RMC-4550 | SHP2抑制剂 | MCE - MCE-生物活性分子大师
RMC-4550 is an allosteric inhibitor of SHP2 and stabilizes the auto-inhibited conformation of wild-type SHP2 enzyme, with a mode of inhibition similar to SHP099. Consistent with an allosteric mode of inhibition, RMC-4550 inhibits the activity of full-length wild-type SHP2 enzyme activated by a di-phosphotyrosine peptide, but lacks activity ...
WWP1 inhibition increases SHP2 inhibitor efficacy in colorectal …
2024年7月16日 · Both the SHP2 inhibitor RMC4550 and the JAK2 inhibitor decreased RAS-GTP levels in myeloproliferative neoplasm cells, and their combined employment enhanced ERK inactivation and increased ...
RMC-4550(RMC-4550) - 药物靶点：SHP2_在研适应症：KRAS突 …
美银证券认为加科思的二代 shp2 抑制剂 jab-3312 有三大优势：临床前数据优于同类，特别是结合动力学显著优于 rmc-4550；更强大的抗肿瘤活性，更低的剂量（每日仅 1 - 8 毫克）；ic50 仅 1.5nm，显著低于同类产品。
RMC-4550 – 美仑生物
简介： RMC-4550是一种新型、有效、选择性的SHP2磷酸酶变构抑制剂，其IC 50 值为0.583 nM。 我司产品为非无菌包装，若用于细胞培养，请提前做预处理（如0.22μm滤膜过滤），除去热原细菌，否则会导致染菌。 溶解性是在室温下测定的，如果温度过低，可能会影响其溶解性。 科研试剂，广泛应用于分子生物学、药理学等科研方面，严禁用于人体。 为了您的安全和健康，请穿实验服并戴一次性手套操作。 部分产品我司仅能提供部分信息，我司不保证所提供信息的权 …
RMC-4550 | phosphatase 抑制剂 | 现货供应 | 美国品牌 | 免费采购 …
RMC-4550是 SHP-2 的抑制剂，IC50为1.55 nM，而对试验中468种激酶、15种磷酸酶催化区域、GPCRs、转运体和离子通道等无明显活性。 RMC-4550抑制纯化后的活化全长人源SHP2，IC50为1.55 nM。 在PC9细胞中，其IC50为39 nM。 RMC-4550在10 μM浓度下对SHP2的催化亚基、14种其他的蛋白磷酸酶、468种蛋白激酶没有可观测到的抑制活性，RMC-4550在体外各物种肝细胞中，仅具有低-中度内源清除率，高被动渗透率，流出率为1 [1]。 将细胞以30,000/孔的密度铺 …
RMC-4550, an Allosteric Inhibitor of SHP2, Displays Therapeutic ...
2019年11月13日 · Combination treatment of the allosteric SHP2 inhibitor RMC-4550 (Revolution Medicines) with ruxolitinib prevented the development of ruxolitinib persistent cells and pre-established persistent cells remained sensitive to SHP2 inhibition. RMC-4550 treatment led to significantly reduced levels of pERK consistent with the role of SHP2 in RAS ...
RMC-4550 | 99.88%(HPLC) | In Stock | phosphatase inhibitor
RMC-4550 inhibits purified, activated full length human SHP2 with an IC50 of 1.55 nM, and has cellular IC50 of 39 nM in PC9 cells with a pERK readout. RMC-4550 has no detectable inhibitory activity up to 10 µM against the catalytic domain of SHP2, a panel of 14 additional protein phosphatases, and a panel of 468 protein kinases.
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RMC-4550 (RMC4550) - Chemietek
RMC-4550 is a potent, selective and orally available small molecule allosteric inhibitor of SHP2, acting by stabilizing the SHP2 protein in an inactive conformation that is unable to transmit cell growth signals.
美国GlpBio - RMC-4550 | Cas# 2172651-73-7
RMC-4550 is an inhibitor of Src homology region 2 domain-containing phosphatase 2 (SHP-2; IC 50 = 1.55 nM). 1 It is selective for SHP-2 over a panel of 14 additional protein phosphatases and a panel of 468 protein kinases at 10 ?M. It inhibits tumor ERK phosphorylation in a KYSE-520 human esophageal cancer xenograft model in a dose-dependent ...
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Allosteric SHP2 inhibition increases apoptotic dependency on …
2023年11月21日 · Hereby, we report the pre-clinical efficacy of co-targeting SHP2, a critical node in MAPK signaling, and BCL2 in RTK-driven AML. The allosteric SHP2 inhibitor RMC-4550 suppresses proliferation of AML cell lines with FLT3 and KIT mutations, including cell lines with acquired resistance to FLT3i.