1449240-68-9
K145 (hydrochloride)
CAS: 1449240-68-9
Molecular Formula: C18H25ClN2O3S
1449240-68-9 - Names and Identifiers
1449240-68-9 - Physico-chemical Properties
| Molecular Formula | C18H25ClN2O3S |
| Molar Mass | 384.9207 |
| Solubility | 10 mM in DMSO |
| Appearance | powder |
| Color | white to beige |
| Storage Condition | 2-8°C |
| In vitro study | K145 (0-10 µM; 24-72 hours; U937 cells) treatment significantly inhibits the growth of U937 cells in a concentration-dependent manner. K145 (10 µM; 24 hours; U937 cells) treatment significantly induces apoptosis in U937 cells. K145 (4-8 µM; 3 hours; U937 cells) treatment decreases the phosphorylation of ERK and Akt. Treatment with K145 (10 µM) causes a decrease of total cellular S1P without significant effects on ceramide levels. Cell Viability Assay Cell Line: U937 cells Concentration: 0 µM, 4 µM, 6 µM, 8 µM, 10 µM Incubation Time: 24 hours, 48 hours, 72 hours Result: Significantly inhibited the growth of U937 cells in a concentration-dependent manner. Apoptosis Analysis Cell Line: U937 cells Concentration: 10 µM Incubation Time: 24 hours Result: Significantly induced apoptosis in U937 cells. Western Blot Analysis Cell Line: U937 cells Concentration: 4 µM, 8 µM Incubation Time: 3 hours Result: Phosphorylated ERK and Akt were decreased. |
| In vivo study | K145 (50 mg/kg; oral gavage; daily; for 15 days; BALB/c-nu mice) treatment significantly inhibits the growth of U937 tumors in nude mice. Animal Model: BALB/c-nu mice injected with U937 cells Dosage: 50 mg/kg Administration: Oral gavage; daily; for 15 days Result: Inhibited the growth of U937 tumors at 50 mg/kg dose and no apparent toxicity was observed. |
1449240-68-9 - Risk and Safety
| WGK Germany | 3 |
1449240-68-9 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.598 ml | 12.99 ml | 25.979 ml |
| 5 mM | 0.52 ml | 2.598 ml | 5.196 ml |
| 10 mM | 0.26 ml | 1.299 ml | 2.598 ml |
| 5 mM | 0.052 ml | 0.26 ml | 0.52 ml |
Last Update：2024-01-02 23:10:35
1449240-68-9 - Reference Information
| Biological activity | K145 hydrochloride is a selective, substrate competitive and oral activity SphK2 inhibitor, IC50 is 4.3 µM,Ki is 6.4 µM. K145 hydrochloride has no activity against SphK1 and other protein kinases. K145 hydrochloride can induce apoptosis and has strong anti-tumor activity. |
| target | IC50: 4.3 µM (SphK2) Ki: 6.4 µM (SphK2) |
| in vitro study | K145 (0-10 µM; 24-72 hours; U937 cells) treatment significantly inhibits the growth of U937 cells in a concentration-dependent manner. K145 (10 µM; 24 hours; U937 cells) treatment significantly induces apoptosis in U937 cells. K145 (4-8 µM; 3 hours; u937 cells) treatment decreases the phosphorylation of ERK and Akt. Treatment with K145 (10 m) causesa decrease of total cellular S1P without significant effects on ceramide levels. Cell Viability Assay Cell Line: U937 cells Concentration: 0 m, 4 m, 6 m, 8 m, 10 m Incubation time: 24 hours, 48 hours, 72 hours result: significantly inhibited the growth of U937 cells in a concentration-dependent manner. Apoptosis Analysis Cell Line: U937 cells Concentration: 10 µM Incubation Time: 24 hours Result: Significantly induced apoptosis in U937 cells. Western Blot Analysis Cell Line: U937 cells Concentration: 4 µM, 8 µM Incubation Time: 3 hours Result: Phosphorylated ERK and Akt were decreased. |
| Cell Line: | U937 cells U937 cells U937 cells |
| Concentration: | 0 µM, 4 µM, 6 µM, 8 µM, 10 µM 10 µM 4 µM, 8 µM |
| Incubation Time: | 24 hours, 48 hours, 72 hours 24 hours 3 hours |
| Result: | Significantly inhibited the growth of U937 cells in a concentration-dependent manner. Significantly induced apoptosis in U937 cells. Phosphorylated ERK and Akt were decreased. Inhibited the growth of U937 tumors at 50 mg/kg dose and no apparent toxicity was observed. |
| in vivo study | K145 (50 mg/kg; oral gavage; daily; for 15 days; BALB/c-nu mice) treatment significantly inhibits the growth of U937 tumors in nude mice. Animal Model: BALB/c-nu mice injected with U937 cells Dosage: 50 mg/kg Administration: Oral gavage; daily; for 15 days result: inhibited the growth of U937 tumors at 50 mg/kg dose and no apparent toxicity was observed. |
| Animal Model: | BALB/c-nu mice injected with U937 cells |
| Dosage: | 50 mg/kg |
| Administration: | Oral gavage; daily; for 15 days |
Last Update：2024-04-10 22:29:15
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