PDEδ-IN-99

PDEδ-IN-99

中文名称PDEδ-IN-99
中文同义词K-RAS-PDEΔ-IN-1;N-(4-氟苯乙基)-4-(4-甲基-7-氧代-2-(对甲苯基)-2H-吡唑并[3,4-D]哒嗪-6(7H)-基)丁酰胺;化合物K-RAS-PDEΔ-IN-1
英文名称PDEδ-IN-99
英文同义词PDEδ-IN-99;N-(4-fluorophenethyl)-4-(4-methyl-7-oxo-2-(p-tolyl)-2,7-dihydro-6H-pyrazolo[3,4-d]pyridazin-6-yl)butanamide;K-Ras-PDEδ-IN-1;6H-Pyrazolo[3,4-d]pyridazine-6-butanamide, N-[2-(4-fluorophenyl)ethyl]-2,7-dihydro-4-methyl-2-(4-methylphenyl)-7-oxo-;N-(4-Fluorophenethyl)-4-(4-methyl-7-oxo-2-(p-tolyl)-2H-pyrazolo[3,4-d]pyridazin-6(7H)-yl)butanamide;KRasPDEδIN1,PDEδ,cancer,pyrazolopyridazinone-based,inhibit,K Ras PDEδ IN 1,Inhibitor,Phosphodiesterase (PDE);PDEδ-IN-99
CAS号1841464-21-8
分子式C25H26FN5O2
分子量447.5
EINECS号
相关类别
Mol文件1841464-21-8.mol
结构式PDEδ-IN-99 结构式

PDEδ-IN-99 性质

密度1.27±0.1 g/cm3(Predicted)
储存条件Sealed in dry,Room Temperature
形态固体
酸度系数(pKa)15.85±0.46(Predicted)
颜色白色至米白色

PDEδ-IN-99 用途与合成方法

K-Ras-PDEδ-IN-1 是一种新颖的、有效的 K-Ras-PDEδ 抑制剂。K-Ras-PDEδ-IN-1 以低纳摩尔 Kd 8 nM 与 PDEδ 的法尼基结合袋竞争性结合。

PDE4

8.3 nM (Kd)

K-Ras-PDEδ-IN-1 exhibits an IC 50 value of 12.3 μM in PaTu8902/Panc1 CTG assay.

K-Ras-PDEδ-IN-1 (oral or intraperitoneal injection; 10 mg/kg; single dose) is in different vehicles (A=5% Tween-80, 50% NaCl, 45% H2O; B=20% DMSO, 80% PEG200; C=15% DMSO, 9.5% Cremophor EL/EtOH (1:1), 75.5 % H2O) for oral and intraperitoneal (IP) administration.whereas only very low compound levels are found in plasma after oral dosage, but significantly higher plasma concentrations are found after IP administration in vehicle A, B or C at 10 mg kg.K-Ras-PDEδ-IN-1 (intravenous injection; 3 mg kg; single dose; 24 hours) shows a significant increase of the plasma exposure as well as the terminal half-life (t 1/2 =0.4 hours)when compares to compound 93,exhibits a t 1/2 , CO, AUC 0-tz , AUC 0.inf-obs , Cl obs , and Vss 0-inf-obs values of 4.1 hours, 2790.9 ng/ml, 1646.4 h.ng/ml, 1662.5 h.ng/ml, 1.8 L/h/kg, 5.9 l/kg.

安全信息

MSDS信息

更新日期产品编号产品名称CAS号包装价格
2024/04/30HY-115555K-Ras-PDEδ-IN-11 mg1090元
2024/04/30HY-115555PDEδ-IN-99
K-Ras-PDEδ-IN-1
1841464-21-85mg2400元

PDEδ-IN-99 上下游产品信息

"PDEδ-IN-99"相关产品信息
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