MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報(bào)，我們不為任何個(gè)人用途提供產(chǎn)品和服務(wù)。

CAS No. : 2088852-47-3

MCE 國際站：Uzansertib phosphate

產(chǎn)品活性：Uzansertib (INCB053914) phosphate 是一種具有口服活性的，ATP 競爭性泛-PIM 激酶抑制劑，對于 PIM1，PIM2 和 PIM3 的 IC₅₀ 分別為 0.24 nM，30 nM 和 0.12 nM。Uzansertib phosphate 對多種血液腫瘤細(xì)胞系具有廣泛的抗增殖活性。

研究領(lǐng)域：JAK/STAT Signaling

作用靶點(diǎn)：Pim

In Vitro: Uzansertib phosphate inhibits proliferation in all multiple myeloma (MM) cell lines tested, with mean GI₅₀ values ranging from 13.2 nM to 230.0 nM in AML, MM, DLBCL, MCL, and T-ALL cell lines.
Uzansertib phosphate (0.1, 0.3, 1, 3, 10, 30, 100, 300, 1000 nM) inhibits the phosphorylation of downstream PIM kinase substrates (p70S6K/S6 and 4E-BP1) in a dose-dependent manner in MOLM-16 (AML), Pfeiffer (DLBCL), and KMS-12-PE/BM (MM) cell lines.
PIM kinase-mediated phosphorylation of BAD in MOLM-16 and KMS-12-BM cells is particularly sensitive to inhibition by Uzansertib phosphate (mean IC₅₀, 4 nM and 27 nM, respectively).

In Vivo: Uzansertib phosphate (25-100 mg/kg; PO; twice a day; for 15 days) inhibits tumor growth in a dose-dependent manner in mice bearing MOLM-16 (AML) or KMS-12-BM (MM) .
Uzansertib phosphate demonstrates a dose-dependent inhibition of BAD phosphorylation relative to vehicle at 4 hours post dose (MOLM-16 tumors, IC₅₀=70 nM; KMS-12-BM tumors, IC₅₀=145 nM) .

相關(guān)產(chǎn)品：Drug Repurposing Compound Library Plus  |  Clinical Compound Library Plus  |  Bioactive Compound Library Plus  |  Epigenetics Compound Library  |  Immunology/Inflammation Compound Library  |  JAK/STAT Compound Library  |  Kinase Inhibitor Library  |  Anti-Cancer Compound Library  |  Clinical Compound Library  |  Drug Repurposing Compound Library  |  Anti-COVID-19 Compound Library  |  Orally Active Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  Anti-Blood Cancer Compound Library  |  Targeted Diversity Library  |  PIM-447 dihydrochloride  |  AZD1208  |  Pim1/AKK1-IN-1  |  SGI-1776  |  Hispidulin  |  TCS-PIM-1-4a  |  TP-3654  |  Quercetagetin  |  CX-6258  |  TCS PIM-1 1  |  GDC-0339  |  SMI-16a  |  M-110  |  CK2/ERK8-IN-1  |  CK2/PIM1-IN-1  |  CX-6258 hydrochloride  |  MNK/PIM-IN-1  |  R8-T198wt  |  SEL24-B489  |  Uzansertib  |  GNE-955  |  PIM1-IN-1

熱門產(chǎn)品線：重組蛋白  |  化合物庫  |  天然產(chǎn)物  |  染料試劑  |  PROTAC  |  同位素標(biāo)記物

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Dye Reagents  |  PROTAC  |  Isotope-Labeled Compounds

品牌介紹:
•   MCE (MedChemExpress) 擁有數(shù)百種全球獨(dú)家化合物，我們致力于為全球科研客戶提供最新最全的高品質(zhì)小分子活性化合物；
•   10,000 多種高選擇性抑制劑、激動(dòng)劑涉及各熱門信號(hào)通路及疾病領(lǐng)域；
•   設(shè)有專業(yè)的實(shí)驗(yàn)中心和嚴(yán)格的質(zhì)控、驗(yàn)證體系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各項(xiàng)質(zhì)檢報(bào)告，確保產(chǎn)品的高純度、高品質(zhì)；
•   產(chǎn)品的生物活性多經(jīng)各國客戶實(shí)驗(yàn)驗(yàn)證；
•   Nature, Cell, Science 等多種頂級(jí)期刊及制藥專利收錄了MCE客戶的科研成果；
•   專業(yè)團(tuán)隊(duì)跟蹤最新的制藥及生命科學(xué)研究進(jìn)展，為您提供全球最新的活性化合物；
•   與世界各大制藥公司及知名科研機(jī)構(gòu)建立了長期的合作。