计算溶液所需的质量、体积或浓度。
为什么选择此级别
，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
2-8°C储存,干燥。低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
AMG 925 HCl is a potent, selective, and orally available FLT3 / CDK4 dual inhibitor with IC 50 s of 2±1 nM and 3±1 nM, respectively.
In Vitro
AMG 925 also inhibits CDK6, CDK2, and CDK1 in kinase assays with IC 50 s of 8±2 nM, 375±150 nM, 1.90±0.51 μM, respectively. A fair overall kinase selectivity of AMG 925 is as determined by KinomScan against a panel of 442 various kinases. Cellular selectivity (on-target vs. off-target activity) of AMG 925 is about 50-fold as evaluated by comparison of its growth-inhibiting activity in RB-positive (RB + ) and RB-negative (RB - ) non- acute myeloid leukemia (AML) cancer cell lines. AMG 925 potently inhibits growth of AML cell lines MOLM13 (FLT3-ITD; IC 50 =19 μM) and Mv4-11 (FLT3-ITD; IC 50 =18 μM). MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MOLM13 tumor-bearing mice are dosed twice daily by oral administration 6 hours apart with 12.5, 25, or 37.5 mg/kg AMG 925. Tumors are then harvested 3, 9, 12, and 24 hours after the first dose, and analyzed for levels of P-STAT5 and P-RB. Maximum inhibition of P-STAT5 and P-RB is achieved at 6 and 12 hours respectively at the 37.5 mg/kg dose of AMG 925. Interestingly, a rebound of P-STAT5 at 24 hours is observed, possibly as a result of compensational feedback. The pharmacodynamic responses of P-STAT5 and P-RB inhibition correlated with plasma concentrations of AMG 925. AMG 925 inhibits AML xenograft tumor growth by 96% to 99% without significant body weight loss. The antitumor activity of AMG 925 correlates with the inhibition of STAT5 and retinoblastoma protein (RB) phosphorylation, the pharmacodynamic markers for inhibition of FLT3 and CDK4, respectively. In addition, AMG 925 is also found to inhibit FLT3 mutants (e.g., D835Y) that are resistant to the current FLT3 inhibitors (e.g., AC220 and Sorafenib) . MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Form:Solid
IC50& Target:FLT3 2 nM (IC 50 ) CDK4 3 nM (IC 50 ) CDK6 8 nM (IC 50 ) CDK2 375 nM (IC 50 ) CDK1 1.9 μM (IC 50 )
规格
别名
AMG 925 盐酸
英文名称
AMG 925 HCl
生化机理
AMG 925 HCl 是一种强效、选择性和口服型 FLT3 / CDK4 双抑制剂，其 IC 50 s 分别为 2±1 nM 和 3±1 nM。
储存条件
2-8°C储存,干燥
运输条件
低温运输
作用类型
抑制剂
名称和识别符
分子类型
小分子
IUPAC Name
2-hydroxy-1-[2-[[8-(4-methylcyclohexyl)-4,6,8,11-tetrazatricyclo[7.4.0.02,7]trideca-1(9),2,4,6,10,12-hexaen-5-yl]amino]-7,8-dihydro-5H-1,6-naphthyridin-6-yl]ethanone;hydrochloride
INCHI
1S/C26H29N7O2.ClH/c1-16-2-5-18(6-3-16)33-22-13-27-10-8-19(22)20-12-28-26(31-25(20)33)30-23-7-4-17-14-32(24(35)15-34)11-9-21(17)29-23;/h4,7-8,10,12-13,16,18,34H,2-3,5-6,9,11,14-15H2,1H3,(H,28,29,30,31);1H
InChi Key
JJDSFFVYZSLRLY-UHFFFAOYSA-N
Smiles
CC1CCC(CC1)N2C3=C(C=CN=C3)C4=CN=C(N=C42)NC5=NC6=C(CN(CC6)C(=O)CO)C=C5.Cl
PubChem CID
分子量
508.02
技术文档
高级数据
三维结构
交互式化学结构模型
化学和物理性质
溶解性
DMSO : 1 mg/mL (1.97 mM; Need ultrasonic)
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
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