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临床前CDMO研发化合物筛选
AZD9496
中文名称:(E)-3-[3,5-二氟-4-[(1R,3R)-2-(2-氟-2-甲基丙基)-3-甲基-2,3,4,9-四氢-1H-吡啶并[3,4-B]吲哚-1-基]苯基]丙烯酸
CAS号:1639042-08-2
分子式: C25H25F3N2O2 分子量: 442.47
产品形式: free base
研发状态: Completed
研发用途: Postmenopausal Women With ER+ HER2- Primary Breast Cancer
研究机构: AstraZeneca
研发日期: October 5 2017
研发阶段: Phase 1
AZD9496 is an oral estrogen receptor inhibitor that blocks the growth of ER-positive and ESR1 mutant breast tumours in preclinical models.
ONC206
CAS号:1638178-87-6
分子式: C23H22F2N4O 分子量: 408.44
产品形式: free base
研发状态: Recruiting
研发用途: Central Nervous System Neoplasms; Glioblastoma; Gliosarcoma Adult; Anaplastic Oligodendroglioma; Anaplastic Astrocytoma; Pilocytic Astrocytoma; Oligodendroglioma; Gliomatosis Cerebri; Pleomorphic Xanthoastrocytoma; Anaplastic Pleomorphic Xanthoastrocytoma; Diffuse Midline Glioma H3 K27M-Mutant; Ependymoma; Ependymoma Anaplastic; Medulloblastoma; Teratoid Rhabdoid Tumor; Neuroectodermal Tumors Primitive; Neuroectodermal Tumors; Anaplastic Meningioma; Atypical Meningioma; Choroid Plexus Neoplasms; Pineal Tumor; Diffuse Astrocytoma; Glial Tumor
研究机构: Chimerix; National Institutes of Health (NIH)
研发日期: October 26 2020
研发阶段: Phase 1
ONC206 is a selective antagonist of DRD2/3/4 with broad-spectrum anti-tumor activity.
Alobresib (GS-5829)
CAS号:1637771-14-2
分子式: C26H23N5O2 分子量: 437.49
产品形式: Free Base
研发状态: Terminated
研发用途: Advanced Estrogen Receptor Positive HER2- Breast Cancer
研究机构: Gilead Sciences
研发日期: January 10 2017
研发阶段: Phase 1 : Phase 2
Alobresib (GS-5829) is a novel BET inhibitor that represents a highly effective therapeutics agent against recurrent/chemotherapy-resistant USC-overexpressing c-Myc. Alobresib (GS-5829) inhibits CLL cell proliferation and induces leukemia cell apoptosis through deregulation of key signaling pathways, such as BLK, AKT, ERK1/2, and MYC. Alobresib (GS-5829) also inhibits NF-κB signaling.
KA2507
CAS号:1636894-46-6
分子式: C16H14N6O2 分子量: 322.32
产品形式: free base
研发状态: Withdrawn
研发用途: Biliary Tract Cancer
研究机构: Karus Therapeutics Limited; University College London
研发日期: March 5 2020
研发阶段: Phase 2
KA2507, a potent, orally active and selective HDAC6 inhibitor with IC50 of 2.5 nM, shows antitumor activities and immune modulatory effects in preclinical models.
Teriflunomide
中文名称: 特立氟胺
CAS号:163451-81-8
分子式: C12H9F3N2O2 分子量: 270.21
产品形式: free base
研发状态: Recruiting
研发用途: HAM/TSP
研究机构: National Institute of Neurological Disorders and Stroke (NINDS); National Institutes of Health Clinical Center (CC)
研发日期: September 24 2021
研发阶段: Phase 1 : Phase 2
Teriflunomide (A77 1726, HMR-1726) is the active metabolite of leflunomide, inhibiting pyrimidine de novo synthesis by blocking the enzyme dihydroorotate dehydrogenase, used as an immunomodulatory agent.
tetrathiomolybdate
CAS号:16330-92-0
分子式: MoS4 分子量: 224.20
产品形式: free base
研发状态: Not yet recruiting
研发用途: Nephropathy; Diabetic Nephropathies; Diabetes Mellitus Type 1; Albuminuria; Diabetic Complications Renal; Diabetic Complications Cardiovascular; Hypoxia
研究机构: Steno Diabetes Center Copenhagen; Juvenile Diabetes Research Foundation; King''s College London; Glostrup University Hospital Copenhagen
研发日期: Aug-24
研发阶段: Phase 4
Tetrathiomolybdate (TM) is used in the clinic for the treatment of Wilson’s disease by inducing dimerization of the metal-binding domain of the cellular copper efflux protein ATP7B (WLN4) through a unique sulfur-bridged Mo2S6O2 cluster.
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