MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

CDK6/PIM1-IN-1

CAS No. : 2677026-14-9

MCE 站：CDK6/PIM1-IN-1

产品活性：CDK6/PIM1-IN-1 是一种有效且平衡的双重 CDK6/PIM1 抑制剂，IC₅₀ 分别为 39 nM 和 88 nM。CDK6/PIM1-IN-1 抑制 CDK4 (IC₅₀=3.6 nM)。CDK6/PIM1-IN-1 可显著抑制急性髓系白血病 (AML) 细胞增殖，将细胞周期阻滞在 G1 期，并促进细胞凋亡。CDK6/PIM1-IN-1 具有抗AML活性。

研究领域：Cell Cycle/DNA Damage  |  JAK/STAT Signaling  |  Apoptosis

作用靶点：CDK  |  Pim  |  Apoptosis

In Vitro: CDK6/PIM1-IN-1 (compound 51)exhibits more than 10 times selectivity over CDK1 (IC₅₀>10 μM), CDK2 (IC₅₀=2.274 μM), CDK3 (IC₅₀>10 μM), CDK5 (IC₅₀>10 μM), CDK7 (IC₅₀=393 nM), CDK9 (IC₅₀=440 nM), CDK12 (IC₅₀>10 μM), ａnd CDK13 (IC₅₀>10 μM). CDK6/PIM1-IN-1shows inhibitory activity against PIM2 (IC₅₀>10 μM) ａnd PIM3 (IC₅₀=92 nM).
CDK6/PIM1-IN-1 inhibits proliferation in AML cells (K562 cell,GI₅₀=1.026 μM; HL-60 cell,GI₅₀=1.069 μM; MOLM13 cell, GI₅₀=1.362 μM).
CDK6/PIM1-IN-1 (0.5, 1, 1.5 μM) causes a G1 arrest in a dose-dependent manner in K562 ａnd HL-60 cell lines.
CDK6/PIM1-IN-1(1, 2, 4 μM) promotes the apoptosis of K562 ａnd HL-60 cell lines in a dose-dependent manner.
CDK6/PIM1-IN-1 (0.5, 1, 1.5 μM; for 24 h) reducesp-retinoblastoma (RB) andp-BAD levels in a concentration-dependent manner. CDK6/PIM1-IN-1 decreases the PIM1 level.

In Vivo: CDK6/PIM1-IN-1 (compound 51; orally; 60, 90 mg/kg/day; 17 days) displays more potent antitumor activityin BALB/c mice with K562 cell lines.
CDK6/PIM1-IN-1 (iv; 5 mg/kg) has the t_1/2, MRT_0-∞, ａnd AUC_0-∞values of 9.78 h, 14.61 h, ａnd 1153.74 hng/mL, respectively in SpragueDawley (SD) rats.
CDK6/PIM1-IN-1 (po; 5 mg/kg) has thet_1/2, T_max, C_max, ａnd AUC_0-∞ of 15.81 h, 11 h, 152.31 ng/mL, ａnd 5152.92 hng/mL, respectively in SD rats.

相关产品：MG-132  |  LY294002  |  Doxorubicin hydrochloride  |  Bafilomycin A1  |  Y-27632 dihydrochloride  |  Paclitaxel  |  Acetylcysteine  |  Angiotensin II human  |  Tamoxifen  |  Staurosporine  |  5-Fluorouracil  |  2-Deoxy-D-glucose  |  Bortezomib  |  Sorafenib  |  SP600125  |  Trametinib  |  Gemcitabine  |  Temozolomide  |  Verteporfin  |  MK-2206 dihydrochloride  |  Decitabine  |  Palbociclib  |  Etoposide  |  CCCP  |  Rote  |  DAPT  |  Ruxolitinib  |  BAY 11-7082  |  Actinomycin D

热门产品线：重组蛋白  |  化合物库  |  天然产物  |  染料试剂  |  PROTAC  |  同位素标记物

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

品牌介绍:
•   MCE (MedChemExpress) 拥有数百种全球独家化合物，我们致力于为全球科研客户提供*新*全的高品质小分子活性化合物；
•   10,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域；
•   设有专业的实验中心和严格的质控、验证体系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；
•   产品的生物活性多经各国客户实验验证；
•   Nature, Cell, Science 等多种期刊及制药收录了MCE客户的科研成果；
•   专业团队跟踪*新的制药及生命科学研究进展，为您提供全球*新的活性化合物；
•   与世界各大制药公司及知名科研机构建立了长期的合作。