CFT-2718
Based on 1 Customer Validation
CFT-2718 is a selective CRBN-dependent BRD4 PROTAC degrader. CFT-2718 mediates rapid, selective BRD4 degradation, reduces total and phosphorylated Ser2 RPB1 levels, and reduces MYC protein levels. CFT-2718 can inhibit cancer cells proliferation and induce apoptosis. CFT-2718 reduces growth of lung cancer and pancreatic patient-derived xenograft models. CFT-2718 can be used for the research of cancer, such as small-cell lung cancer and pancreatic cancer.
(Pink: BRD4 ligand (HY-132942); Blue: Cereblon ligand (HY-A0003); Black: linker).
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- Pureté: 99.87%
- Formule: C45H47ClN10O3
- Masse moléculaire:811.37
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Stockage:Powder -20°C, 3 years , 4°C, 2 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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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BRD4 |
CFT-2718 (0.01-1000 nM; 3 h) potently induces BRD4 degradation in 293T cells with endogenously tagged BRD4, achieving 90% degradation at 10 nM after 3 hours of treatment[1].
CFT-2718 (0.01-1000 nM; 72 h) reduces viability of MOLT4 CRBN+/+ acute lymphoblastic leukemia cells in a concentration-dependent manner, killing ~75% of cells at 10 nM after 72 hours of treatment[1].
CFT-2718 (0.1-10 nM; 2 h) induces rapid, concentration-dependent, CRBN-mediated BRD4 degradation in MOLT4 CRBN+/+ cells[1].
CFT-2718 (72 h) reduces viability of SCLC and pancreatic cancer cell lines in a concentration-dependent manner, with IC50 values of 0.02, 0.47, 6.33 and 578 nM for H69, H446, PNX-001 and PNX-017 cells[1].
CFT-2718 (10 nM; 2-24 h) potently induces apoptosis (measured via PARP cleavage) in H69, H446 and PNX-017 cells and no activity in PNX-001 pancreatic cells[1].
CFT-2718 (10 nM; 2-24 h) induces rapid, sustained BRD4 degradation in H69 and H446 SCLC cells (detected within 2 hours) and delayed but sustained degradation in PNX-001 and PNX-017 pancreatic cells (detected by 6 hours)[1].
CFT-2718 (10 nM；2-24 h) potently and persistently inhibits transcriptional signaling (reducing pSer2, pSer5, and total RPB1 levels) and reduces MYC expression in H69 and H446 SCLC cells, and PNX-001 and PNX-017 pancreatic cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SCLC cell lines H69, H446; pancreatic cancer cell lines PNX-001, PNX-017
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Concentration:10 nM
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Incubation Time:2, 6, 12, 24 h
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Result:Induced rapid BRD4 degradation in H69 and H446 SCLC cells, with significant reduction observed within 2 hours and sustained through 24 hours.
Caused marked BRD4 reduction in PNX-001 and PNX-017 pancreatic cells by 6 hours, which remained depressed through 24 hours.
Significantly reduced levels of pSer2, pSer5, and total RPB1 in all four cell lines within 6 hours, with pSer2 levels remaining strongly depressed through 24 hours.
Reduced MYC expression in all cell lines: maximal loss occurred by 2 hours in H69 and H446 SCLC cells (with sustained suppression through 24 hours) and by 6 hours in PNX-001 and PNX-017 pancreatic cells (with partial rebound of MYC levels over time).
| Species | Dose | Route | C0 | T1/2 | Vdss | CL | AUC0-last |
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| Mice[1] | 3 mg/kg | i.v. | 36087 ng/mL | 5.15 h | 1.24 L/kg | 41.8 mL/min/kg | 1194 ng·h/mL |
CFT-2718 (1-1.8 mg/kg; retro-orbital injection; once weekly; 2 weeks) is well-tolerated in C.B17 scid mice, and causes statistically significant reduction in liver BRD4 expression without inducing significant caspase-3-mediated apoptosis[1].
CFT-2718 (1.8 mg/kg; i.v.; once weekly; 3 weeks) inhibits RS4;11 acute lymphoblastic leukemia xenograft growth in mice[1].
CFT-2718 (1.8 mg/kg; retro-orbital injection; once weekly; 3 weeks) is significantly more effective than the control agent at inhibiting LX-36 small-cell lung cancer PDX tumor growth, and induces significant BRD4 degradation in tumor tissue[1].
CFT-2718 (1.8 mg/kg; retro-orbital injection; once weekly; 3 weeks) inhibits PNX-001 and PNX-017 pancreatic cancer PDX tumor growth, induces significant BRD4 degradation in tumor tissue, and causes transient, mild body weight loss[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C.B17 scid with PNX-001 and PNX-017 pancreatic cancer cells[1]
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Dosage:1.8 mg/kg
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Administration:Retro-orbital injection; once weekly; 3 weeks
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Result:Inhibited PNX-001 and PNX-017 tumor growth at endpoint stage compared with vehicle.
Induced a statistically significant reduction in BRD4 H-score in excised tumor tissue compared with vehicle.
Caused a statistically significant reduction in body weight compared with vehicle and control agent groups, though this did not exceed 10% at any point.
Chemical Information
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Appearance Solid
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Masse moléculaire 811.37
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Formule C45H47ClN10O3
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Color Off-white to pink
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SMILES
O=C1N(CC2=C(C=CC=C21)N[C@@H]3CCN(C3)CCCCCCN4N=CC(C5=CC6=C(C=C5)N7C(C)=NN=C7C8(CC8)N=C6C9=CC=C(C=C9)Cl)=C4)C%10C(NC(CC%10)=O)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 100 mg/mL (123.25 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
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Fiche technique (276 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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Instruction de manipulation (2659 KB)
Références
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 | 1.2325 mL | 6.1624 mL | 12.3248 mL | 30.8121 mL |
| 5 mM | 0.2465 mL | 1.2325 mL | 2.4650 mL | 6.1624 mL | |
| 10 mM | 0.1232 mL | 0.6162 mL | 1.2325 mL | 3.0812 mL | |
| 15 mM | 0.0822 mL | 0.4108 mL | 0.8217 mL | 2.0541 mL | |
| 20 mM | 0.0616 mL | 0.3081 mL | 0.6162 mL | 1.5406 mL | |
| 25 mM | 0.0493 mL | 0.2465 mL | 0.4930 mL | 1.2325 mL | |
| 30 mM | 0.0411 mL | 0.2054 mL | 0.4108 mL | 1.0271 mL | |
| 40 mM | 0.0308 mL | 0.1541 mL | 0.3081 mL | 0.7703 mL | |
| 50 mM | 0.0246 mL | 0.1232 mL | 0.2465 mL | 0.6162 mL | |
| 60 mM | 0.0205 mL | 0.1027 mL | 0.2054 mL | 0.5135 mL | |
| 80 mM | 0.0154 mL | 0.0770 mL | 0.1541 mL | 0.3852 mL | |
| 100 mM | 0.0123 mL | 0.0616 mL | 0.1232 mL | 0.3081 mL |
CFT-2718 Related Classifications
HY-132941 Related Classifications
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