945614-12-0
Chemical Structure
Pexmetinib
Synonym(s): ARRY-614
- CAS No.: 945614-12-0
- Formula:C31H33FN6O3
- Molecular Weight:556.63
IUPAC Name: 1-(3-(tert-butyl)-1-(p-tolyl)-1H-pyrazol-5-yl)-3-(5-fluoro-2-((1-(2-hydroxyethyl)-1H-indazol-5-yl)oxy)benzyl)urea
InChIKey: LNMRSSIMGCDUTP-UHFFFAOYSA-N
SMILES: O=C(NCC1=CC(F)=CC=C1OC2=CC3=C(N(CCO)N=C3)C=C2)NC4=CC(C(C)(C)C)=NN4C5=CC=C(C)C=C5
Biological Activity: Pexmetinib (ARRY-614) is an orally active dual Tie-2 and p38 MAPK inhibitor. Pexmetinib binds to Tie-2 and p38 MAPK in a "DFG-out" conformation, attenuates the phosphorylation of p38, inhibits STAT3 activation, reduces the promoter-binding activity of NFATc1, and decreases the expression of MMPs. Pexmetinib inhibits leukemia cell proliferation, abrogates TNF-α-mediated myelosuppression of healthy hematopoietic stem cells, stimulates hematopoiesis in primary myelodysplastic syndrome (MDS) samples, inhibits RANKL-induced osteoclast formation and bone resorption, and suppresses migration, invasion and induced osteolysis of breast cancer cells. Pexmetinib can be used in research related to myelodysplastic syndrome, acute myeloid leukemia and breast cancer-induced osteolysis[1][2].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
|
|
Pexmetinib | 99.81% | Pexmetinib (ARRY-614) is an orally active dual Tie-2 and p38 MAPK inhibitor. Pexmetinib binds to Tie-2 and p38 MAPK in a "DFG-out" conformation, attenuates the phosphorylation of p38, inhibits STAT3 activation, reduces the promoter-binding activity of NFATc1, and decreases the expression of MMPs. Pexmetinib inhibits leukemia cell proliferation, abrogates TNF-α-mediated myelosuppression of healthy hematopoietic stem cells, stimulates hematopoiesis in primary myelodysplastic syndrome (MDS) samples, inhibits RANKL-induced osteoclast formation and bone resorption, and suppresses migration, invasion and induced osteolysis of breast cancer cells. Pexmetinib can be used in research related to myelodysplastic syndrome, acute myeloid leukemia and breast cancer-induced osteolysis. | ||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
|
|
Pexmetinib (Standard) | ≥98% | Pexmetinib (Standard) (ARRY-614 (Standard)) is the analytical standard of Pexmetinib (HY-16782). This product is intended for research and analytical applications. Pexmetinib (ARRY-614) is an orally active dual Tie-2 and p38 MAPK inhibitor. Pexmetinib binds to Tie-2 and p38 MAPK in a "DFG-out" conformation, attenuates the phosphorylation of p38, inhibits STAT3 activation, reduces the promoter-binding activity of NFATc1, and decreases the expression of MMPs. Pexmetinib inhibits leukemia cell proliferation, abrogates TNF-α-mediated myelosuppression of healthy hematopoietic stem cells, stimulates hematopoiesis in primary myelodysplastic syndrome (MDS) samples, inhibits RANKL-induced osteoclast formation and bone resorption, and suppresses migration, invasion and induced osteolysis of breast cancer cells. Pexmetinib can be used in research related to myelodysplastic syndrome, acute myeloid leukemia and breast cancer-induced osteolysis. | ||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
References
- [1]. Bachegowda L, et al. Pexmetinib: A Novel Dual Inhibitor of Tie2 and p38 MAPK with Efficacy in Preclinical Models of Myelodysplastic Syndromes and Acute Myeloid Leukemia. Cancer research. 2016 Aug 15;76(16):4841-4849. [Content Brief]
- [2]. Jie Z, et al. Pexmetinib suppresses osteoclast formation and breast cancer induced osteolysis via P38/STAT3 signal pathway. Journal of bone oncology. 2022 Aug;35:100439.
