| Chemical Properties | Back Directory | [storage temp. ]
4°C, away from moisture | [solubility ]
DMSO : 200 mg/mL (388.72 mM; Need ultrasonic) | [form ]
Solid | [color ]
White to light yellow |
| Hazard Information | Back Directory | [Uses]
EZM0414 TFA is the TFA salt form of EZM0414 (HY-144858). EZM0414 TFA is a potent, selective, orally active inhibitor of SETD2 (IC50=18 nM in SETD2 biochemical assay; IC50=34 nM in cellular assay). EZM0414 TFA can be used for the research of relapsed or refractory multiple myeloma and diffuse large B-cell lymphoma[1]. | [Biological Activity]
SETD2-IN-1 TFA is a potent, selective and orally active inhibitor of SETD2 which is a human histone methyltransferase. SETD2-IN-1 TFA has anti-proliferative effects[1]. | [in vivo]
EZM0414 (15 和 30 mg/kg, p.o., twice a day for 35 days) inhibits tumor growth in NOD SCID mouse xenograft model implanted with human KMS-11 cells, and is well-tolerated[3].
EZM0414 (50 mg/kg, p.o.) shows almost 100% oral bioavailability in rats and mice, t1/2 of 1.8 h (mice)and 3.8 h (rats)[3]. | Animal Model: | KMS-11 Xenograft mouse models[3] | | Dosage: | 15-30 mg/kg | | Administration: | po, twice a day for 35 days | | Result: | Inhibited tumor growth. |
| [IC 50]
SETD2/KMT3A | [References]
[1]. John Lampe, et al. Substituted indoles and methods of use thereof. WO2020037079A1. |
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| Company Name: |
ABBIOCHEM
|
| Telephone: |
021-18964309092 18964309092 |
| Website: |
www.abbiochemical.com |
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