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临床前CDMO研发化合物筛选
BGT226 (NVP-BGT226) maleate
中文名称: 1-(3-三氟甲基-4-(哌嗪-1-基)苯基)-8-(6-甲氧基吡啶-3-基)-3-甲基-1H-咪唑并[4,5-C]喹啉-2(3H)-酮马来酸盐
CAS号:1245537-68-1
分子式: C28H25F3N6O2.C4H4O 分子量: 650.60
产品形式: maleate
研发状态: Terminated
研发用途: Cancer; Solid Tumor; Advanced Solid Tumor
研究机构: Novartis Pharmaceuticals; Novartis
研发日期: November 17 2008
研发阶段: Phase 1
BGT226 (NVP-BGT226) maleate is a novel class I PI3K/mTOR inhibitor for PI3Kα/β/γ with IC50 of 4 nM/63 nM/38 nM. Phase 1/2.
LGK-974
中文名称:2',3-二甲基-N-[5-(2-吡嗪基)-2-吡啶基]-[2,4'-联吡啶]-5-乙酰胺
CAS号:1243244-14-5
分子式: C23H20N6O 分子量: 396.44
产品形式: free base
研发状态: Active not recruiting
研发用途: Pancreatic Cancer; BRAF Mutant Colorectal Cancer; Melanoma; Triple Negative Breast Cancer; Head and Neck Squamous Cell Cancer; Cervical Squamous Cell Cancer; Esophageal Squamous Cell Cancer; Lung Squamous Cell Cancer
研究机构: Novartis Pharmaceuticals; Novartis
研发日期: December 1 2011
研发阶段: Phase 1
LGK-974 (NVP-LGK974, WNT974) is a potent and specific PORCN inhibitor, and inhibits Wnt signaling with IC50 of 0.4 nM in TM3 cells. Phase 1.
AZD3514
中文名称:AZD3514抑制剂
CAS号:1240299-33-5
分子式: C25H32F3N7O2 分子量: 519.56
产品形式: free base
研发状态: Completed
研发用途: Prostate Cancer
研究机构: AstraZeneca
研发日期: Aug-11
研发阶段: Phase 1
AZD3514 is a potent and oral androgen receptor downregulator with Ki of 2.2 μM and has ability of reducing AR protein expression.Phase 1.
Ixazomib Citrate (MLN9708)
中文名称:枸橼酸艾沙佐米
CAS号:1239908-20-3
分子式: C20H23BCl2N2O9 分子量: 517.12
产品形式: Free Base
研发状态: Completed
研发用途: Multiple Myeloma
研究机构: Takeda
研发日期: June 1 2023
研发阶段: --
Ixazomib citrate (MLN9708, Ninlaro) is a prodrug of Ixazomib (MLN2238), which is a selective, orally bioavailable inhibitor of 20S proteasome that inhibits the chymotrypsin-like proteolytic (β5) site with IC50 of 3.4 nM and Ki of 0.93 nM, respectively. Ixazomib (MLN2238) also inhibits caspase-like (β1) and trypsin-like (β2) proteolytic sites with IC50 of 31 nM and 3500 nM, respectively.
Topotecan
中文名称:拓扑替康
CAS号:123948-87-8
分子式: C23H23N3O5 分子量: 421.45
产品形式: free base
研发状态: Terminated
研发用途: Eye Cancer Retinoblastoma
研究机构: Prof. Beck Popovic Maja; University of Lausanne Hospitals
研发日期: November 15 2021
研发阶段: Phase 2
Topotecan(NSC609699,Nogitecan,SKFS 104864A) is an antineoplastic agent used to treat ovarian cancer that works by inhibiting DNA topoisomerases.
TAK-063
CAS号:1238697-26-1
分子式: C23H17FN6O2 分子量: 428.42
产品形式: free base
研发状态: Completed
研发用途: Healthy Volunteers
研究机构: Takeda
研发日期: Oct-13
研发阶段: Phase 1
TAK-063 (Balipodect) is a novel and selective phosphodiesterase 10A(PDE10A) inhibitor with an IC50 of 0.30 nM.
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