2. Metabolic Enzyme/Protease Protein Tyrosine Kinase/RTK
  3. HIF/HIF Prolyl-Hydroxylase VEGFR
  4. Casdatifan

Casdatifan (AB521) is an orally active and selective allosteric small-molecule inhibitor of hypoxia-inducible factor 2α (HIF-2α). Casdatifan inhibits pro-tumor gene transcription by blocking the heterodimerization of HIF-2α with ARNT, and significantly suppresses tumor growth in clear cell renal cell carcinoma (ccRCC) models either as a monotherapy or in combination with agents such as Zimberelimab (HY-P99109). Casdatifan is applicable for the research of ccRCC.

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Casdatifan

Casdatifan 構造式

CAS 番号 : 2709069-30-5

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 8800 在庫あり
Solution
10 mM * 1 mL in DMSO USD 8800 在庫あり
Solid
100 μg $700 在庫あり
500 μg $1750 在庫あり
1 mg $2800 在庫あり
2 mg $4500 在庫あり
5 mg $8000 在庫あり
10 mg $12800 在庫あり
50 mg   お問い合わせ  
100 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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Casdatifan 関連抗体

Top Publications Citing Use of Products

HIF/HIF Prolyl-Hydroxylase 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
HIF-1α HIF

VEGFR 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
VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

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製品説明

Casdatifan (AB521) is an orally active and selective allosteric small-molecule inhibitor of hypoxia-inducible factor 2α (HIF-2α). Casdatifan inhibits pro-tumor gene transcription by blocking the heterodimerization of HIF-2α with ARNT, and significantly suppresses tumor growth in clear cell renal cell carcinoma (ccRCC) models either as a monotherapy or in combination with agents such as Zimberelimab (HY-P99109). Casdatifan is applicable for the research of ccRCC[1].

体外実験

Casdatifan (2-10 μM; 24 h) reduces HIF-2α protein levels in 786-O and A-498 clear cell renal cell carcinoma (ccRCC) cells under normoxic conditions[1].
Casdatifan potently inhibits VEGF secretion in 786-O ccRCC cells, with an IC50 of 28.9 nM[1].
Casdatifan (0.001-10 μM; 21 days) inhibits the anchorage-independent growth of 786-O ccRCC cells in a concentration-dependent manner[1].
Casdatifan (1 μM; 20 h) inhibits HIF-2α-dependent gene transcription in hypoxically induced primary human M2-polarized macrophages[1].
Casdatifan (3 days) reduces HIF-2α protein levels in activated hypoxic primary human CD8+ T cells without impairing T cell proliferation or cytokine secretion[1].

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

Casdatifan 関連抗体

Western Blot Analysis[1]

Cell Line: 786-O and A-498 cells
Concentration: 2, 10 μM
Incubation Time: 24 h
Result: Caused a marked reduction in HIF-2α protein levels in both 786-O and A-498 cells.
体内実験

Casdatifan (3-100 mg/kg; p.o.; once daily; until study endpoint) dose-dependently inhibits HIF-2α-mediated transcription and significantly suppresses tumor growth in nude mice bearing 786-O and A-498 xenograft models[1].
Casdatifan (30 mg/kg; p.o.; once daily; until study endpoint) significantly enhances the antitumor efficacy in the NSG-MHC I/II DKO humanized PBMC A-498 ccRCC xenograft model when administered in combination with Zimberelimab (HY-P99109)[1].

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

Animal Model: NU-Foxn1nu nude mice (female, 6-8 weeks old, subcutaneous xenograft of 786-O or A-498 cells)[1]
Dosage: 3 mg/kg; 10 mg/kg; 30 mg/kg; 100 mg/kg
Administration: p.o.; daily; until the end of the study
Result: Significantly reduced tumour burden in both 786-O and A-498 models.
Decreased HIF-2α protein levels and tumour cell proliferation (Ki-67 staining), and downregulated HIF-2α target genes (VEGFA, CCND1, CXCR4) in tumour tissues in a dose-dependent manner.
Animal Model: NSG-MHC I/II DKO (female, 4-5 weeks old, humanized PBMC A-498 xenograft model)[1]
Dosage: 30 mg/kg
Administration: p.o.; daily; until the end of the study
Result: Led to more rapid and sustained tumour regression than either monotherapy, with 60% of mice achieving a complete response after treatment cessation.
Induced considerable tumour regression but growth resumed after treatment stop until the end of the study, while Zimberelimab alone showed modest efficacy.
分子量

439.42

分子式

C21H17F4NO3S
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

CS(C(C1=C2C[C@@H](F)[C@H]1O)=CC=C2[C@](C[C@H](F)[C@@H]3F)([H])C4=C3C=C(F)C=C4C#N)(=O)=O
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 : 100 mg/mL (227.57 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 2.2757 mL 11.3786 mL 22.7573 mL
5 mM 0.4551 mL 2.2757 mL 4.5515 mL
10 mM 0.2276 mL 1.1379 mL 2.2757 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. 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)

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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）

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体積 （開始）

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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: ≥ 2.5 mg/mL (5.69 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (5.69 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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+
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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
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. 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 2.2757 mL 11.3786 mL 22.7573 mL 56.8932 mL
5 mM 0.4551 mL 2.2757 mL 4.5515 mL 11.3786 mL
10 mM 0.2276 mL 1.1379 mL 2.2757 mL 5.6893 mL
15 mM 0.1517 mL 0.7586 mL 1.5172 mL 3.7929 mL
20 mM 0.1138 mL 0.5689 mL 1.1379 mL 2.8447 mL
25 mM 0.0910 mL 0.4551 mL 0.9103 mL 2.2757 mL
30 mM 0.0759 mL 0.3793 mL 0.7586 mL 1.8964 mL
40 mM 0.0569 mL 0.2845 mL 0.5689 mL 1.4223 mL
50 mM 0.0455 mL 0.2276 mL 0.4551 mL 1.1379 mL
60 mM 0.0379 mL 0.1896 mL 0.3793 mL 0.9482 mL
80 mM 0.0284 mL 0.1422 mL 0.2845 mL 0.7112 mL
100 mM 0.0228 mL 0.1138 mL 0.2276 mL 0.5689 mL
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Casdatifan Related Classifications

  • 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 *
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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.

Keywords:

Casdatifan2709069-30-5AB521AB 521AB-521HIF/HIF Prolyl-HydroxylaseVEGFRHypoxia-inducible factorsHIFsHIF-PHVascular endothelial growth factor receptorendothelial cellsARNTA-498 cells786-O cellscancer cellsInhibitorinhibitorinhibit

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製品名:
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製品番号:
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