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  3. ZXH-4-130 TFA

ZXH-4-130 TFA is a highly potent and selective degrader of CRBN. ZXH-4-130 is a CRBN-VHL compound (hetero-PROTAC). ZXH-4-130 TFA induces ~80% CRBN degradation at 10 nM in MM1.S cells.

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ZXH-4-130 TFA

ZXH-4-130 TFA 構造式

CAS 番号 : 2711006-67-4

容量 価格(税別) 在庫状況 数量
>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 412 在庫あり
Solution
10 mM * 1 mL in DMSO USD 412 在庫あり
Solid
5 mg $190 在庫あり
10 mg $310 在庫あり
25 mg $692 在庫あり
50 mg $1108 在庫あり
100 mg $1772 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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カスタマーレビュー

Based on 2 publication(s) in Google Scholar

Other Forms of ZXH-4-130 TFA:

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PROTACs アイソフォーム固有の製品をすべて表示:

  • 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

ZXH-4-130 TFA is a highly potent and selective degrader of CRBN. ZXH-4-130 is a CRBN-VHL compound (hetero-PROTAC). ZXH-4-130 TFA induces ~80% CRBN degradation at 10 nM in MM1.S cells[1].

IC50 & Target

VHL

 

体外実験

ZXH-4-130 (100 nM; 2 h pre-treatment; followed by 96-hour treatment with 1 μM of Pomalidomide) TFA prevents Pomalidomide (1 μM) cytotoxicity to a significant extent, ZXH-4-130 TFA has statistically significant amounts of prevention[1].
ZXH-4-130 TFA (pretreatment with 50 nM) rescues GSPT1 degradation induced by CC-885 in MM1.S cells[1].
ZXH-4-130 (100 nM; 2 h pre-treatment; followed by 6 h treatment with THAL-SNS-032)TFA induces nearly complete CRBN degradation, but THAL-SNS-032's activity against CDK9 is only partially prevented[1].

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

分子量

985.08

分子式

C48H59F3N6O11S

CAS 番号
Appearance

Solid

Color

Off-white to gray

SMILES

O=C([C@H]1N(C([C@@H](NC(CCCCCCCCCCOC2=CC=CC(C(N3C(CC4)C(NC4=O)=O)=O)=C2C3=O)=O)C(C)(C)C)=O)C[C@H](O)C1)NCC5=CC=C(C6=C(C)N=CS6)C=C5.OC(C(F)(F)F)=O

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

-20°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

溶剤 & 溶解度
体外: 

DMSO : 170 mg/mL (172.57 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 1.0151 mL 5.0757 mL 10.1515 mL
5 mM 0.2030 mL 1.0151 mL 2.0303 mL
10 mM 0.1015 mL 0.5076 mL 1.0151 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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • 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)

一般には略語で表示されます:C1V1 = C2V2

濃度 (開始)

C1

×
体積 (開始)

V1

=
濃度 (終了)

C2

×
体積 (終了)

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    90% Corn Oil

    Solubility: ≥ 4.25 mg/mL (4.31 mM); Clear solution

    This protocol yields a clear solution of ≥ 4.25 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 (42.5 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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

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%

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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.0151 mL 5.0757 mL 10.1515 mL 25.3786 mL
5 mM 0.2030 mL 1.0151 mL 2.0303 mL 5.0757 mL
10 mM 0.1015 mL 0.5076 mL 1.0151 mL 2.5379 mL
15 mM 0.0677 mL 0.3384 mL 0.6768 mL 1.6919 mL
20 mM 0.0508 mL 0.2538 mL 0.5076 mL 1.2689 mL
25 mM 0.0406 mL 0.2030 mL 0.4061 mL 1.0151 mL
30 mM 0.0338 mL 0.1692 mL 0.3384 mL 0.8460 mL
40 mM 0.0254 mL 0.1269 mL 0.2538 mL 0.6345 mL
50 mM 0.0203 mL 0.1015 mL 0.2030 mL 0.5076 mL
60 mM 0.0169 mL 0.0846 mL 0.1692 mL 0.4230 mL
80 mM 0.0127 mL 0.0634 mL 0.1269 mL 0.3172 mL
100 mM 0.0102 mL 0.0508 mL 0.1015 mL 0.2538 mL
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  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます:C1V1 = C2V2

濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
× = ×
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.

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備考

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Inquiry Information

製品名:
ZXH-4-130 TFA
製品番号:
HY-132857A
数量:
MCE 日本正規代理店: