SphK1-IN-2 是一种有效的选择性SphK1抑制剂，SphK1 和 SphK2 的IC50值分别为 19.81 nM和 ＞10 μM。SphK1-IN-2 具有抗增殖活性，诱导细胞周期阻滞和凋亡 (apoptosis)。SphK1-IN-2 可用于癌症研究。
| 生物活性 | SphK1-IN-2 is a potent, selectiveSphK1inhibitor withIC50values of 19.81 nM and ＞10 μM forSphK1andSphK2, respectively. SphK1-IN-2 exhibits anti-proliferative activities and induces cell cycle arrest andapoptosis. SphK1-IN-2 can be used forcancerresearch[1]. |
| IC50& Target[1] | SphK1 19.81 nM (IC50) | SphK2 ＞10 μM (IC50) |
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体外研究
(In Vitro) | SphK1-IN-2 (4-24 μM; 72 hours; cancer cell lines) has anti-proliferative activity on cancer cells[1].
SphK1-IN-2 (10-30 μM; 48 hours; HT-29 cells and MDA-MB-231 cells) induces G0/G1 phase arrest and apoptosis in colon cancer cells[1].
Cell Viability Assay[1] | Cell Line: | HT-29, SW480, MDA-MB231 and MCF-7 cells | | Concentration: | 4-24 μM | | Incubation Time: | 72 hours | | Result: | Had inhibitory activity against HT-29 and MDA-MB-231 with IC50of 3.85 and 7.14 μM, respectively. |
Cell Cycle Analysis[1] | Cell Line: | HT-29 cells and MDA-MB-231 cells | | Concentration: | 10 and 30 μM | | Incubation Time: | 72 hours | | Result: | Arrestd cell cycle at G0/G1 phase and reduced the expression of cyclin A, cyclin E1, cyclin D1, and CDK6. |
Apoptosis Analysis[1] | Cell Line: | HT-29 cells and MDA-MB-231 cells | | Concentration: | 10 and 30 μM | | Incubation Time: | 48 hours | | Result: | Induced cell apoptosis in a dose-dependent manner. |
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体内研究
(In Vivo) | SphK1-IN-2 (50-100 mg/kg; i.p.; daily; for 14 days; female BALB/c nude mice) inhibits the growth of colon tumors and breast tumors in vivo[1].
SphK1-IN-2 (2-50 mg/kg; p.o., i.p. and i.v.; female BALB/c nude mice) exhibits a long half-life (T1/2=8.13 h) and high plasma exposure (AUClast= 8061 h*ng/mL)[1].
| Animal Model: | Female BALB/c nude mice[1] | | Dosage: | 2, 20 and 50 mg/kg(Pharmacokinetic Analysis) | | Administration: | Oral administration, intraperitoneal injection and intravenous injection | | Result: | 1.19| admin. | p.o. | i.p. | i.v. | | Tmax(min) | 0.83 | 0.18 | | | Cmax(ng/mL) | 171 | 78582 | | | AUClast(h*ng/mL) | 242 | 8061 | 408 | | T1/2(h) | 8.13 | 4.20 | 2.23 | | CL_obs (mL/min/kg) | | | 81.10 | | F (%) | 2.38 | 79.00 | |
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| Animal Model: | Female BALB/c nude mice[1] | | Dosage: | 50 and 100 mg/kg | | Administration: | Intraperitoneal injection; daily; for 14 days | | Result: | Inhibited the growth of HT29 tumors at a dose of 50 mg/kg and inhibited the growth of MDA-MB-231 breast tumors in a dose-dependent manner. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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