ABS-752 hydrochloride
Based on 1 Customer Validation
ABS-752 hydrochloride is an orally active prodrug targeting CRBN-modulating molecular glue with selectivity in protein degradation. ABS-752 hydrochloride preferentially degrades GSPT1 and induces cytotoxicity through this degradation, while it also degrades NEK7, SALL4 and CK1α, with weaker degradation potency against CK1α. As a prodrug, ABS-752 hydrochloride requires metabolic activation to ABT-002 to form the active complex; VAP-1 mediates its conversion to an aldehyde intermediate. ABS-752 hydrochloride induces cell death, reduces cell viability, and exhibits antitumor activity, leading to regression and inhibition of tumor growth. ABS-752 hydrochloride shows no cytotoxicity in primary human hepatocytes. ABS-752 hydrochloride can be used in the research of hepatocellular carcinoma.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 98.81%
- CAS 番号: 2922884-90-8
- 分子式: C14H15ClFN3O3
- 分子量:327.74
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保管条件:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
Eukaryotic Release Factor (eRF) アイソフォーム固有の製品をすべて表示
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生物活性
製品説明
IC50 & Target
[1]|
eRF3a/GSPT1 1 nM (DC50, Hep3B, 24 h) |
NEK7 9 nM (DC50, Hep3B, 24 h) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Hep3B | DC50 |
7 nM
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Degradation of GSPT1 protein in Hep3B cells after 6 hours of treatment measured via Western blot-based protein degradation assay.
Degradation of GSPT1 protein in Hep3B cells after 6 hours of treatment measured via Western blot-based protein degradation assay.
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40813917 |
| Hep3B | DC50 |
1 nM
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Degradation of GSPT1 protein in Hep3B cells after 24 hours of treatment measured via Western blot-based protein degradation assay.
Degradation of GSPT1 protein in Hep3B cells after 24 hours of treatment measured via Western blot-based protein degradation assay.
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40813917 |
| Hep3B | DC50 |
104 nM
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Degradation of NEK7 protein in Hep3B cells after 6 hours of treatment measured via Western blot-based protein degradation assay.
Degradation of NEK7 protein in Hep3B cells after 6 hours of treatment measured via Western blot-based protein degradation assay.
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40813917 |
| Hep3B | DC50 |
9 nM
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Degradation of NEK7 protein in Hep3B cells after 24 hours of treatment measured via Western blot-based protein degradation assay.
Degradation of NEK7 protein in Hep3B cells after 24 hours of treatment measured via Western blot-based protein degradation assay.
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40813917 |
| Hep3B | DC50 |
35 nM
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Degradation of CK1α protein in Hep3B cells after 24 hours of treatment measured via Western blot-based protein degradation assay.
Degradation of CK1α protein in Hep3B cells after 24 hours of treatment measured via Western blot-based protein degradation assay.
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40813917 |
| Kelly | DC50 |
40 nM
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Degradation of SALL4 protein in Kelly cells after 24 hours of treatment measured via Western blot-based protein degradation assay.
Degradation of SALL4 protein in Kelly cells after 24 hours of treatment measured via Western blot-based protein degradation assay.
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40813917 |
体外実験
ABS-752 (1-50 μM; 72 h) hydrochloride reduces viability in wild-type Hep3B cells, but has no effect on Hep3B GSPT1G575N cells, demonstrating that GSPT1 degradation drives its cytotoxic activity[1].
ABS-752 (0.1 nM-30 μM; 72 h) hydrochloride has viability-reducing activity in Hep3B cells that is dependent on VAP-1[1].
ABS-752 (0.1 μM; 6 h) hydrochloride preferentially degrades GSPT1, with greater degradation of NEK7 than CK1α[1].
ABS-752 (1-10 μM) hydrochloride does not form a biochemical ternary complex with CRBN and GSPT1, NEK7, CK1α, or IKZF1, but shows recruitment activity with SALL4[1].
ABS-752 (10 μM; 0-20 h) hydrochloride is converted to the aldehyde metabolite ABT-971 by recombinant mVAP-1[1].
ABS-752 (125-2500 μM; 15 min) hydrochloride is oxidized by recombinant human VAP-1 with a Km of 674 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:wild-type Hep3B cells, CRISPR-engineered Hep3B GSPT1 G575N (degradation-resistant) cells
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Concentration:1 nM-50 μM
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Incubation Time:72 h
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Result:Potently reduced viability in wild-type Hep3B cells.
Had no effect on the viability of Hep3B GSPT1 G575N cells.
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Cell Line:Hep3B cells
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Concentration:10 μM PXS-4728A; 0.1 nM-30 μM ABS-752
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Incubation Time:1 h (PXS-4728A pre-incubation); 72 h (ABS-752 co-incubation)
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Result:Pre-treatment with PXS-4728A abolished the viability-reducing activity of ABS-752 in Hep3B cells.
The activity of control compound CC-90009 was unaffected by PXS-4728A pre-treatment.
体内実験
ABS-752 (100 mg/kg; p.o.; BID; 20-21 days) hydrochloride induces tumor growth inhibition in 80% of tested HCC PDX models, with >50% TGI in four models and complete regression in one model at the 100 mg/kg BID dose[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NSG mice (female)[1]
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Dosage:10 mg/kg; 3 mg/kg; 1 mg/kg
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Administration:p.o.; BID; 14 days
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Result:Induced strong tumor growth regression, with complete eradication in some animals at 10 mg/kg.
Induced remarkable tumor growth inhibition at 3 mg/kg and 1 mg/kg.
Confirmed strong degradation of GSPT1 in tumors excised 2 and 4 hours post-dose.
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Animal Model:BALB/c nude mice (female)[1]
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Dosage:100 mg/kg
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Administration:p.o.; BID; 20-21 days
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Result:Inhibited tumor growth in 8/10 models, with tumor growth inhibition (TGI) ranging from 16-100%.
Achieved >50% TGI in four models, including complete tumor regression in the LI6643 model by day 15-16.
Induced strong tumor growth control in the LI0050, LI0752, and LI1069 models.
- Cell Cytotoxicity Assay
- Mammalian live/dead viability and cytotoxicity staining
- Patient-Derived Xenograft (PDX)
- Apoptosis Solutions
- Patient-Derived Orthotopic Xenograft (PDOX)
- CCK-8/WST-8 Cell Proliferation Assay
- Liver Cancer Modeling
- MTT Cell Proliferation Assay
- Subcutaneous Cell-Line-Derived Xenograft
- Orthotopic Cell-Line Xenograft
- Cell Viability Determination by MTT Colorimetric Assay
化学情報
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CAS 番号 2922884-90-8
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性状 Solid
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分子量 327.74
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分子式 C14H15ClFN3O3
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Color White to off-white
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SMILES
O=C1C2=CC(F)=C(CN)C=C2CN1C3C(NC(CC3)=O)=O.Cl
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶剤 & 溶解度
体外:
DMSO : 25 mg/mL (76.28 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (286 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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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, 6 months; -20°C, 1 month (sealed storage, away from moisture). 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 | 3.0512 mL | 15.2560 mL | 30.5120 mL | 76.2800 mL |
| 5 mM | 0.6102 mL | 3.0512 mL | 6.1024 mL | 15.2560 mL | |
| 10 mM | 0.3051 mL | 1.5256 mL | 3.0512 mL | 7.6280 mL | |
| 15 mM | 0.2034 mL | 1.0171 mL | 2.0341 mL | 5.0853 mL | |
| 20 mM | 0.1526 mL | 0.7628 mL | 1.5256 mL | 3.8140 mL | |
| 25 mM | 0.1220 mL | 0.6102 mL | 1.2205 mL | 3.0512 mL | |
| 30 mM | 0.1017 mL | 0.5085 mL | 1.0171 mL | 2.5427 mL | |
| 40 mM | 0.0763 mL | 0.3814 mL | 0.7628 mL | 1.9070 mL | |
| 50 mM | 0.0610 mL | 0.3051 mL | 0.6102 mL | 1.5256 mL | |
| 60 mM | 0.0509 mL | 0.2543 mL | 0.5085 mL | 1.2713 mL |
ABS-752 hydrochloride 関連分類
HY-W998347 関連分類
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