SLV-2436
SLV-2436 Basic information
- Product Name:
- SLV-2436
- Synonyms:
-
- SLV-2436
- SEL-201
- 5-(3-Amino-1H-indazol-6-yl)-1-(3-chlorob...
- SEL201-88
- V-2436
- 2(1H)-Pyridinone, 5-(3-amino-1H-indazol-6-yl)-1-[(3-chlorophenyl)methyl]-
- MAP kinase interacting kinase,SEL 201,inhibit,SLV-2436,SEL201,SLV2436,MAPK interacting kinase,Mitogen activated protein kinase interacting kinase,Inhibitor,MNK
- 5-(3-amino-1H-indazol-6-yl)-1-(3-chlorobenzyl)pyridin-2(1H)-one
- CAS:
- 2095704-43-9
- MF:
- C19H15ClN4O
- MW:
- 350.8
- Mol File:
- 2095704-43-9.mol
SLV-2436 Chemical Properties
- storage temp.
- Store at -20°C
- solubility
- DMSO : ≥ 100 mg/mL (285.06 mM)
- form
- Solid
- color
- Light brown to brown
SLV-2436 Usage And Synthesis
Uses
SLV-2436 is a highly potent and ATP-competitive inhibitor of MNK1 and MNK2 with IC50s of 10.8 nM and 5.4 nM, respectively.
in vivo
To investigate the pharmacodynamic properties of SLV-2436 (SEL201), 5 consecutive oral doses of 10, 25, and 50 mg/kg are administered to mice every 12 hours (twice-daily schedule). At the 10 mg/kg twice-daily dosage, 4 hours after the fifth administration, a low plasma concentration of 125 ng/mL SLV-2436 is determined. However, dosing at 25 and 50 mg/kg twice daily, equivalent to 50 and 100 mg/kg/d of SLV-2436, yields substantially increased dose-dependent plasma exposure, reaching an average level of 1,299 ng/mL and 2,075 ng/mL, respectively. At the 24-hour time point, SLV-2436 is still detectable in the plasma, with dose-dependent concentrations of 9, 73, and 124 ng/mL in the 10, 25, and 50 mg/kg twice-daily treatment groups. Oral (p.o.) administration of SLV-2436 at the dosage of 50 mg/kg twice daily, that is, 100 mg/kg/d, for 37 days is well tolerated in mice[1].
IC 50
MNK2: 5.4 nM (IC50); MNK1: 10.8 nM (IC50)
References
[1] Zhan Y, et al. MNK1/2 inhibition limits oncogenicity and metastasis of KIT-mutant melanoma. J Clin Invest. 2017 Nov 1;127(11):4179-4192. DOI:10.1172/JCI91258
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