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临床前CDMO研发化合物筛选
Bafetinib (INNO-406)
中文名称:巴氟替尼
CAS号:859212-16-1
分子式: C30H31F3N8O 分子量: 576.62
产品形式: free base
研发状态: Completed
研发用途: Chronic Myeloid Leukemia; Acute Lymphocytic Leukemia
研究机构: CytRx
研发日期: Jul-06
研发阶段: Phase 1
Bafetinib (INNO-406, NS-187) is a potent and selective dual Bcr-Abl/Lyn inhibitor with IC50 of 5.8 nM/19 nM in cell-free assays, does not inhibit the phosphorylation of the T315I mutant and is less potent to PDGFR and c-Kit.
Lenvatinib (E7080) Mesylate
中文名称: 乐伐替尼甲磺酸盐
CAS号:857890-39-2
分子式: C21H19ClN4O4.CH4O3S 分子量: 522.96
产品形式: Mesylate
研发状态: Not yet recruiting
研发用途: Neoplasms
研究机构: National Cancer Institute (NCI); National Institutes of Health Clinical Center (CC)
研发日期: May 15 2024
研发阶段: Phase 1
Lenvatinib Mesylate (E7080) is a synthetic, orally available tyrosine kinase inhibitor that inhibits vascular endothelial growth factor receptor (VEGFR1-3), fibroblast growth factor receptor (FGFR1-4), platelet-derived growth factor receptor α (PDGFRα), stem cell factor receptor (Kit (c-Kit)), and rearranged during transfection (RET (c-RET)). Lenvatinib Mesylate has potential antineoplastic activity.
Motesanib Diphosphate (AMG-706)
中文名称:二磷酸莫替沙尼
CAS号:857876-30-3
分子式: C22H23N5O.2H3PO4 分子量: 569.44
产品形式: Diphosphate
研发状态: Completed
研发用途: Advanced Solid Tumors
研究机构: Amgen
研发日期: May-09
研发阶段: Phase 1
Motesanib Diphosphate (AMG-706) is a potent ATP-competitive inhibitor of VEGFR1/2/3 with IC50 of 2 nM/3 nM/6 nM, respectively; similar activity against Kit (c-Kit), ~10-fold more selective for VEGFR than PDGFR and Ret. Phase 3.
WP1066
中文名称:(2E)-3-(6-溴-2-吡啶基)-2-氰基-N-[(1S)-1-苯基乙基]-2-丙烯酰胺
CAS号:857064-38-1
分子式: C17H14BrN3O 分子量: 356.22
产品形式: free base
研发状态: Completed
研发用途: Brain Tumor; Medulloblastoma; Brain Metastases
研究机构: Emory University; CURE Childhood Cancer Inc.; Peach Bowl LegACy Fund
研发日期: May 4 2020
研发阶段: Phase 1
WP1066 is a novel inhibitor of JAK2 and STAT3 with IC50 of 2.30 μM and 2.43 μM in HEL cells; shows activity to JAK2, STAT3, STAT5, and ERK1/2 not JAK1 and JAK3. WP1066 induces apoptosis. Phase 1.
Cediranib Maleate
中文名称:西地尼布马来酸盐
CAS号:857036-77-2
分子式: C25H27FN4O3.C4H4O4 分子量: 566.58
产品形式: maleate
研发状态: Completed
研发用途: Adult Grade III Lymphomatoid Granulomatosis; Adult Nasal Type Extranodal NK/T-cell Lymphoma; Anaplastic Large Cell Lymphoma; Angioimmunoblastic T-cell Lymphoma; Childhood Burkitt Lymphoma; Childhood Diffuse Large Cell Lymphoma; Childhood Grade III Lymphomatoid Granulomatosis; Childhood Immunoblastic Large Cell Lymphoma; Childhood Nasal Type Extranodal NK/T-cell Lymphoma; Cutaneous B-cell Non-Hodgkin Lymphoma; Extranodal Marginal Zone B-cell Lymphoma of Mucosa-associated Lymphoid Tissue; Hepatosplenic T-cell Lymphoma; Intraocular Lymphoma; Nodal Marginal Zone B-cell Lymphoma; Noncutaneous Extranodal Lymphoma; Peripheral T-cell Lymphoma; Progressive Hairy Cell Leukemia Initial Treatment; Recurrent Adult Burkitt Lymphoma; Recurrent Adult Diffuse Large Cell Lymphoma; Recurrent Adult Diffuse Mixed Cell Lymphoma; Recurrent Adult Diffuse Small Cleaved Cell Lymphoma; Recurrent Adult Hodgkin Lymphoma; Recurrent Adult Immunoblastic Large Cell Lymphoma; Recurrent Adult Lymphoblastic Lymphoma; Recurrent Adult T-cell Leukemia/Lymphoma; Recurrent Childhood Anaplastic Large Cell Lymphoma; Recurrent Childhood Large Cell Lymphoma; Recurrent Childhood Lymphoblastic Lymphoma; Recurrent Childhood Small Noncleaved Cell Lymphoma; Recurrent Grade 1 Follicular Lymphoma; Recurrent Grade 2 Follicular Lymphoma; Recurrent Grade 3 Follicular Lymphoma; Recurrent Mantle Cell Lymphoma; Recurrent Mycosis Fungoides/Sezary Syndrome; Recurrent/Refractory Childhood Hodgkin Lymphoma; Refractory Hairy Cell Leukemia; Small Intestine Lymphoma; Splenic Marginal Zone Lymphoma; Stage IV Adult Burkitt Lymphoma; Stage IV Adult Diffuse Large Cell Lymphoma; Stage IV Adult Diffuse Mixed Cell Lymphoma; Stage IV Adult Diffuse Small Cleaved Cell Lymphoma; Stage IV Adult Hodgkin Lymphoma; Stage IV Adult Immunoblastic Large Cell Lymphoma; Stage IV Adult Lymphoblastic Lymphoma; Stage IV Adult T-cell Leukemia/Lymphoma; Stage IV Childhood Anaplastic Large Cell Lymphoma; Stage IV Childhood Hodgkin Lymphoma; Stage IV Childhood Large Cell Lymphoma; Stage IV Childhood Lymphoblastic Lymphoma; Stage IV Childhood Small Noncleaved Cell Lymphoma; Stage IV Grade 1 Follicular Lymphoma; Stage IV Grade 2 Follicular Lymphoma; Stage IV Grade 3 Follicular Lymphoma; Stage IV Mantle Cell Lymphoma; Stage IVA Mycosis Fungoides/Sezary Syndrome; Stage IVB Mycosis Fungoides/Sezary Syndrome; T-cell Large Granular Lymphocyte Leukemia; Testicular Lymphoma; Unspecified Adult Solid Tumor Protocol Specific; Unspecified Childhood Solid Tumor Protocol Specific; Waldenström Macroglobulinemia
研究机构: National Cancer Institute (NCI)
研发日期: May-07
研发阶段: Phase 1
Cediranib Maleate (AZD-2171) is the maleate salt of Cediranib, which is a potent inhibitor of VEGFR with IC50 of <1 nM and also inhibits Flt1/4 with IC50 of 5 nM/≤3 nM.
Tedizolid (TR-700)
中文名称:特地唑胺
CAS号:856866-72-3
分子式: C17H15FN6O3 分子量: 370.34
产品形式: Oxazolidinone
研发状态: Unknown status
研发用途: Prostheses Infection
研究机构: Fundacion Clinic per a la Recerca Biomédica
研发日期: March 1 2020
研发阶段: Phase 4
Tedizolid(TR-700) is an oxazolidinone-class antibiotic prodrug used for the treatment of acute bacterial skin and skin structure infections caused by susceptible isolates of several Gram-positive bacteria.
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