- RKI1447
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- $5.00 / 5KG
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2019-09-04
- CAS:1342278-01-6
- Min. Order: 1KG
- Purity: 99%
- Supply Ability: 1ton
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| | RKI1447 Basic information |
| Product Name: | RKI1447 | | Synonyms: | CS-855;RKI 1447; RKI1447;RKI 1447;RKI1447;RKI-1447;1-(3-HYDROXYBENZYL)-3-(4-(PYRIDIN-4-YL)THIAZOL-2-YL)UREA;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 | | CAS: | 1342278-01-6 | | MF: | C16H14N4O2S | | MW: | 326.37 | | EINECS: | 200-256-5 | | Product Categories: | Inhibitors | | Mol File: | 1342278-01-6.mol |  |
| | RKI1447 Chemical Properties |
| Melting point | >205oC (dec.) | | density | 1.408±0.06 g/cm3(Predicted) | | storage temp. | -20°C Freezer | | solubility | DMSO (Slightly), Methanol (Slightly, Heated) | | pka | 6.36±0.70(Predicted) | | form | Solid | | color | Pale Yellow to Pale Beige | | InChI | InChI=1S/C16H14N4O2S/c21-13-3-1-2-11(8-13)9-18-15(22)20-16-19-14(10-23-16)12-4-6-17-7-5-12/h1-8,10,21H,9H2,(H2,18,19,20,22) | | InChIKey | GDVRVPIXWXOKQO-UHFFFAOYSA-N | | SMILES | N(CC1=CC=CC(O)=C1)C(NC1=NC(C2C=CN=CC=2)=CS1)=O |
| | RKI1447 Usage And Synthesis |
| Description | RKI-1447 is an inhibitor of the Rho-associated kinases ROCK1 and 2 (IC50s = 14.5 and 6.2 nM, respectively) that functions by binding to the ATP binding site of the kinase. In cancer cells, RKI-1447 at a concentration of 100 nM has been found to suppress the activation of ROCK substrates myosin light chain (MLC)-2 and the MLC phosphatase PP1 regulatory subunit MYPT1 without effect on the phosphorylation of Akt, MEK, or S6 kinase. Furthermore, it can prevent ROCK-mediated migration, invasion, and anchorage-independent growth of MDA-MB-231 breast cancer cells (IC50 = 709 nM). | | Uses | RKI-1447 is a potent and selective ROCK1 and ROCK2 inhibitor with significant anti-invasive and anti-tumor activies. | | in vivo | RKI-1447 is highly effective at inhibiting the outgrowth of mammary tumors in a transgenic mouse model. RKI-1447 inhibits mammary tumor growth by 87% and on average the mammary tumors from RKI-1447 treated mice are 7.7 fold smaller compared to those tumors from mice treated with the vehicle control[1]. | | IC 50 | ROCK2: 6.2 nM (IC50); ROCK1: 14.5 nM (IC50) | | references | [1] patel r a et al. , rki-1447 is a potent inhibitor of the rho-associated rock kinases with anti-invasive and antitumor activities in breast cancer. cancer res, 2012, 72(19): 5025-5034. |
| | RKI1447 Preparation Products And Raw materials |
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