Tefinostat
CAS No. : 914382-60-8
(Synonyms: CHR-2845)
| Size | Price | Stock |
|---|---|---|
| 5mg | $290 | In-stock |
| 10mg | $430 | In-stock |
| 50mg | $860 | In-stock |
| 100mg | $1360 | In-stock |
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| 500 mg | Get quote | |
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| Cat. No. : | HY-106409 |
| M.Wt: | 495.61 |
| Formula: | C28H37N3O5 |
| Purity: | >98 % |
| Solubility: | DMSO : 100 mg/mL (ultrasonic) |
Tefinostat (CHR-2845) is a monocyte/macrophage targeted histone deacetylase (HDAC) inhibitor. Tefinostat can be cleaved into active acid CHR-2847 by the intracellular esterase human carboxylesterase-1 (hCE-1). Tefinostat can be used for the research of leukaemias[1].
IC50 & Target:EC50: 57 nM- 2.3 μM (in AML cell lines)[1]
In Vitro:Tefinostat (CHR-2845) (1-4 nM) has efficacy in AML cell lines HL60 (M2 FAB type), MV411 (M4, FLT3-ITD), OCIAML3 (M4 NPM1mut) and THP1 (M5) with EC50 values of 2.3 μM, 57 nM, 110 nM and 560 nM, respectively[1].
Tefinostat (0, 0.5, 1 and 5μM; 24, 48 h) has dose-dependent induction of apoptosis and significant growth inhibitory effects[1].
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