|
|
| | LY 345899) Basic information |
| Product Name: | LY 345899) | | Synonyms: | LY 345899);LY-345899
(LY345899;L-Glutamic acid, N-[4-(3-amino-1,2,5,6,6a,7-hexahydro-1,9-dioxoimidazo[1,5-f]pteridin-8(9H)-yl)benzoyl]-;(2S)-2-(4-(3-Amino-1,9-dioxo-1,2,5,6,6a,7-hexahydroimidazo[1,5-f]pteridin-8(9H)-yl)benzamido)pentanedioic acid;inhibit,LY345899,LY-345899,Inhibitor,LY 345899,Methylenetetrahydrofolate Dehydrogenase (MTHFD) | | CAS: | 10538-99-5 | | MF: | C20H21N7O7 | | MW: | 471.42 | | EINECS: | | | Product Categories: | | | Mol File: | 10538-99-5.mol |  |
| | LY 345899) Chemical Properties |
| density | 1.82±0.1 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | DMSO:125.0(Max Conc. mg/mL);265.16(Max Conc. mM) | | form | A solid | | pka | 3.46±0.10(Predicted) |
| | LY 345899) Usage And Synthesis |
| Biological Activity | LY 345899, a folate analog, is also a methylenetetrahydrofolate dehydrogenase (MTHFD1; DC301) and MTHFD2 inhibitor with IC50 values of 96 nM and 663 nM, respectively, and Ki value for MTHFD1 of 18 nM. | | in vitro | LY 345899 could suppress the MTHFD enzyme in the cytoplasm and mitochondria.
LY 345899 could disturb the NADPH and redox homeostases and accelerate cell death under oxidative stress, such as hypoxia, or causing in vitro anchorage independence and in vivo impaired tumor growth and metastasis. | | in vivo | LY345899 (Intraperitoneal injection; 5-10 mg/kg; 5 d/wk; 4 weeks) shows potent antitumor activity and displays therapeutic activity against CRC in vivo . < td class="col1 fwb"> Animal Model: | SW620 or PDX-based BABL/c nude colorectal cancer (CRC) model | < td class="col1 fwb"> Dosage: | 5-10 mg/kg | | Administration: | Intraperitoneal injection; 5-10 mg/kg; 5 d/wk; 4 weeks | | Result : | Displayed lower cell proliferation indices and higher cell apoptosis. Exhibited no statistically significant weight loss or other signs of acute or delayed toxicity in mice. | table> | target | Ki: 18 nM (MTHFD1); IC50: 96 nM (MTHFD1) and 663 nM (MTHFD2) |
| | LY 345899) Preparation Products And Raw materials |
|
|
Tag:LY 345899)(10538-99-5)
Related Product Information
|
|
LY-2940094
LY 456236
[2-[(4-Fluorophenyl)amino]-4-methyl-5-thiazolyl]-3-thienylmethanone
3-AMINO-5-CHLORO-N-CYCLOPROPYL-6-METHOXY-4-METHYLTHIENO[2,3-B]PYRIDINE-2-CARBOXAMIDE
LY2955303
LY 334370 HYDROCHLORIDE
|
According to the laws, regulations and policies related to "patent products", the sale of this product is prohibited!
ChemicalBook prompt
The patent owner or licensee of the product has not released any relevant information for the time being.
|