KRCA-0008 是选择性的ALK/Ack1抑制剂，对 ALK 和 Ack1 的IC50值分别为 12 和 4 nM。KRCA-0008 可用于癌症的研究。
| 生物活性 | KRCA-0008 is a selectiveALK/Ack1inhibitor withIC50s of 12 and 4 nM for ALK andAck1, respectively. KRCA-0008 can be used for the research ofcancer[1][2]. |
| IC50& Target | IC50: 12 nM (ALK), 4 nM (Ack1)[1] |
体外研究
(In Vitro) | 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[1].KRCA-0008 (0-1000 nM; 4 h) inhibits ALK-dependent signaling pathways more potently than crizotinib[2].KRCA-0008 (0-1000 nM; 72 h) induces cell apoptosis[2].KRCA-0008 (0-100 nM; 48 h) affects cell cycle[2].
Cell Proliferation Assay[1] | 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[2] | 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[2] | 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[2] | 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[2] | 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 in ALCL cells expressing NPM-ALK. |
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体内研究
(In Vivo) | 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[2].
| Animal Model: | NOD/SCID mice with Karpas-299 xenografts[2] | | 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 230 mg/mL(377.59 mM;Need ultrasonic) 配制储备液 | 1 mM | 1.6417 mL | 8.2086 mL | 16.4171 mL | | 5 mM | 0.3283 mL | 1.6417 mL | 3.2834 mL | | 10 mM | 0.1642 mL | 0.8209 mL | 1.6417 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 5.75 mg/mL (9.44 mM); Clear solution
此方案可获得 ≥ 5.75 mg/mL (9.44 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 57.5 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 2. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 5.75 mg/mL (9.44 mM); Clear solution
此方案可获得 ≥ 5.75 mg/mL (9.44 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 57.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 1.25 mg/mL (2.05 mM); Clear solution
此方案可获得 ≥ 1.25 mg/mL (2.05 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 *以上所有助溶剂都可在本网站选购。
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