TD-1092 is a pan-inhibitor of apoptosis (IAP) degrader with two different types of E3 ligase conjugates, IAP and CRBN, that induces proteasomal degradation of cIAP2 and XIAP in a CRBN-dependent manner. TD1092 also activates apoptotic proteases (apoptosis 3/7) and leads to apoptosis by promoting IAP degradation. In addition, TD1092 also blocks the TNFα-mediated NF-κB signaling pathway and inhibits the phosphorylation of IKK, IkBα, p65, and p38. TD1092 can be used as a PROTAC for cancer research.
| Molecular Weight | 987.19 |
| Formula | C55H70N8O9 |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related IAP Products |
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| Sanggenon G
Sanggenon G is a cell-permeable and potent inhibitor of X-linked inhibitor of apoptosis protein (XIAP). |
| LBW242
LBW242, a 3-mer and Smac mimetic, is a potent and orally active proapoptotic IAP inhibitor. LBW242 shows effects on mutant FLT3-expressing cells. LBW242 has activity against multiple myeloma, and potentiates TRAIL- and anticancer agent-mediated cell death of ovarian cancer cells. |
| UC-112
UC-112 is a novel potent IAP(Inhibitor of apoptosis) inhibitor. UC-112 potently inhibit cell growth in two human melanoma (A375 and M14) and two human prostate (PC-3 and DU145) cancer cell lines(IC50=0.7-3.4 uM). |
| SBP-0636457
SBP-0636457 (SB1-0636457) is a SMAC mimetic, and as an IAP antagonist. SBP-0636457 binds to the BIR-domains of the IAP proteins, with a Ki of 0.27 μM. SBP-0636457 can be used for the research of solid tumors and hematologic cancers. |
| XIAP/cIAP1 antagonist-1
XIAP/cIAP1 antagonist-1 is a potent and orally active XIAP/cIAP1 antagonist with EC50s of 5.1 nM and 0.32 nM for XIAP and cIAP1, respectively. XIAP/cIAP1 antagonist-1 inhibits the tumor growth in dose-dependent manner in vivo. |
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