobility shift assay
Inhibition of human C-terminal 6His-tagged SYK (356 to 635 residues) expressed in Sf9 insect cells using 5-carboxyfluorescein(FAM)-EEPLYWSFPAKKK-NH2 as substrate after 1 hr in presence of ATP by electrophoretic mobility shift assay
[PMID: 27839918]
Sf9 IC50
4.6 nM
Compound: 3b; TAK-659
Inhibition of human N-terminal 6His-tagged FLT3 (564 to 993 residues) expressed in Sf9 insect cells using 5-carboxyfluorescein(FAM)-KKKKEEIYFFFG-NH2 as substrate after 1 hr in presence of ATP by electrophoretic mobility shift assay
Inhibition of human N-terminal 6His-tagged FLT3 (564 to 993 residues) expressed in Sf9 insect cells using 5-carboxyfluorescein(FAM)-KKKKEEIYFFFG-NH2 as substrate after 1 hr in presence of ATP by electrophoretic mobility shift assay
[PMID: 27839918]
体外研究
(In Vitro)

TAK-659 inhibits cellular proliferation in SYK-dependent DLBCL and FLT3-dependent AML cell lines[1][3].
TAK-659 (5 μM; 1-24 hours) induces Casp3 activation in the LMP2A/MYC cells which was readily apparent at 4 h and reached maximum levels at 8 h of treatment[4].
TAK-659 (0.01-10 μM; 1 hour) stimulates expression of phospho-Syk at Tyr525 and Tyr352 and phospho-ERK1/2 increased in Ramos cells[2].

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

Mivavotinib 相关抗体:

Apoptosis Analysis[4]

Cell Line: LMP2A/MYC cells
Concentration: 5 µM
Incubation Time: 1 hour, 2 hours, 4 hours, 8 hours, 24 hours
Result: Induced apoptosis in LMP2A/MYC lymphoma cells.

Western Blot Analysis[2]

Cell Line: Ramos cells
Concentration: 0.01 μM,0.1 μM,1 μM,10 μM
Incubation Time: 1 hour
Result: Enhanced expression of phospho-Syk at Tyr525 and Tyr352 and phospho-ERK1/2 in stimulated Ramos cells.
体内研究
(In Vivo)

TAK-659 (100 mg/kg/day; p.o.; for 10 days) treatment totally abrogates splenomegaly and tumor development in LMP2A/MYC mice in both pretumor and tumor cell transfer experiments[4].
TAK-659 treatment kills tumor cells, but not host cells within the spleen and tumors[4].
TAK-659 treatment abrogates metastasis of tumor cells into bone marrow[4].

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

Animal Model: LMP2A/MYC double transgenic mice[4]
Dosage: 100 mg/kg/day
Administration: Oral gavage; for 10 days
Result: Inhibited LMP2A-induced tumor cell survival in vivo.
Clinical Trial
分子量

344.39

Formula

C17H21FN6O
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

Mivavotinib 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:

Mivavotinib1312691-33-0TAK-659 CB-659TAK659TAK 659CB659CB 659CB-659SykFLT3Spleen tyrosine kinaseCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3Inhibitorinhibitorinhibit

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：
Mivavotinib
目录号：
HY-100867
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