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FKBP12 PROTAC dTAG-13 is a PROTAC and selective degrader that can be used for target validation during drug discovery by splicing FKBP12 F36V with CRBN and thereby degrading FKBP12 F36V.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $74 | In Stock | |
5 mg | $163 | In Stock | |
25 mg | Inquiry | In Stock |
Description | FKBP12 PROTAC dTAG-13 is a PROTAC and selective degrader that can be used for target validation during drug discovery by splicing FKBP12 F36V with CRBN and thereby degrading FKBP12 F36V. |
In vitro | FKBP12 PROTAC dTAG-13 selectively degrades FKBP12^F36V fusion proteins without affecting wild-type FKBP12. In 293T, PATU-8988T, and EOL-1 cells, FKBP12 PROTAC dTAG-13 (500 nM, 4 h) effectively degraded FKBP12^F36V-KRAS^G12V or FKBP12^F36V-ABL1 and suppressed downstream signaling. Dose-dependent degradation was observed from 10 to 500 nM[1]. |
In vivo | In NOD/SCID mice bearing PATU-8988T FKBP12^F36V-KRAS^G12V xenografts, a single intraperitoneal dose of FKBP12 PROTAC dTAG-13 (35 mg/kg) reduced fusion protein levels in tumors within 2 h, lasting ≥12 h[1]. |
Alias | dTAG-13 |
Molecular Weight | 1049.17 |
Formula | C57H68N4O15 |
Cas No. | 2064175-41-1 |
Smiles | O=C1C=2C(C(=O)N1C3C(=O)NC(=O)CC3)=CC=CC2OCCCCCCNC(COC4=C([C@H](OC(=O)[C@H]5N(C([C@@H](CC)C6=CC(OC)=C(OC)C(OC)=C6)=O)CCCC5)CCC7=CC(OC)=C(OC)C=C7)C=CC=C4)=O |
Relative Density. | 1.260 g/cm3 (Predicted) |
Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 80 mg/mL (76.25 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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