| 产品描述： | KRCA-0008 is a selective ALK/Ack1 inhibitor with IC50s of 12 and 4 nM for ALK and Ack1, respectively. KRCA-0008 can be used for the research of cancer |
| 靶点： |
IC50: 12 nM (ALK), 4 nM (Ack1);ACK; ALK |
| 体外研究： |
KRCA-0008 (0-1000 μM) shows potency to ALK (wt), ALK L1196 M, ALK C1156Y, ALK F1174L, ALK R1275Q and insulin receptor with IC50s of 12, 75, 4, 17, 17 and 210 nM, respectively. KRCA-0008 (0-1000 nM; 4 h) inhibits ALK-dependent signaling pathways more potently than crizotinib. KRCA-0008 (0-1000 nM; 72 h) induces cell apoptosis. KRCA-0008 (0-100 nM; 48 h) affects cell cycle. Cell Proliferation Assay Cell Line: H3122 and H1993 cell lines Concentration: 200 nM Incubation Time: 6 hours Result: Inhibited cell proliferation of H3122 and H1993 cells with IC50s of 0.08 and 3.6 nM, respectively. Cell Proliferation Assay Cell Line: NPM-ALK-positive ALCL cell lines (Karpas-299 and SU-DHL-1) and U937 NPM ALK-negative lymphoma cell line Concentration: 200 nM Incubation Time: 72 hours Result: Inhibited proliferation of Karpas-299, SU-DHL-1 and U937 cells with GI50s of 12 nM, 3 nM and 3.5 μM, respectively. Western Blot Analysis Cell Line: Karpas-299 and SU-DHL-1 cell lines Concentration: 0, 10, 100 and 1000 nM Incubation Time: 4 hours Result: Completely suppressed phosphorylation of ALK and its effectors at a dose of 100 nM in NPM-ALK-positive ALCL cells. Apoptosis Analysis Cell Line: SU-DHL-1 cell line Concentration: 0-1 μM Incubation Time: 72 hours Result: Dose-dependently increased cspase-3/7 activities and induced cell apoptosis. Cell Cycle Analysis Cell Line: Karpas-299 and SU-DHL-1 cell lines Concentration: 0-100 nM Incubation Time: 48 hours Result: Induced G0/G1 cell cycle arrest i |
| 体内研究： |
KRCA-0008 (25 and 50 mg/kg; p.o. twice a day for two weeks) suppresses tumor growth in an ALK-positive Karpas-299 xenograft model. Animal Model: NOD/SCID mice with Karpas-299 xenografts Dosage: 25 and 50 mg/kg Administration: Oral gavage; 25 and 50 mg/kg twice a day; for two weeks Result: Significantly inhibited tumor growth by inhibiting NPM-ALK phosphorylation without showing overt signs of toxicity or significant compound-related body weight loss. |
| 参考文献： |
1. Park CH, et al. Novel bis-ortho-alkoxy-para-piperazinesubstituted-2,4-dianilinopyrimidines (KRCA-0008) as potent and selective ALK inhibitors for anticancer treatment. Bioorg Med Chem Lett. 2013 Nov 15;23(22):6192-6. 2. Hwang J, et al. KRCA-0008 suppresses ALK-positive anaplastic large-cell lymphoma growth. Invest New Drugs. 2020 Oct;38(5):1282-1291. |
| 溶解性： |
soluble in DMSO |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
1.642 ml |
8.209 ml |
16.417 ml |
| 5 mM |
0.328 ml |
1.642 ml |
3.283 ml |
| 10 mM |
0.164 ml |
0.821 ml |
1.642 ml |
| 50 mM |
0.033 ml |
0.164 ml |
0.328 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京