2. Metabolic Enzyme/Protease
  3. Isocitrate Dehydrogenase (IDH)
  4. DS-1001b

DS-1001b is an orally active, blood-brain permeable, potent IDH-1 (isocitrate dehydrogenase-1) mutant inhibitor. DS-1001b has antitumor activity.

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DS-1001b 構造式

DS-1001b 構造式

CAS 番号 : 1898207-64-1

容量 価格（税別） 在庫状況 数量
無料サンプル (0.1 - 0.5 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 121 在庫あり
Solution
10 mM * 1 mL in DMSO USD 121 在庫あり
Solid
5 mg USD 90 在庫あり
10 mg USD 150 在庫あり
25 mg USD 250 在庫あり
50 mg USD 450 在庫あり
100 mg USD 750 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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Based on 1 publication(s) in Google Scholar

Other Forms of DS-1001b:

DS-1001b 関連抗体

Top Publications Citing Use of Products

Isocitrate Dehydrogenase (IDH) アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
IDH1 IDH2

  • 生物活性

  • 純度とドキュメンテーション

  • 参考文献

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製品説明

DS-1001b is an orally active, blood-brain permeable, potent IDH-1 (isocitrate dehydrogenase-1) mutant inhibitor. DS-1001b has antitumor activity[1][2][3].

IC50 & Target

IDH-1[1]
体外実験

DS-1001b (0.1-10 μM, 14 days) inhibits the proliferation of IDH1-mutated chondrosarcoma cells[2].

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

DS-1001b 関連抗体

Cell Proliferation Assay[2]

Cell Line: JJ012, L835
Concentration: 0.1, 1, 10 μM
Incubation Time: 14 days
Result: Inhibited cell proliferation in a dose-dependent manner. GI50 values for JJ012, L835 are 81 and 77 nM.

RT-PCR[2]

Cell Line: L835
Concentration: 10 μM
Incubation Time: 6 weeks
Result: Upregulated the expression of SOX9, RUNX2, COL2A1, COL10A1 and ACAN.

Cell Cycle Analysis[2]

Cell Line: JJ012
Concentration: 1 μM
Incubation Time: 7 days
Result: Induced G1 phase arrest. Increased the percentage of cells in the G0/G1 phase by 5.4% and decreased that of cells in the S phase by 4.4%.
体内実験

DS-1001b (continuous feeding of DS-1001b mixed sterile pellet food from 3 weeks after transplantation) can damage the growth of subcutaneous tumor in JJ012 xenografted mice[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
臨床実験
分子量

608.92

分子式

C29H29Cl3FN3O4
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

CC(C)(N)C.O=C(N1C2=CC=CC(/C=C/C(O)=O)=C2C(C)=C1)C3=C(C(C)(F)C)ON=C3C4=C(C=C(Cl)C=C4Cl)Cl
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 29 mg/mL (47.63 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6423 mL 8.2113 mL 16.4225 mL
5 mM 0.3285 mL 1.6423 mL 3.2845 mL
10 mM 0.1642 mL 0.8211 mL 1.6423 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.42 mg/mL (3.97 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.42 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (24.2 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.42 mg/mL (3.97 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.42 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (24.2 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション

純度: 99.71%

COA (259 KB) HNMR (153 KB) RP-HPLC (160 KB) LCMS (224 KB)

取扱説明書 (2659 KB)
参考文献

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.6423 mL 8.2113 mL 16.4225 mL 41.0563 mL
5 mM 0.3285 mL 1.6423 mL 3.2845 mL 8.2113 mL
10 mM 0.1642 mL 0.8211 mL 1.6423 mL 4.1056 mL
15 mM 0.1095 mL 0.5474 mL 1.0948 mL 2.7371 mL
20 mM 0.0821 mL 0.4106 mL 0.8211 mL 2.0528 mL
25 mM 0.0657 mL 0.3285 mL 0.6569 mL 1.6423 mL
30 mM 0.0547 mL 0.2737 mL 0.5474 mL 1.3685 mL
40 mM 0.0411 mL 0.2053 mL 0.4106 mL 1.0264 mL
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DS-1001b Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

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

DS-1001b1898207-64-1Isocitrate Dehydrogenase (IDH)IDHMutantInhibitorJJ012L835Antitumorinhibitorinhibit

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製品名:
DS-1001b
製品番号:
HY-129545
数量:
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