135897-06-2

中文名稱 SB218078

英文名稱 SB218078

CAS 135897-06-2

分子式 C24H15N3O3

分子量 393.39

MOL 文件 135897-06-2.mol

135897-06-2 結(jié)構(gòu)式

基本信息物理化學(xué)性質(zhì) 安全數(shù)據(jù) SB218078價(jià)格(試劑級(jí)) 常見(jiàn)問(wèn)題列表

基本信息

中文別名

化合物 T16848

英文別名

SB218078 ?SB-218078
9,10,11,12-Tetrahydro-9,12-epoxy-1H-diindolo[1,2,3-fg:3',2',1'-kl]pyrrolo[3,4-i][1,6]benzodiazocine-1,3(2H)-dione
9,12-Epoxy-1H-diindolo[1,2,3-fg:3',2',1'-kl]pyrrolo[3,4-i][1,6]benzodiazocine-1,3(2H)-dione, 9,10,11,12-tetrahydro-

所屬類(lèi)別

生物化工：抑制劑

物理化學(xué)性質(zhì)

熔點(diǎn)>340 °C

密度1.80±0.1 g/cm3(Predicted)

儲(chǔ)存條件Store at RT

溶解度≤5mg/ml in DMSO;5mg/ml in dimethyl formamide

酸度系數(shù)(pKa)9.75±0.20(Predicted)

形態(tài)結(jié)晶固體

顏色Light yellow to yellow

InChI1S/C24H15N3O3/c28-23-19-17-11-5-1-3-7-13(11)26-15-9-10-16(30-15)27-14-8-4-2-6-12(14)18(22(27)21(17)26)20(19)24(29)25-23/h1-8,15-16H,9-10H2,(H,25,28,29)

InChIKeyOTPNDVKVEAIXTI-UHFFFAOYSA-N

安全數(shù)據(jù)

危險(xiǎn)性符號(hào)(GHS) 有害 (GHS07)

GHS07

警示詞警告

危險(xiǎn)性描述H302-H315-H319-H335

防范說(shuō)明P261-P305+P351+P338

WGK GermanyWGK 1

存儲(chǔ)類(lèi)別11 - Combustible Solids

SB218078價(jià)格(試劑級(jí))

報(bào)價(jià)日期	產(chǎn)品編號(hào)	產(chǎn)品名稱	CAS號(hào)	包裝	價(jià)格
2026/06/05	HY-107407	SB218078 SB-218078	135897-06-2	1 mg	1380元
2026/06/05	HY-107407	SB218078 SB-218078	135897-06-2	5 mg	3450元
2026/06/05	HY-107407	SB218078 SB-218078	135897-06-2	10 mg	5700元

常見(jiàn)問(wèn)題列表

生物活性

SB-218078 是一種有效的，選擇性，ATP 競(jìng)爭(zhēng)性且細(xì)胞可滲透的檢查點(diǎn)激酶 1 (Chk1) 抑制劑，可抑制 cdc25C 的 Chk1 磷酸化，IC50 為 15 nM。SB-218078 對(duì) Cdc2 (IC50 為 250 nM) 和 PKC (IC50 為 1000 nM) 的抑制作用較弱。SB-218078 通過(guò) DNA 損傷和細(xì)胞周期停滯誘導(dǎo)細(xì)胞凋亡。

靶點(diǎn)

Chk1

15 nM (IC ₅₀ )

Cdc2

250 nM (IC ₅₀ )

PKC

1000 nM (IC ₅₀ )

Apoptosis

體外研究

SB-218078 (2.5-5 μM; 18 hours; HeLa cells) treatment abrogates G2 cell cycle arrest caused by either γ-irradiation or a topoisomerase I Topotecan inhibition.
SB-218078 (500-625 μM; 96 hours; HeLa and HT-29 cells) treatment significantly increases the cytotoxicity of DNA damage .

Cell Cycle Analysis

Cell Line:	HeLa cells
Concentration:	2.5 μM, 5 μM
Incubation Time:	18 hours
Result:	Abrogated G2 cell cycle arrest caused by γ-irradiation and topoisomerase I inhibition.

Cell Cytotoxicity Assay

Cell Line:	HeLa and HT-29 cells
Concentration:	500 nM, 625 nM
Incubation Time:	96 hours
Result:	Enhanced cytotoxicity of DNA damage.

體內(nèi)研究

SB-218078 (5 mg/kg; intraperitoneal injection; for 16 hours; C57/Bl6 mice) treatment could promote a strong increase of γ-H2AX and apoptosis throughout the lymphoma, while having no effect on a healthy spleen in Myc-induced lymphomas mouse model.