PROTAC FLT-3 degrader 1
CAS No. : 2230826-81-8
| Size | Price | Stock |
|---|---|---|
| 1mg | $120 | In-stock |
| 5mg | $360 | In-stock |
| 10mg | $580 | In-stock |
| 25mg | $1220 | In-stock |
| 50mg | $1980 | In-stock |
| 100mg | $3200 | In-stock |
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| Cat. No. : | HY-114323 |
| M.Wt: | 1020.23 |
| Formula: | C52H61N9O9S2 |
| Purity: | >98 % |
| Solubility: | DMSO : 150 mg/mL (ultrasonic) |
PROTAC FLT-3 degrader 1 is an effective and selective FLT-3 PROTAC degrader with an IC50 of 0.6 nM. PROTAC FLT-3 degrader 1 inhibits both FLT-3 and FLT-3 ITD mutants. PROTAC FLT-3 degrader 1 has the activity of anti-proliferation and induction of apoptosis, which can be used in the study of tumor. (Pink: FLT3 ligand (HY-168702); Black: Linker (HY-124380); Blue: VHL ligand (HY-125845))[1].
In Vitro: PROTAC FLT-3 degrader 1 (0.05 nM-1 μM; 24 h) induces FLT-3 ITD protein degradation and inhibits downstream STAT-5, MEK and ERK phosphorylation, and has anti-proliferation and apoptosis-inducing activities in MV4-11 cells[1].
In Vivo: PROTAC FLT-3 degrader 1 (30 mg/kg; Intraperitoneal injection; 3 days) can degrade FLT-3 protein in mouse tumor model[1].
Pharmacokinetic Analysis in Mouse[1]
| Route | Dose (mg/kg) | Cmax (ng/mL) | Tmax (hr) | t1/2 (hr) | Plasma Protein Binding |
| i.p. | 10 | 1069 | 2 | 2.31 | 98.0 % |