2. Metabolic Enzyme/Protease
  3. Isocitrate Dehydrogenase (IDH)
  4. Safusidenib

Safusidenib  (Synonyms: AB-291; DS-1001)

目录号: HY-145594
产品使用指南

摩尔计算器

Safusidenib (AB-291; DS-1001) 是一种口服有效的选择性 IDH1突变型抑制剂。Safusidenib 强烈抑制突变型 IDH1 但不抑制野生型 IDH1。Safusidenib 会削弱软骨肉瘤中的肿瘤活性。Safusidenib 对 IDH1R132H 和 IDH1R132C 具有活性，在没有预孵育的情况下，IC50 分别为 15 和 130 nM。

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 DS-1001b 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

Safusidenib Chemical Structure

Safusidenib Chemical Structure

CAS No. : 1898206-17-1

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.

Safusidenib 的其他形式现货产品:

Customer Review

Other Forms of Safusidenib:

Safusidenib 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 1 篇科研文献

查看 Isocitrate Dehydrogenase (IDH) 亚型特异性产品:

查看所有亚型
IDH1 IDH2

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Safusidenib (AB-291; DS-1001) is an orally bioavailable, selective mutant IDH1 inhibitor. Safusidenib strongly inhibits mutant IDH1 but not wild-type IDH1. Safusidenib impairs tumor activity in chondrosarcoma[1]. Safusidenib exhibits activity against IDH1R132H, and IDH1R132C with IC50s of 15, and 130 nM in assays without any preincubation, respectively[2].

IC50 & Target

IDH1

 

体外研究
(In Vitro)

Safusidenib (DS-1001b) impairs the proliferation of IDH1-mutated chondrosarcoma cell lines and decreases 2-HG levels[1].
Safusidenib impairs the proliferation of IDH1 mutant chondrosarcoma cell lines in a dose-dependent manner, whereas Safusidenib has little effect on the proliferation of the IDH wild-type cell lines OUMS27 and NDCS-1; GI50 values for JJ012, L835, OUMS27, and NDCS-1 cells are 81?nM (day 14), 77?nM (6 weeks), >10?μM (day 10), and >10?μM (day 10), respectively[1].
Safusidenib (1, and 10?μM; for 6 weeks) markedly upregulates SOX9, a key regulator of chondrocyte differentiation, at the protein level[1].
Safusidenib (1 μM) significantly upregulates CDKN1C at the protein level[1].
Safusidenib (DS-1001b) exhibits activity against IDH1 or IDH2 enzymes with IC50s of 8.4, 11, and 180 nM for IDH1R132H, IDH1R132C, and IDH1WT in assays conducted with a 2-hour preincubation step[2].

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

Safusidenib 相关抗体:

Cell Proliferation Assay[1]

Cell Line: The IDH1 mutant cell lines JJ012 and L835 cells
Concentration: 0.1, 1, and 10 μM
Incubation Time: 0, 3, 6, 9, 12, and 15 days
Result: Impaired proliferation in both cell lines in a dose-dependent manner.

Western Blot Analysis[1]

Cell Line: L835 cells
Concentration: 0, 1, and 10 μM
Incubation Time: 6 weeks
Result: Markedly upregulated SOX9 at the protein level.
体内研究
(In Vivo)

Safusidenib (DS-1001b) has antineoplastic activity in JJ012 xenografts. Continuous administration of Safusidenib (mixed with sterilized pellet food and fed continuously for 6 weeks) impairs tumor growth in xenograft mice[1].

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

Animal Model: NOD-SCID bearing JJ012 xenograft[3]
Dosage: Mixed with sterilized pellet food (CRF-1; Oriental Yeast) and fed ad libitum for 6 weeks. Mixed with sterilized pellet food (CRF-1; Oriental Yeast) and fed ad libitum for 6 weeks.
Administration: Fed continuously starting at 3 weeks
Result: Continuous administration significantly impaired tumor growth in JJ012 xenograft mice.
Clinical Trial
分子量

535.78

Formula

C25H18Cl3FN2O4
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

Safusidenib 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:

Safusidenib1898206-17-1AB-291 DS-1001AB291AB 291DS1001DS 1001DS-1001Isocitrate Dehydrogenase (IDH)orally bioavailablemutant IDH1 inhibitorchondrosarcomaIDH1R132HIDH1R132CInhibitorinhibitorinhibit

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：
Safusidenib
目录号：
HY-145594
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