KDM5A-IN-1

小分子

KDM5A-IN-1

K649083-5mg

5mg

≥99%

-20°C储存

超低温冰袋运输

KDM5A-IN-1 is a potent, orally bioavailable pan- histone lysine demethylases 5 (KDM5) inhibitor with IC 50 s of 45 nM, 56 nM and 55 nM for KDM5A , KDM5B and KDM5C , respectively, and with an EC 50 value of 960 nM for PC9 H3K4Me3. KDM5A-IN-1 is significantly less potent against other KDM5B enzymes (1A, 2B, 3B, 4C, 6A, 7B) In Vivo KDM5A-IN-1 (Compound 50, 5 mg/kg; oral administration; female CD-1 mice) treatment shows moderate clearance (28 mL/min/kg) in mice with good oral bioavailability (F% 34) and remarkably low plasma protein binding in mice (40%), with t 1/2 of 0.4 hours . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female CD-1 mice Dosage: 5 mg/kg Administration: Oral administration (Pharmacokinetic study) Result: Moderate clearance (28 mL/min/kg) in mice with good oral bioavailability (F% 34), and showed remarkably low plasma protein binding in mice (40%). Form:Solid IC50& Target:IC50: 45 nM ( KDM5A ), 56 nM ( KDM5B ) and 55 nM ( KDM5C )

KDM5A-IN-1 是一种口服生物活性泛组蛋白赖氨酸去甲基化酶 5 (KDM5) 抑制剂，对 KDM5A、KDM5B 和 KDM5C 的 IC 50 s 分别为 45 nM、56 nM 和 55 nM，对 PC9 H3K4Me3 的 EC 50 值为 960 nM。KDM5A-IN-1 对 PC9 H3K4Me3

1905481-36-8

C15H22N4O2

290.36 g/mol

119081409

CC(C)C1=CC(=NN1)C(=O)N2CC[C@H](C2)NC(=O)C3CC3

N-[(3R)-1-(5-propan-2-yl-1H-pyrazole-3-carbonyl)pyrrolidin-3-yl]cyclopropanecarboxamide

1S/C15H22N4O2/c1-9(2)12-7-13(18-17-12)15(21)19-6-5-11(8-19)16-14(20)10-3-4-10/h7,9-11H,3-6,8H2,1-2H3,(H,16,20)(H,17,18)/t11-/m1/s1

CXEXTVGTDZRKJS-LLVKDONJSA-N

CC(C)C1=CC(=NN1)C(=O)N2CCC(C2)NC(=O)C3CC3

119081409

DMSO : ≥ 50 mg/mL (172.20 mM)

2

3

4

290.174 Da

290.174 Da

78.100 Ų

21

0

422

0

1

1.1