BR-cpd7
Based on 1 Customer Validation
BR-cpd7 is an orally active, selective PROTAC degrader targeting FGFR1 and FGFR2, with a DC50 of 2.2 nM against FGFR1. BR-cpd7 reduces FGFR signaling. BR-cpd7 induces cell cycle arrest and selectively blocks the proliferation of FGFR1/FGFR2-dependent tumor cells. BR-cpd7 exhibits significant antitumor efficacy in FGFR1-dependent lung cancer animal models, while achieving complete depletion of FGFR1. BR-cpd7 can be used for cancer-related research.
(Pink: FGFR1 and FGFR2 ligand (HY-160013); Blue: Cereblon ligand (HY-131717); Black: linker).
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 : 98.01%
- 分子式: C44H47Cl2N11O8
- 分子量:928.82
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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
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生物活性
製品説明
IC50 & Target
[1]|
FGFR1 2.2 nM (DC50) |
FGFR2 |
体外実験
BR-cpd7 exhibits remarkable FGFR1/2 subtype specificity and shows almost no antiproliferative activity against cancer cells without FGFR abnormalities[1].
BR-cpd7 (10-1000 nM; 24 h) decreases FGFR1 protein abundance in DMS114 cells and reaches the maximum inhibitory effect at 10 nM and 100 nM; BR-cpd7 (24 h exposure) downregulates FGFR2 protein levels in KATO III cells with the optimal activity at 100 nM; BR-cpd7 fails to suppress FGFR3 protein expression in RT112/84 cells[2].
BR-cpd7 inhibits the proliferation of KATO III cells after 5 days of treatment, with an IC50 value of 8.6 nM[2].
BR-cpd7 (10-1000 nM; 40 h) reduces the FGFR2 protein level in KATO III cells, but does not induce PARP cleavage after 40 h of treatment, with the most significant reduction in FGFR2 level observed at 100 nM[2].
BR-cpd7 (administered for 4-5 days) potently inhibits the proliferation of human cancer cell lines harboring genomic FGFR aberrations (IC50 values ranging from 4.6 nM to 124 nM), while exerting no antiproliferative effect on cell lines without FGFR aberrations (IC50 > 10000 nM)[2].
BR-cpd7 potently and selectively degrades FGFR1/2 in FGFR1/2-dependent tumor cells (DC50 of approximately 10 nmol/L), inhibits the FGFR signaling pathway, induces cell cycle arrest, blocks tumor cell proliferation, and exhibits no antiproliferative activity against cancer cells without FGFR abnormalities[2].
BR-cpd7 exhibits strong binding affinity to purified FGFR1 and FGFR2, and potently inhibits their activities[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:DMS114 (FGFR1-amplified small cell lung cancer) cells
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Concentration:10, 100, 1000 nM
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Incubation Time:24 h
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Result:Reduced FGFR1 protein levels in a concentration-dependent manner.
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Cell Line:KATO III (FGFR2-amplified gastric carcinoma) cells
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Concentration:10, 100, 1000 nM
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Incubation Time:24 h
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Result:Reduced FGFR2 protein levels in a concentration-dependent manner.
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Cell Line:RT112/84 cells
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Concentration:10, 100, 1000 nM
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Incubation Time:24 h
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Result:Did not reduce FGFR3 protein levels, with levels remaining near or above untreated control levels.
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Cell Line:KATO III (FGFR2-amplified gastric carcinoma) cells
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Concentration:10, 100, 1000 nM
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Incubation Time:40 h
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Result:Reduced FGFR2 protein levels in a concentration-dependent manner.
Did not induce PARP cleavage, with cleaved PARP levels remaining near control levels across all tested concentrations.
Parmacokinetics
| Species | Dose | Route | Tmax | Cmax | T1/2 | MRT | AUClast | AUCinf | F | C0 | Vz | Vss | CL |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Mice[2] | 2 mg/kg | i.v. | / | / | 5.48 h | 2.12 h | 2441 ng·h/mL | 2468 ng·h/mL | / | 6049 ng/mL | 6.40 L/kg | 1.72 L/kg | 13.5 mL/min/kg |
| Mice[2] | 5 mg/kg | i.p. | 0.50 h | 964 ng/mL | 3.85 h | 4.81 h | 6071 ng·h/mL | 6157 ng·h/mL | 99.8 % | / | / | / | / |
| Mice[2] | 10 mg/kg | p.o. | 0.50 h | 69 ng/mL | 5.89 h | 5.79 h | 254 ng·h/mL | 265 ng·h/mL | 2.2 % | / | / | / | / |
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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性状 Solid
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分子量 928.82
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分子式 C44H47Cl2N11O8
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Color Light yellow to yellow
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SMILES
COC1=CC(OC)=C(C(NC(N(C2=CC(NC3=CC=C(C=C3)N4CCN(CC4)C5CCN(CC5)C(CNC6=CC=CC7=C6C(N(C7=O)C8CCC(NC8=O)=O)=O)=O)=NC=N2)C)=O)=C1Cl)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
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
体外:
DMSO : 100 mg/mL (107.66 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. 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. 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 (274 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. 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 | 1.0766 mL | 5.3832 mL | 10.7663 mL | 26.9159 mL |
| 5 mM | 0.2153 mL | 1.0766 mL | 2.1533 mL | 5.3832 mL | |
| 10 mM | 0.1077 mL | 0.5383 mL | 1.0766 mL | 2.6916 mL | |
| 15 mM | 0.0718 mL | 0.3589 mL | 0.7178 mL | 1.7944 mL | |
| 20 mM | 0.0538 mL | 0.2692 mL | 0.5383 mL | 1.3458 mL | |
| 25 mM | 0.0431 mL | 0.2153 mL | 0.4307 mL | 1.0766 mL | |
| 30 mM | 0.0359 mL | 0.1794 mL | 0.3589 mL | 0.8972 mL | |
| 40 mM | 0.0269 mL | 0.1346 mL | 0.2692 mL | 0.6729 mL | |
| 50 mM | 0.0215 mL | 0.1077 mL | 0.2153 mL | 0.5383 mL | |
| 60 mM | 0.0179 mL | 0.0897 mL | 0.1794 mL | 0.4486 mL | |
| 80 mM | 0.0135 mL | 0.0673 mL | 0.1346 mL | 0.3364 mL | |
| 100 mM | 0.0108 mL | 0.0538 mL | 0.1077 mL | 0.2692 mL |
BR-cpd7 関連分類
HY-163705 関連分類
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