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。

Asciminib hydrochloride

CAS No. : 2119669-71-3

产品活性：Asciminib (ABL001) hydrochloride is a potent and selective allosteric BCR-ABL1 inhibitor, which inhibits Ba/F3 cells grown with an IC₅₀ of 0.25 nM.

研究领域：Protein Tyrosine Kinase/RTK

作用靶点：Bcr-Abl

In Vitro: Asciminib (ABL001) hydrochloride binds to the myristoyl pocket of ABL1 and induces the formation of an inactive kinase conformation.
Asciminib hydrochloride binds potently (dissociation constant=0.5-0.8 nM) and selectively to the myristoyl pocket of ABL1 and induces the inactive C-terminal helix conformation. Asciminib hydrochloride exhibits the same non-ATP-competitive biochemical kinetics as the BCR–ABL inhibitor GNF-2 but with approximately 100-fold greater potency.
Asciminib hydrochloride lacks activity against more than 60 kinases, including SRC, and is similarly inactive against G-protein-coupled receptors, ion channels, nuclear receptors and transporters.
In BCR–ABL1-transformed Ba/F3 cells grown without IL-3, Asciminib hydrochloride has an anti-proliferative with IC₅₀ value of 0.25 nM. In the CML blast-phase cell line KCL-22, Asciminib hydrochloride inhibits phosphorylation of both STAT5 (Tyr694; pSTAT5) and BCR–ABL1 (Tyr245; pBCR–ABL1) after 1 h using concentrations that correlate with those required for inhibition of cell proliferation.
Asciminib hydrochloride is selectively active against all BCR–ABL1 lines (IC₅₀ value of 1–20 nM), irrespective of the presence of either the p210 or the p190 BCR–ABL1 isoform.

In Vivo: Single doses of 7.5, 15 and 30 mg/kg Asciminib, administered to mice bearing KCL- 22 xenografts, inhibits pSTAT5 (Tyr694), which return to baseline at 10, 12 and 16-20 h after administration of the dose, respectively. In mice implanted with KCL-22 tumors, the minimum dose of Asciminib required for complete regression is 7.5 mg/kg twice a day (BID) or 30 mg/kg once a day (QD), and is tolerated at doses up to 250 mg/kg BID.

相关产品：Drug Repurposing Compound Library Plus  |  FDA-Approved Drug Library Plus  |  FDA-Approved Drug Library Mini  |  Bioactive Compound Library Plus  |  Kinase Inhibitor Library  |  Protein Tyrosine Kinase Compound Library  |  FDA-Approved Drug Library  |  Anti-Cancer Compound Library  |  Drug Repurposing Compound Library  |  Cytoskeleton Compound Library  |  FDA Approved & Pharmacopeial Drug Library  |  Anti-Alzheimer's Disease Compound Library  |  Anti-Blood Cancer Compound Library  |  Anti-Parkinson's Disease Compound Library  |  Neurodegenerative Disease-related Compound Library  |  Rare Diseases Drug Library  |  FDA-Approved Anticancer Drug Library  |  Heterocyclic Compound Library  |  SNIPER(ABL)-013  |  AT9283  |  Bafetinib  |  Flumatinib mesylate  |  Olverembatinib  |  GNF-2  |  BCR-ABL-IN-6  |  Ponatinib hydrochloride  |  GNF-5  |  Vamotinib  |  CT-721  |  ON 146040  |  Bosutinib hydrate  |  Ponatinib-d₈  |  Imatinib-d₈  |  GMB-475  |  BCR-ABL-IN-5  |  Dasatinib monohydrate  |  Imatinib-d₄  |  Debio 0617B  |  Nilotinib monohydrochloride monohydrate  |  SNIPER(ABL)-049  |  SNIPER(ABL)-033  |  KW-2449  |  Imatinib-d₃ (hydrochloride)  |  CHMFL-ABL-039  |  SNIPER(ABL)-050  |  BCR-ABL1-IN-1

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  |  寡核苷酸  |  抗体  |  点击化学

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Fluorescent Dye  |  PROTAC  |  Isotope-Labeled Compounds  |  Oligonucleotides  |  Antibodies  |  Click Chemistry

品牌介绍:
•   MCE (MedChemExpress) 拥有200 多种*仅有化合物库，我们致力于为*科研客户提供前沿的高品质小分子活性化合物；
•   50,000 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；
•   产品种类涵盖各种重组蛋白，多肽，常用试剂盒 ，更有 PROTAC、ADC 等特色产品，广泛应用于新药研发、生命科学等科研项目；
•   提供虚拟筛选，离子通道筛选，代谢组学分析检测分析，药物筛选等专业技术服务；
•   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 等多种顶级期刊及制药 Patent 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*新的活性化合物；
•   与世界各大制药公司及*科研机构建立了长期的合作。