SML2051

LY2109761

≥98% (HPLC)

• Szinonimák: 4-[5,6-Dihydro-2-(2-pyridinyl)-4H-pyrrolo[1,2-b]pyrazol-3-yl]-7-[2-(4-morpholinyl)ethoxy]-quinoline, LY-2109761
• Tapasztalati képlet (Hill-képlet): C₂₆H₂₇N₅O₂
• CAS-szám: 700874-71-1
• Molekulatömeg: 441.52
• MDL-szám: MFCD12923354
• UNSPSC kód: 12352200

Tulajdonságok

• Teszt: ≥98% (HPLC)
• Forma: powder
• szín: white to beige
• oldhatóság: DMSO: 2 mg/mL, clear
• tárolási hőmérséklet: −20°C
• SMILES string: [n]21nc(c(c2CCC1)c4c5c(ncc4)cc(cc5)OCCN6CCOCC6)c3ncccc3
• InChI: 1S/C26H27N5O2/c1-2-9-27-22(4-1)26-25(24-5-3-11-31(24)29-26)21-8-10-28-23-18-19(6-7-20(21)23)33-17-14-30-12-15-32-16-13-30/h1-2,4,6-10,18H,3,5,11-17H2
• Nemzetközi kémiai azonosító kulcs: IHLVSLOZUHKNMQ-UHFFFAOYSA-N

Leírás

Alkalmazás

LY2109761 has been used as an inhibitor of type I and II transforming growth factor-beta (TGFβ) receptors to reduce the phosphorylation of SMAD2 (mothers against decapentaplegic homolog) in HepG2 cells.

Biokémiai/fiziológiai hatások

LY2109761 is a potent and orally active TGF-β receptor (TGFβR) type I & II dual inhibitor (IC50 = 70 and 322 nM against TGFβRI/ALK5 and TGFβRII autophosphorylation, respectively, with 4 μM ATP), inhibiting Fyn/JNK3/Lck/MKK6/SAPK2α only at much higher concentrations (58-89% inhibition at 20 μM) and exhibiting little or no potency against 37 other kinases (IC50 >20 μM). LY2109761 inhibits 0.25 ng/mL TGFβ-induced NIH/3T3 proliferation in cultures (IC50 = 210 nM; 2-hr pretreatment prior to TGFβ for 24 hrs) and suppresses human MX1 breast carcinoma xenograft tumor growth in mice in vivo (by ∼80% on day 37; 75 mg/kg p.o. bid from day 7 to 20). When administered in combination with gemcitabine (25 mg/kg/day i.p.), LY2109761 (50 mg/kg p.o. bid) is shown to significantly reduce tumor burden and spontaneous abdominal metastases in a murine model of metastatic pancreatic cancer.

LY2109761 suppresses transforming growth factor (TGF)-β1-induced fibroblasts proliferation and collagen synthesis in hypertrophic scar fibroblasts. Therefore, it is used in treating hypertrophic scars.

Biztonsági adatok

• Tárolási osztály kódja: 11 - Combustible Solids
• WGK: WGK 3
• Lobbanási pont (F): Not applicable
• Lobbanási pont (C): Not applicable