PROTAC FLT3/JAK2/BRD4 Degrader-1
PROTAC FLT3/JAK2/BRD4 Degrader-1 is a PROTAC degrader that target FLT3, JAK2, and BRD4 with DC50 values of 5.23, 0.678, and 1.17 nM, respectively. PROTAC FLT3/JAK2/BRD4 Degrader-1 exhibits potent antiproliferative activity against MV4;11 cells (IC50 = 0.79 nM) and FLT3 mutant-transformed Ba/F3 cells. PROTAC FLT3/JAK2/BRD4 Degrader-1 induces apoptosis in MV4;11 cells. PROTAC FLT3/JAK2/BRD4 Degrader-1 demonstrates significant anti-tumor efficacy in the MV4;11 xenograft model established in NOD SCID mice. PROTAC FLT3/JAK2/BRD4 Degrader-1 can be used for the study of acute myeloid leukemia (AML).
(Pink: FLT3 and BRD4 and JAK2 ligand (HY-175611); Blue: Cereblon ligand (HY-W087383); Black: linker).
For research use only. We do not sell to patients.
- CAS No.: 3067695-20-6
- Formula: C44H51FN10O7S
- Molecular Weight:883.00
-
Storage:
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]
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
All PROTACs Isoforms
More
Biological Activity
|
Cereblon |
BRD4 1.17 nM (DC50) |
JAK2 0.678 nM (DC50) |
FLT3 5.23 nM (DC50) |
PROTAC FLT3/JAK2/BRD4 Degrader-1 (Compound 13e) degrades FLT3, JAK2, and BRD4 in MV4;11 cells with DC50 values of 5.23, 0.678, and 1.17 nM, respectively[1].
PROTAC FLT3/JAK2/BRD4 Degrader-1 (1 μM, 8 h) induces cereblon- and proteasome-dependent degradation via the ubiquitin-proteasome system (UPS) of FLT3, JAK2, and BRD4 in MV4;11 cells[1].
PROTAC FLT3/JAK2/BRD4 Degrader-1 (0.00001-1000 nM, 96 h) potently inhibits MV4;11 cell proliferation with an IC50 of 0.79 nM[1].
PROTAC FLT3/JAK2/BRD4 Degrader-1 (96 h) exhibits potent anti-proliferative activity against FLT3 mutant-transformed Ba/F3 cells, including FLT3-ITD-D835Y (IC50 = 35.64 nM), FLT3-ITD-F691L (IC50 = 24.34 nM ), FLT3-ITD-N676D (IC50 = 43.71 nM ), FLT3-ITD-D835V (IC50 = 6.63 nM ), FLT3-ITD-Y842C (IC50 = 8.80 nM), and FLT3-ITD (IC50 = 28.62 nM )[1].
PROTAC FLT3/JAK2/BRD4 Degrader-1 (1-1000 nM, 48 h) induces over 70% apoptosis in MV4;11 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:MV4;11 cells
-
Concentration:1, 10, 100, 1000 nM
-
Incubation Time:48 h
-
Result:Induced over 70% apoptosis in MV4;11 cells.
Suppressed activated apoptotic proteins PARP, Caspase 9, Caspase 3.
Upregulated Cleaved-caspase 3.
| Species | Dose | Route | T1/2 | Tmax | Cmax | AUC0-t | CL |
|---|---|---|---|---|---|---|---|
| Rat[1] | 10 mg/kg | i.p. | 5.90 h | 0.08 h | 3793 ng/mL | 1862 ng·h/mL | 1.62 mL/min/kg |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:MV4;11 cells (3 × 106) were subcutaneously implanted into the right flanks of four-week-old female nonobese diabetic severe combined immune-deficiency (NOD SCID) mice to establish the MV4;11 xenograft model[1]
-
Dosage:10 mg/kg
-
Administration:i.p., once daily, 21 days
-
Result:Achieved a tumor growth inhibition (TGI) rate of 62% at a dose of 10 mg/kg in the MV4;11 xenograft model.
Showed no significant changes in body weight.
Chemical Information
-
CAS No. 3067695-20-6
-
Molecular Weight 883.00
-
Formula C44H51FN10O7S
-
SMILES
CC1=C(N=C(N=C1)NC2=CC=C(C(F)=C2)N3CCN(CC3)C(CCCCCNC4=CC=C5C(C(N(C5=O)C6CCC(NC6=O)=O)=O)=C4)=O)NC7=CC=CC(NS(C(C)(C)C)(=O)=O)=C7
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PROTAC FLT3/JAK2/BRD4 Degrader-1 Related Classifications
HY-175610 Related Classifications
Powered by Bioz