300809-71-6
中文名稱
4-(苯并[D]噻唑-2-基硫基)-3-氯苯胺
英文名稱
4-(benzo[d]thiazol-2-ylthio)-3-chloroaniline
CAS
300809-71-6
分子式
C13H9ClN2S2
分子量
292.81
MOL 文件
300809-71-6.mol
更新日期
2023/02/22 11:54:00
300809-71-6 結(jié)構(gòu)式
基本信息
中文別名
化合物KRAS INHIBITOR-94-(苯并[D]噻唑-2-基硫基)-3-氯苯胺
英文別名
DUN097160375-0604
4-(benzo[d]thiazol-2-ylthio)-3-chloroaniline
Benzenamine, 4-(2-benzothiazolylthio)-3-chloro-
non-small,proliferation,inhibit,KRAS inhibitor 9,KRAS inhibitor9,cytotoxicity,Apoptosis,cell,H460,mutant,H2122,H358,lung,Inhibitor,Ras,cancer,cells,KRAS inhibitor-9,GTP-KRAS
物理化學(xué)性質(zhì)
沸點(diǎn)492.4±55.0 °C(Predicted)
密度1.49±0.1 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度DMSO: 250 mg/mL (853.80 mM)
酸度系數(shù)(pKa)2.37±0.10(Predicted)
形態(tài)Solid
顏色White to off-white
4-(苯并[D]噻唑-2-基硫基)-3-氯苯胺價(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 |
| 2023/01/06 | S2958 | 4-(苯并[D]噻唑-2-基硫基)-3-氯苯胺 0375-0604 (KRAS inhibitor-9) | 300809-71-6 | 25mg | 4168.71元 |
常見問題列表
生物活性
KRAS inhibitor-9 是有效的 KRAS 抑制劑 (Kd=92 μM)，阻止 GTP-KRAS 的形成和 KRAS 下游激活。KRAS inhibitor-9 以中等的結(jié)合親和力與 KRAS G12D，KRAS G12C 和 KRAS Q61H 蛋白結(jié)合。KRAS inhibitor-9 導(dǎo)致 G2/M 細(xì)胞周期停滯并誘導(dǎo)凋亡 (apoptosis)。KRAS inhibitor-9 選擇性抑制具有 KRAS 突變的 NSCLC 細(xì)胞的增殖，但不抑制正常肺細(xì)胞的增殖。KRAS inhibitor-9體外研究
KRAS inhibitor-9 bound to KRASG12D, KRAS G12C and KRAS Q61H protein with a moderate binding affinity of -5.38, -5.41, and -3.97 kcal/mol, respectively.
KRAS inhibitor-9 (0-100 μM) shows strong inhibition selectivity in NSCLC cells with IC
50
s ranging from 39.56 to 66.02 μM for H2122, H358 and H460 cells (at 72 hours).
KRAS inhibitor-9 (0-100 μM; 24 hours) blocks GTP-KRAS formation in H2122, H358 and H460 cells.
KRAS inhibitor-9 (25-100 μM; 48 hours) inhibits the activation of KRAS downstream signaling pathway.
KRAS inhibitor-9 (0-100 μM; 24-72 hours) induces cell cycle arrest and apoptosis in NSCLC.
Cell Viability Assay
| Cell Line: | H2122 (KRAS G12C), H358 (KRAS G12C) and H460 (KRAS Q61H) cell lines |
| Concentration: | 0, 25, 50, 100 μM |
| Incubation Time: | 24, 48, and 72 hours |
| Result: | Inhibited three NSCLC cell lines in a dose- and time-dependent manner, but not in normal lung fibroblast cell line CCD-19Lu. |
Western Blot Analysis
| Cell Line: | H2122, H358 and H460 cells |
| Concentration: | 0, 25, 50, 100 μM |
| Incubation Time: | 48 hours |
| Result: | Reduces the levels of phosphorylation of CRAF and AKT in a dose-dependent manner in H2122, H358 and H460 cells. |
Apoptosis Analysis
| Cell Line: | H2122, H358, H460 cells |
| Concentration: | 0, 25, 50, 100 μM |
| Incubation Time: | 24-72 hours |
| Result: | Significantly decreased in G0/G1 phase while remarkably increased in G2/M phase after 24 hours and induced a significantly increased apoptosis for 48h in NSCLC cell lines. |