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临床前CDMO研发化合物筛选
AR-42
中文名称:(S)-(+)-N-羟基-4-(3-甲基-2-苯基丁酰氨基)苯甲酰胺
CAS号:935881-37-1
分子式: C18H20N2O3 分子量: 312.36
产品形式: free base
研发状态: Terminated
研发用途: Renal Cell Carcinoma; Soft Tissue Sarcoma; Metastatic Disease
研究机构: Virginia Commonwealth University; National Cancer Institute (NCI)
研发日期: July 8 2016
研发阶段: Phase 1
AR-42 (HDAC-42) is an HDAC inhibitor with IC50 of 30 nM. Phase 1.
CXD101
CAS号:934828-12-3
分子式: C24H29N5O 分子量: 403.52
产品形式: free base
研发状态: Withdrawn
研发用途: Diffuse Large B Cell Lymphoma
研究机构: University College London; Celleron Therapeutics Ltd.; Merck Sharp & Dohme LLC
研发日期: Oct-19
研发阶段: Phase 1 : Phase 2
CXD101 (HDAC-IN-4) is a potent, selective and orally active class I histone deacetylase (HDAC) inhibitor with IC50s of 63 nM, 570 nM and 550 nM for HDAC1, HDAC2 and HDAC3, respectively.
Glimepiride
中文名称:格列美脲
CAS号:93479-97-1
分子式: C24H34N4O5S 分子量: 490.62
产品形式: free base
研发状态: Unknown status
研发用途: Fall; Congestive Heart Failure; Chronic Kidney Failure; Adverse Drug Event
研究机构: RAND; Northwestern University; University of California Los Angeles; University of Southern California; University of Pittsburgh; National Institute on Aging (NIA)
研发日期: February 11 2019
研发阶段: Not Applicable
Glimepiride(HOE-490) is a potent Kir6.2/SUR inhibitor with IC50 of 3.0 nM, 5.4 nM, and 7.3 nM for SUR1, SUR2A and SUR2B, used in the treatment of type 2 diabetes mellitus.
Cobimetinib (GDC-0973)
中文名称:考比替尼
CAS号:934660-93-2
分子式: C21H21F3IN3O2 分子量: 531.31
产品形式: free base
研发状态: Suspended
研发用途: Melanoma; Malignant Melanoma
研究机构: ImmVira Pharma Co. Ltd
研发日期: June 30 2024
研发阶段: Phase 2
Cobimetinib (GDC-0973, RG7420) is a potent and highly selective MEK1 inhibitor with IC50 of 4.2 nM, showing more than 100-fold selectively for MEK1 over MEK2 and showed no significant inhibition when tested against a panel of more than 100 of serine-threonine and tyrosine kinases. Cobimetinib induces apoptosis. Phase 3.
TAK-901
中文名称: 5-[3-(乙基磺酰基)苯基]-3,8-二甲基-N-(1-甲基-4-哌啶基)-9H-吡啶并[2,3-b]吲哚-7-羧酰胺
CAS号:934541-31-8
分子式: C28H32N4O3S 分子量: 504.64
产品形式: free base
研发状态: Completed
研发用途: Advanced Solid Tumors; Lymphoma
研究机构: Millennium Pharmaceuticals Inc.
研发日期: Oct-09
研发阶段: Phase 1
TAK-901 is a novel inhibitor of Aurora A/B with IC50 of 21 nM/15 nM. It is not a potent inhibitor of cellular JAK2, c-Src or Abl. Phase 1.
Pilaralisib (XL147)
CAS号:934526-89-3
分子式: C25H25ClN6O4S 分子量: 541.02
产品形式: free base
研发状态: Completed
研发用途: Glioblastoma; Astrocytoma Grade IV
研究机构: Sanofi
研发日期: Jan-11
研发阶段: Phase 1
Pilaralisib (XL147) is a selective and reversible class I PI3K inhibitor for PI3Kα/δ/γ with IC50 of 39 nM/36 nM/23 nM in cell-free assays, less potent to PI3Kβ. Phase 1/2.
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