Free shipping on all orders over $ 500
EZM0414 is a potent, selective, oral bioavailable SETD2 inhibitor (IN SETD2 biochemical analysis, IC50=18 nM; In cell analysis, IC50=34 nM). EZM0414 can be used to study relapsed or refractory multiple myeloma and diffuse large B-cell lymphoma.
| 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.
| Molecular Weight | 400.49 |
| Formula | C22H29FN4O2 |
| CAS Number | |
| Purity | N/A |
| Solubility | N/A |
| Storage | at -20°C |
| Related Histone Methyltransferase Products |
|---|
| Onametostat (JNJ-64619178)
Onametostat (JNJ-64619178) is a pseudo-irreversible, orally active, selective protein arginine methyltransferase 5 (PRMT5) inhibitor with an IC50 of 0.14 nM. Good pharmacokinetic properties and safety. |
| VTP50469
VTP50469 is a potent, highly selective and orally active inhibitor of Menin-MLL Interaction with a Ki value of 104 pM. VTP50469 has anti-leukemia activity. |
| GNA002
GNA002 is a potent, selective, covalent EZH2 inhibitor with an IC50 of 1.1 μM against EZH2. GNA002 can specifically and covalently bind Cys668 in the EZH2-SET domain to induce EZH2 degradation through COOH terminal of ubiquitination mediated by Hsp70 interacting protein (CHIP). GNA002 effectively reduced EZH2-mediated H3K27 trimethylation and reactivated tumor suppressor genes silenced by Polycomb repressor complex 2 (PRC2). |
| PF-06726304
Pf-06726304 is an effective selective EZH2 inhibitor. Pf-06726304 inhibited wild type and Y641N mutant EZH2 with Ki of 0.7 and 3.0 nM, respectively. Pf-06726304 has strong anti-tumor growth activity. |
| CPI-169
Cpi-169 (CPI 169 R-Enantiomer) is a novel and effective EZH2 inhibitor, capable of inhibiting the activity of EZH2 WT, EZH2 Y641N and EZH1 with IC50 value of 0.24 nM, respectively. 0.51 nM and 6.1 nM. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.
