[CAS NO. 2064175-41-1] FKBP12PROTACdTAG-13
PRODUCTS SPECIFICATIONS [2064175-41-1]
DESCRIPTION [2064175-41-1]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 1049.17 |
| Molecular Formula | C57H68N4O15 |
| SMILES | COC1=CC=C(CC[C@H](C2=C(OCC(NCCCCCCOC3=CC=CC4=C3C(N(C5CCC(NC5=O)=O)C4=O)=O)=O)C=CC=C2)OC([C@@H]6CCCCN6C([C@@H](CC)C7=CC(OC)=C(OC)C(OC)=C7)=O)=O)C=C1OC |
Summary
IC50 & Target
|
Cereblon |
FKBP12(F36V) |
In Vitro
TAG-13 (1-1000 nM; 4 hours; 293FT
WT
cells) treatment potently reduces FKBP12
F36V
-Nluc levels in 293FT
WT
cell, indicating the requirement of CRBN for the observed effects
[1]
.
Treatment of MV4;11 cells expressing BRD4(short)-FKBP12
F36V
with dTAG-13 leads to robust degradation of BRD4. dTAG-13 treatment leads to rapid degradation of BRD4 within one hou. dTAG-13 treatment leads to rapid and potent degradation of the BRD4 fusion chimera in the heterozygous and homozygous knock-in clones, with no effect on endogenous FKBP12
WT
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Western Blot Analysis [1]
| Cell Line: | 293FT WT cells |
| Concentration: | 1 nM, 10 nM, 100 nM, 1000 nM |
| Incubation Time: | 4 hours |
| Result: | Potently reduced FKBP12 F36V -Nluc levels in 293FT WT cell. |
In Vivo
Following bone marrow engraftment of MV4;11 cells expressing luc-FKBP12F36V in mice, the bioluminescent signal after vehicle or dTAG-13 administration is monitored. A significant, rapid, and durable effect on bioluminescent signal is observed four hours after dTAG-13 administration, indicating effective degradation of luc-FKBP12F36V. Twenty-eight hours following the final treatment, the recovery of cellular bioluminescence to levels comparable between vehicle and dTAG-13 treatment groups is observed [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 180 mg/mL ( 171.56 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 0.9531 mL | 4.7657 mL | 9.5313 mL |
| 5 mM | 0.1906 mL | 0.9531 mL | 1.9063 mL |
| 10 mM | 0.0953 mL | 0.4766 mL | 0.9531 mL |