Asnuciclib,1421693-22-2

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。

Asnuciclib

CAS No. : 1421693-22-2

MCE 国际站：Asnuciclib

产品活性：Asnuciclib (CDKI-73; LS-007) 是具有口服活性的、高效的 CDK9 抑制剂，其对CDK9、CDK1 和 CDK2 的 K_i 值分别为 4 nM、4 nM 和 3 nM。CDKI-73 可下调 RNA 聚合酶 II 的磷酸化。Asnuciclib 也是一种 Rab11 的抑制剂。

研究领域：Cell Cycle/DNA Damage  |  Apoptosis

作用靶点：CDK  |  Apoptosis

In Vitro: Asnuciclib is highly cytotoxic to primary leukemia cells derived from CLL patients (mean LD₅₀ = 0.08 μM) and shows>500-fold selectivity for primary leukemia cells over normal B-lymphocytes (LD₅₀=40.5 μM).
Asnuciclib (0.1 μM, 4 h) inhibits the phosphorylation of serine 2 of RNA polymerase II and MCL1 protein expression in CLL cells.
Asnuciclib induced caspase-dependent apoptosis that was preceded by dephosphorylation of cdk9 and serine 2 of RNA polymerase II.
Asnuciclib is highly effective against all cell lines tested with an IC₅₀ in the range of 0.012-0.517 μM; in particular three MLL-AML cell lines, namely MOLM13, MV4-11 and THP-1, were highly sensitive to CDKI-73 with IC₅₀ values <0.062 μM.

In Vivo: Asnuciclib (25, 50, 100 mg/kg) markedly decreases tumor growth in a dose-dependent manner and results in a prolongation of animal life span (P < 0.001) without causing body weight loss and other overt toxicities..

相关产品：Bioactive Compound Library Plus  |  Apoptosis Compound Library  |  Cell Cycle/DNA Damage Compound Library  |  Immunology/Inflammation Compound Library  |  Kinase Inhibitor Library  |  Anti-Cancer Compound Library  |  Anti-Aging Compound Library  |  Anti-Breast Cancer Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  Anti-Blood Cancer Compound Library  |  Cancer Stem Cells Compound Library  |  Membrane Protein-targeted Compound Library  |  Cell Death Library  |  Serine/Threonine Kinase Inhibitor Library  |  MG-132  |  Doxorubicin hydrochloride  |  Bafilomycin A1  |  LY294002  |  Tamoxifen  |  Paclitaxel  |  Y-27632  |  Acetylcysteine  |  Angiotensin II human  |  2-Deoxy-D-glucose  |  Staurosporine  |  SB-431542  |  Actinomycin D  |  Deferoxamine mesylate  |  Bortezomib  |  5-Fluorouracil  |  Trametinib  |  Sorafenib  |  Oxaliplatin  |  Gemcitabine  |  Temozolomide  |  Palbociclib  |  Rotenone  |  Mdivi-1  |  Elesclomol  |  Ruxolitinib  |  Decitabine  |  SP600125  |  MK-2206 dihydrochloride  |  Etoposide

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

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