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RGB-286638

CAS No. : 784210-87-3

MCE 国际站：RGB-286638

产品活性：RGB-286638 是一种有效的 CDK 抑制剂，抑制 cyclin T1-CDK9，cyclin B1-CDK1，cyclin E-CDK2，cyclin D1-CDK4，cyclin E-CDK3 和 p35-CDK5 活性，IC₅₀ 分别为 1，2，3，4，5 和 5 nM；同时可抑制 GSK-3β，TAK1，Jak2 和 MEK1，IC₅₀ 值分别为 3，5，50，和 54 nM。

研究领域：Cell Cycle/DNA Damage | Stem Cell/Wnt | PI3K/Akt/mTOR | MAPK/ERK Pathway | JAK/STAT Signaling | Epigenetics

作用靶点：CDK | GSK-3 | MEK | JAK

In Vitro: RGB-286638 is an indenopyrazole-derived CDK inhibitor (CDKI) with K_i-nanomolar activity against transcriptional CDKs. RGB-286638 inhibits several tyrosine ａnd serine/threonine non-CDK enzymes, i.e. GSK-3β, TAK1, AMPK, Jak2, MEK1. The dose- ａnd time-dependent effect of treatment with RGB-286638 (12.5-100nM) is investigated on the growth of human p53-wt (MM.1S, MM.1R, ａnd H929) ａnd p53-mutant (U266, OPM1, ａnd RPMI) MM cells by MTT assay, assessing viability at 24 ａnd 48 hours. The half-maximally effective concentrations (EC₅₀) range between 20 ａnd 70 nM at 48 hours. Dose-dependent differences in growth among p53-wt ａnd -mutant cells are observed after 50nM treatment, with p53-wt MM.1S, MM.1R ａnd H929 being slightly more sensitive to RGB-286638 treatment at 48h.

In Vivo: Dose-finding studies with RGB-286638 identify 40 mg/kg/day IV treatment as the maximum tolerated dose in SCID mice. Five days IV treatment with RGB-286638 significantly suppresses MM tumor growth, with maximum TGI (%) noted at day 14 following end of treatment at 85.06% ａnd 86.34% in the 30 mg/kg ａnd 40 mg/kg treated cohorts respectively. The log10 cell kill (LCK Td: 4.5 days) is 1.6 for both treated groups. RGB-286638 treatment is also associated with improved survival, evidenced by first death at day 24 in controls versus day 43 in both treated groups. No toxic deaths occurred during this study: maximum percentage of body weight (BW) loss is observed on day 5 (8.4%) at 30 mg/kg dosage schedule, ａnd on day 15 (9.9%) after 40 mg/kg dosing, with weight recovery in the following two weeks.

相关产品：Bioactive Compound Library Plus | Cell Cycle/DNA Damage Compound Library | Epigenetics Compound Library | Immunology/Inflammation Compound Library | JAK/STAT Compound Library | Kinase Inhibitor Library | MAPK Compound Library | PI3K/Akt/mTOR Compound Library | Stem Cell Signaling Compound Library | Wnt/Hedgehog/Notch Compound Library | Anti-Cancer Compound Library | Anti-Aging Compound Library | Differentiation Inducing Compound Library | Reprogramming Compound Library | Oxygen Sensing Compound Library | Ferroptosis Compound Library | Glycolysis Compound Library | Cytoskeleton Compound Library | Anti-Alzheimer＇s Disease Compound Library | Anti-Breast Cancer Compound Library | Anti-Pancreatic Cancer Compound Library | Anti-Blood Cancer Compound Library | Anti-Cancer Metabolism Compound Library | Neurodegenerative Disease-related Compound Library | Angiogenesis Related Compound Library | Glucose Metabolism Compound Library | CHIR-99021 | Trametinib | PD98059 | U0126-EtOH | Palbociclib | Ruxolitinib | Abemaciclib | Mirdametinib | AG490 | Tofacitinib | Baricitinib | Dinaciclib | Ribociclib | Selumetinib | Ro-3306 | Deucravacitinib | THZ1 | Cobimetinib | Binimetinib | THZ531 | Upadacitinib | AZD4573 | Seliciclib | PF-06873600 | Fedratinib | Flavopiridol | SB 216763

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