TL4-12 is a selective MAP4K2/GCK inhibitor, dose-dependently downregulates IKZF1 and BCL-6 and leads to MM cell proliferation inhibition (IC50=37 nM) accompanied by induction of apoptosis. TL4-12 can be used to overcome immunomodulatory agent resistance in multiple myeloma (MM).
| Molecular Weight | 500.52 |
| Formula | C25H27F3N6O2 |
| CAS Number | 1620820-12-3 |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| 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 MAPKAPK2/MAP3K/MAP4K Products |
|---|
| MAP4K4-IN-3
MAP4K4-IN-3 is a potent and selective MAP4K4 inhibitor with an IC50 of 14.9 nM in kinase assay, and an IC50 of 470 nM in cell assay. |
| PROTAC MLKL Degrader-1
PROTAC MLKL Degrader-1 is a PROTAC degrader of MLKL, with a Dmax ＞90%. |
| HPK1-IN-37
HPK1-IN-37 is an inhibitor of HPK1 (IC50=3.7 nM). |
| GNE-6893
GNE-6893 is a potent and orally active HPK1 inhibitor. |
| HPK1-IN-39
HPK1-IN-39 is a selective HPK1 Inhibitor (IC50: 29 nM). |
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