Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Asciminib (ABL001) 是一种有效的、选择性的变构BCR-ABL1抑制剂,能够抑制 Ba/F3 细胞生长 (IC50:0.25 nM)。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 383 | 现货 | ||
2 mg | ¥ 552 | 现货 | ||
5 mg | ¥ 911 | 现货 | ||
10 mg | ¥ 1,390 | 现货 | ||
25 mg | ¥ 2,370 | 现货 | ||
50 mg | ¥ 3,530 | 现货 | ||
100 mg | ¥ 4,970 | 现货 | ||
500 mg | ¥ 10,700 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 983 | 现货 |
产品描述 | Asciminib (ABL001) (ABL001) is a potent and selective Bcr-Abl inhibitor (Kd: 0.5–0.8nM). |
靶点活性 | Abl-1:0.45 nM |
体外活性 | In BCR–ABL1-transformed Ba/F3 cells grown without IL-3, ABL001 had an anti-proliferative IC50 value of 0.25nM. By contrast, the addition of IL-3 to bypass BCR–ABL1 dependence renders these cells insensitive to ABL001. In the CML blast-phase cell line KCL-22, ABL001 inhibited phosphorylation of both STAT5 (Tyr694; pSTAT5) and BCR–ABL1 (Tyr245; pBCR–ABL1) after 1h using concentrations that correlate with those required for inhibition of cell proliferation [1]. K562-Dox and K562-ABCG2 cells demonstrated increased LD50 (asciminib) vs K562 control cells: 256 and 299 nM respectively vs 24 nM. Sensitivity was completely restored with specific inhibitors cyclosporine (ABCB1) and Ko143 (ABCG2): K562-Dox LD50 (asciminib+cyclosporine) = 13 nM, K562-ABCG2 LD50 (asciminib+Ko143) = 15 nM [2]. |
体内活性 | Single doses of 7.5, 15 and 30mg kg?1 ABL001, administered to mice bearing KCL22 xenografts, inhibited pSTAT5 (Tyr694), which returned to baseline at 10, 12 and 16–20h after administration of the dose, respectively. In mice implanted with KCL-22 tumours, the minimum dose of ABL001 required for complete regression was 7.5mg/kg twice a day (BID) or 30mg/kg once a day (QD), and was tolerated at doses up to 250mg kg?1 BID. Similarly, in xenografts derived from patients with Ph+ ALL, treatment with 7.5 and 30mg/kg ABL001 led to regressions that were maintained during dosing [1]. |
细胞实验 | Cells were resuspended in fresh culture media before culture in 24-well plates in the presence of TKI or asciminib at a density of 2 × 105 cells/mL. Plates were seeded with 1 mL of cell suspension and incubated for 72 h before cell viability determination with 7-aminoactinomycin (7-AAD) and Phycoerythrin (PE)-conjugated Annexin V. Flow cytometric analysis was conducted with a BD LSRFortessa X-20 and FACSDiva software. The lethal dose of asciminib (LD50 asciminib), imatinib (LD50 IM), nilotinib (LD50 NIL) and dasatinib (LD50 DAS) required to cause 50% death of cells was calculated [2]. |
动物实验 | Asciminib efficacy in three patient-derived ALL systemic xenograft models (ALL-7015, AL-7119 and AL-7155) is assessed by FACS monitoring of the percentage of CD45+ cells per live cell in blood samples taken at varying time points after dosing with either 7.5 mg/kg BID (group 2) or 30 mg/kg BID (group 3) asciminib for 3 weeks [1]. |
别名 | ABL001 |
分子量 | 449.84 |
分子式 | C20H18ClF2N5O3 |
CAS No. | 1492952-76-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: Insoluble
DMSO: 50 mg/mL
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Asciminib 1492952-76-7 Angiogenesis Cytoskeletal Signaling Tyrosine Kinase/Adaptors Bcr-Abl ABL-001 inhibit ABL 001 ABL001 Inhibitor inhibitor