1227637-23-1
1227637-23-1 結(jié)構(gòu)式
基本信息
REL-2,7-雙(((3R,5S)-3,5-二甲基哌啶-1-基)磺?；?蒽-9,10-二酮二肟
Tegavivint
BC-2059
BC2059
TEGAVIVINT
TEGATRABETAN
BC-2059
TEGAVIVINT
9,10-Anthracenedione, 2,7-bis[[(3R,5S)-3,5-dimethyl-1-piperidinyl]sulfonyl]-, 9,10-dioxime, rel-
物理化學(xué)性質(zhì)
| 報(bào)價(jià)日期 | 產(chǎn)品編號(hào) | 產(chǎn)品名稱(chēng) | CAS號(hào) | 包裝 | 價(jià)格 |
| 2024/11/08 | S0733 | 1227637-23-1 Tegatrabetan (BC-2059) | 1227637-23-1 | 5mg | 2269.4元 |
| 2024/11/08 | S0733 | Tegatrabetan (BC-2059) | 1227637-23-1 | 10mM (1mL in DMSO) | 2694.51元 |
| 2024/11/08 | S0733 | 1227637-23-1 Tegatrabetan (BC-2059) | 1227637-23-1 | 25mg | 6855.76元 |
常見(jiàn)問(wèn)題列表
| Target | Value |
|
β-catenin
() |
Tegatrabetan (BC2059; 20-100 nM; 48 hours) inhibits cell proliferation in suspension culture over 120 hours and induces apoptosis of cultured human acute myeloid leukemia (AML) HL-60, OCI-AML3 and MV4-11 cells dose-dependently.
Tegatrabetan (20 and 50 nM; 24 hours) induces a modest but significant accumulation of cells in the G0/G1 phase, with a concomitant decline in the G2/M phase of the cell cycle.
Tegatrabetan (100 nM, 24 hours) depletes the levels of β-catenin and its target genes, including c-MYC and survivin without affecting the levels of the TBL1 in OCI-AML3, HL-60 and MV4-11 cells.
Cell Proliferation Assay
| Cell Line: | HL-60, OCI-AML3 and MV4-11 cells |
| Concentration: | 20, 50, and 100 nM |
| Incubation Time: | 48 hours |
| Result: | Dose-dependently inhibited cell proliferation. |
Cell Cycle Analysis
| Cell Line: | OCI-AML3 cells |
| Concentration: | 20 and 50 nM |
| Incubation Time: | 24 hours |
| Result: | Dose-dependently induced cell cycle growth arrest. |
Western Blot Analysis
| Cell Line: | OCI-AML3, HL-60 and MV4-11 cells |
| Concentration: | 100 nM |
| Incubation Time: | 24 hours |
| Result: | Treatment depleted β-Catenin expression levels. |
Tegatrabetan (BC2059; 1.0 or 5.0 mg/kg/day; intravenously) significantly improves the median survival of the mice from approximately 17.5 to 39 days. Treatment with Tegatrabetan (10 mg/kg/day; intravenously) alone further improves the median survival to 51.5 days.
| Animal Model: | NOD/SCID mice bearing OCI-AML3 xenografts |
| Dosage: | 1 mg/kg; 5 mg/kg; 10 mg/kg |
| Administration: | Intravenously; 1 mg/kg daily 4 days per week or 5 mg/kg or 10 mg/kg of BC2059 twice per week (Tuesday and Thursday) for 3 weeks. |
| Result: | Treatment significantly improved survival of NOD/SCID mice bearing OCI-AML3 xenografts. |