PROTAC BCR-ABL Degrader-2
PROTAC BCR-ABL Degrader-2 is a selective Bcr-AblT315 PROTAC degrader with a DC50 of 108.7 nM in Ba/F3 Bcr-AblT315I cells. PROTAC BCR-ABL Degrader-2 exhibits the most potent degradation efficacy with DR of 69.89% and 94.23% at 100 and 300 nM, respectively. PROTAC BCR-ABL Degrader-2 demonstrates high plasma exposure, and induces significant tumor regression and induces tumor cell apoptosis with a good safety profile in vivo. PROTAC BCR-ABL Degrader-2 can be used for chronic myeloid leukemia (CML) research.
(Pink: Bcr-Abl ligand (HY-15666); Blue: Cereblon ligand (HY-10984); Black: linker).
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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。
- CAS 番号: 2703834-25-5
- 分子式: C48H46F3N9O6
- 分子量:901.93
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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
- 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
体外実験
PROTAC BCR-ABL Degrader-2 (Compound 7o) (72 h) against K562, Ba/F3 Bcr-AbllT315I and Ba/F3 Bcr-AblWT with IC50s of 7.7, 26.8 and 4.2 nM[1].
PROTAC BCR-ABL Degrader-2 (0-300 nM) significantly decreases the level of Bcr-AblT315I protein with a DC50 = 108.7 nM in Ba/F3 Bcr-AblT315I cells[1].
PROTAC BCR-ABL Degrader-2 (0-300 nM, 0-48 h) induces Bcr-AblT315I protein level mediated by CRBN E3 ubiquitin pathway while appeared a “hook” effect in Bcr-AbllT315I cell[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Ba/F3 Bcr-AblT315I and K562 cells
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Concentration:100 nM
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Incubation Time:0, 1, 2, 4, 6, 8, 10, 12, 24, 36 and 48 h
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Result:Caused the degradation of Bcr-AblT315I protein in a time-dependent manner.
Reduced Bcr-AblT315I protein level substantially after 6h treatment while appeared a “hook” effect during 8-10h treatment.
Observed the maximum degradation after24h treatment.
Displayed a different trend for reducing Bcr-AblWT in K562cells with substantially reduction after 36h treatment (this different might be associated with the different states of E3 ligase in Ba/F3Bcr-AblT315I and K562 cells.).
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Cell Line:MG132 (HY-13259) (20 ) Ba/F3 Bcr-AblT315I cells
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Concentration:100 and 300 nM
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Incubation Time:24 h
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Result:Induced Bcr-AblT315I degradation rescuing by MG132.
体内実験
PROTAC BCR-ABL Degrader-2 (10-20 mg/kg, i.p., once every two days for 14 days) displays significant anti-cancer activity and safety in the Ba/F3 Bcr-AblT315I mice xenograft models[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Ba/F3 cells expressing Bcr-AblT315I (2 x 106 cells/0.1 mL) induced-CB17-SCID mice [1]
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Dosage:10 or 20 mg/kg
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Administration:i.p., once every two days for 14 days
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Result:Obviously sup pressed the growth of Ba/F3 Bcr-AblT315I xenograft tumor with a tumor growth inhibition (TGI) value of 90.8% at the dose of 20 mg/kg.
Induced the Bcr-AblT315I degradation and apoptosis.
Resulted no mortality or significant body weight loss.
化学情報
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CAS 番号 2703834-25-5
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分子量 901.93
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分子式 C48H46F3N9O6
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SMILES
O=C(C1=CC=C(C)C(C#CC2=CC3=C(NN=C3)N=C2)=C1)NC4=CC=C(CN5CCN(CCCCCCC(NC6=CC=CC(C(N7C8C(NC(CC8)=O)=O)=O)=C6C7=O)=O)CC5)C(C(F)(F)F)=C4
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[1]. Jiang L, et al. Design, synthesis, and biological evaluation of Bcr-Abl PROTACs to overcome T315I mutation. Acta Pharm Sin B. 2021 May;11(5):1315-1328. [Content Brief]
[2]. Chen X, et al. Mighty mini-PROTACs: an emerging class of degraders. Eur J Med Chem. 2026 Jan 5;301:118202. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
PROTAC BCR-ABL Degrader-2 関連分類
HY-180967 関連分類
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