SML3792
MRIA9 Trifluoroacetate
≥96% (HPLC)
别名:
8-(((2r,5r)-5-Amino-1,3-dioxan-2-yl)methyl)-6-(2-chloro-4-(3-fluoropyridin-2-yl)phenyl)-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one trifluoroacetate, 8-[(trans -5-Amino-1,3-dioxan-2-yl)methyl]-6-[2-chloro-4-(3-fluoro-2-pyridinyl)phenyl]-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one trifluoroacetate
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关于此项目
经验公式（希尔记法）:
C24H22ClFN6O3 · xC2HF3O2
分子量:
496.92 (free base basis)
UNSPSC Code:
12352200
NACRES:
NA.21
MDL number:
SMILES string
Fc1c(nccc1)c2cc(c(cc2)C3=Cc4c(nc(nc4)NC)N(C3=O)C[C@@H]5OC[C@H](CO5)N)Cl
InChI key
QKNBRNSGPNCARD-SGNKCFNYSA-N
assay
≥96% (HPLC)
form
powder
storage condition
desiccated
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
-10 to -25°C
Quality Level
Biochem/physiol Actions
ATP site-targeting, dual salt-inducible kinase (SIK1/2/3) & p21-activated kinase (PAK2/3) inhibitor with excellent selectivity over other kinases.
MRIA9 is an ATP site-targeting, dual salt-inducible kinase (SIK1/2/3 IC50 = 55/48/22 nM; SIK2/3 IC50 = 180/127 nM by cell-based NanoBRET) & p21-activated kinase (PAK2/3 IC50 = 41/140 nM; PAK1 IC50 = 580 nM) inhibitor with excellent selectivity over other kinases. MRIA9 sensitizes ovarian cancer cells to mitotic agent paclitaxel (Pac) treatment in SKOV3 cultures (1 nM Pac plus 0.5-5 µM MRIA9) and HeLa spheroids (2 nM Pac plus 5 µM MRIA9).
Disclaimer
Hygroscopic
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
新产品
此项目有
Roberta Tesch et al.
Journal of medicinal chemistry, 64(12), 8142-8160 (2021-06-05)
Salt-inducible kinases (SIKs) are key metabolic regulators. The imbalance in SIK function is associated with the development of diverse cancers, including breast, gastric, and ovarian cancers. Chemical tools to clarify the roles of SIK in different diseases are, however, sparse
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