LY 345899

LY 345899

L647218-5mg

5mg

≥98%

-20°C储存

超低温冰袋运输

LY 345899 is a Folate analog and is a methylene tetrahydrofolate dehydrogenase ( MTHFD1 ; DC301 ) and MTHFD2 inbhibitor with IC 50 values of 96 nM and 663 nM, respectively and a K i of 18 nM for MTHFD1 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: SW620 or PDX-based BABL/c nude colorectal cancer (CRC) modelDosage: 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. Form:Solid IC50& Target:Ki: 18 nM (MTHFD1),IC50: 96 nM (MTHFD1) and 663 nM (MTHFD2)

LY 345899 是叶酸类似物，是亚甲基四氢叶酸脱氢酶（MTHFD1；DC301）和 MTHFD2 的抑制剂，其 IC 50 值分别为 96 nM 和 663 nM，对 MTHFD1 的 K i 为 18 nM。

10538-99-5

C20H21N7O7

471.4 g/mol

135484014

(2S)-2-[[4-(3-amino-1,9-dioxo-5,6,6a,7-tetrahydro-2H-imidazo[1,5-f]pteridin-8-yl)benzoyl]amino]pentanedioic acid

1S/C20H21N7O7/c21-19-24-15-14(17(31)25-19)27-11(7-22-15)8-26(20(27)34)10-3-1-9(2-4-10)16(30)23-12(18(32)33)5-6-13(28)29/h1-4,11-12H,5-8H2,(H,23,30)(H,28,29)(H,32,33)(H4,21,22,24,25,31)/t11?,12-/m0/s1

JSNFRYBHBVDHSG-KIYNQFGBSA-N

C1C2CN(C(=O)N2C3=C(N1)N=C(NC3=O)N)C4=CC=C(C=C4)C(=O)NC(CCC(=O)O)C(=O)O

135484014

5,6,7,8-tetrahydro-N(5),N(10)-carbonylfolic acid;LY 354899;LY-354899

DMSO : 125 mg/mL (265.16 mM; Need ultrasonic)

6

9

7

471.15 Da

471.15 Da

207.000 Ų

34

0

986

0

1

-1.6