2. PROTAC Epigenetics Apoptosis
  3. PROTACs Epigenetic Reader Domain c-Myc Apoptosis
  4. CFT-2718

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).

For research use only. We do not sell to patients.

CFT-2718

CFT-2718 Chemical Structure

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

CFT-2718 Related Antibodies

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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Description

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[1]. (Pink: BRD4 ligand (HY-132942); Blue: Cereblon ligand (HY-A0003); Black: linker).

IC50 & Target[1]

BRD4

 

In Vitro

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.

CFT-2718 Related Antibodies

Western Blot Analysis[1]

Cell Line: SCLC cell lines H69, H446; pancreatic cancer cell lines PNX-001, PNX-017
Concentration: 10 nM
Incubation Time: 2, 6, 12, 24 h
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).
Parmacokinetics
Species Dose Route C0 T1/2 Vdss CL AUC0-last
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
In Vivo

CFT-2718 (2-3 mg/kg; i.v.; once weekly; 3 weeks) is well-tolerated at 2 mg/kg with no significant body weight loss, but causes 9-17% body weight loss at 3 mg/kg in female BALB/c nude mice[1].
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.

Animal Model: C.B17 scid with PNX-001 and PNX-017 pancreatic cancer cells[1]
Dosage: 1.8 mg/kg
Administration: Retro-orbital injection; once weekly; 3 weeks
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.
Molecular Weight

811.37

Formula

C45H47ClN10O3
Appearance

Solid

Color

Off-white to pink

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.2325 mL 6.1624 mL 12.3248 mL
5 mM 0.2465 mL 1.2325 mL 2.4650 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.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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This equation is commonly abbreviated as: C1V1 = C2V2

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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.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.87%

SDS (252 KB)

COA (247 KB) HNMR (329 KB) LCMS (324 KB)

Handling Instructions (2659 KB)
References

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
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CFT-2718 Related Classifications

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:

CFT-2718CFT2718CFT 2718PROTACsEpigenetic Reader Domainc-MycApoptosisMycsmall-cell lung cancerBRD4293T cellsCRBNMYCLX-36pancreatic cancerRPB1MOLT4 CRBN?/? cellsPNX-001Inhibitorinhibitorinhibit

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