1227637-23-1

中文名稱 1227637-23-1

英文名稱 BC2059

CAS 1227637-23-1

分子式 C28H36N4O6S2

分子量 588.74

MOL 文件 1227637-23-1.mol

更新日期 2025/05/13 19:27:08

1227637-23-1 結構式

基本信息物理化學性質安全數(shù)據(jù) 圖譜信息 1227637-23-1價格(試劑級) 常見問題列表

基本信息

中文別名

化合物BC2059
REL-2,7-雙(((3R,5S)-3,5-二甲基哌啶-1-基)磺?；?蒽-9,10-二酮二肟

英文別名

BC2059
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-

物理化學性質

熔點287 °C(Solvent: Dichloromethane; Hexane)

沸點757.6±70.0 °C(Predicted)

密度1.46±0.1 g/cm3(Predicted)

儲存條件Inert atmosphere,2-8°C

溶解度DMSO: 125 mg/mL (212.32 mM)

酸度系數(shù)(pKa)10.07±0.20(Predicted)

形態(tài)Solid

顏色White to light yellow

InChIKeyLQQUOMJXUXVPRB-IOTKHNBZSA-N

SMILES[S](=O)(=O)(N5C[C@H](C[C@H](C5)C)C)c1cc2c(cc1)C(c3c(cc(cc3)[S](=O)(=O)N4C[C@H](C[C@H](C4)C)C)C2N=O)N=O

安全數(shù)據(jù)

WGK GermanyWGK 3

存儲類別11 - Combustible Solids

圖譜信息

1227637-23-1(1227637-23-1)核磁圖(¹HNMR)

1227637-23-1價格(試劑級)

報價日期	產品編號	產品名稱	CAS號	包裝	價格
2026/07/06	S0733	1227637-23-1 Tegatrabetan (BC-2059)	1227637-23-1	5mg	2269.4元
2026/07/06	S0733	Tegatrabetan (BC-2059)	1227637-23-1	10mM (1mL in DMSO)	2694.51元
2026/07/06	S0733	1227637-23-1 Tegatrabetan (BC-2059)	1227637-23-1	25mg	6855.76元

常見問題列表

生物活性

Tegatrabetan (BC2059) 是一種 β-Catenin 的拮抗劑。Tegatrabetan (BC2059) 會破壞β-catenin與scaffold protein transducin β-like 1 (TBL1)的結合以及蛋白酶體降解并降低β-catenin核水平。

靶點

Target	Value
β-catenin ()

體外研究

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.

體內研究

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.