RKI-1447

Min.Order / FOB Price:Get Latest Price

100 Gram	FOB Price: USD 1.0000

100 Gram

FOB Price: USD 1.0000

Min.Order :100 Gram
Purity: 98%
Payment Terms : L/C

Keywords

RKI-1447 RKI 1447;RKI1447;RKI-1447;Urea, N-[(3-hydroxyphenyl)methyl]-N'-[4-(4-pyridinyl)-2-thiazolyl]-;1-(3-Hydroxybenzyl)-3-[4-(pyridin-4-yl)thiazol-2-yl]urea RKI 1447;RKI 1447 1-(3-Hydroxybenzyl)-3-[4-(pyrid 1342278-01-6

Quick Details

Appearance:light yellow solid
Application:CAS：1342278-01-6； RKI 1447;RKI1447;RKI-1447;Urea, N-[(3-hydroxyphenyl)methyl]-N'-[4-(4-pyridinyl)-2-thiazolyl]-;1-(3-Hydroxybenzyl)-3-[4-(pyridin-4-yl)thiazol-2-yl]urea RKI 1447;RKI 1447 1-(3-Hydro
PackAge:100g,500g,1kg,25kg
ProductionCapacity:1000|Gram|Month
Storage:Dry seal
Transportation:shipping

Superiority:

We are specialized in custom synthesis, chemical/pharmaceutical/ pesticides outsourcing and contract research.

We are committed to provide excellence in researching, manufacturing and drug discovery process.

Our research team of scientists consists of western-trained Ph.D.s with experience and capabilities in drug R&D methodologies and medicinal chemistry.

Details:

RKI-1447 is a potent small molecule inhibitor of ROCK1 and ROCK2.
IC50 Value: 15.4 nM (ROCK1); 6.2 nM (ROCK2) [1]
Target: ROCK1/2
in vitro: RKI-1447 inhibits potently ROCK1 and ROCK2 in a dose-dependent manner with IC50 values of 14.5 nM and 6.2 nM, respectively. RKI-1447 suppressed phosphorylation of the ROCK substrates MLC-2 and MYPT-1 in human cancer cells, but had no effect on the phosphorylation levels of the AKT, MEK, and S6 kinase at concentrations as high as 10 μmol/L. RKI-1447 was also highly selective at inhibiting ROCK-mediated cytoskeleton re-organization (actin stress fiber formation) following LPA stimulation, but does not affect PAK-meditated lamellipodia and filopodia formation following PDGF and Bradykinin stimulation, respectively. RKI-1447 inhibited migration, invasion and anchorage-independent tumor growth of breast cancer cells [1].
in vivo: Mammary tumors were measured beginning at the time of tumor onset and treatment (once a day for 14 days) with vehicle (20% HPCD) or RKI-1447 (200 mpk/day) began when tumor volumes reached 75 to 2,300 mm3. A wide range of tumor volumes was used to ensure that responses were not volume dependent [1].

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