MK-4101
作者：齊岳
發(fā)布時(shí)間：2023-09-06
08:59:45
點(diǎn)擊數(shù)：
產(chǎn)品名稱：MK-4101
產(chǎn)品描述：
| 產(chǎn)品描述 | MK-4101, an effective inhibitor of the Hedgehog pathway, has anti-tumor activity through the induction of extensive apoptosis and inhibition of proliferation in tumor cells. |
| 靶點(diǎn)活性 | 293 cells:1.1 μM (IC50), mouse cells:1.5 μM (IC50), KYSE180 oesophageal cancer cells:1 μM (IC50) |
| 體外活性 | MK-4101 inhibits Hh signaling both in a reporter gene assay in an engineered mouse cell line (Gli_Luc) with IC50 = 1.5 μM and in human KYSE180 oesophageal cancer cells with an IC50 = 1 μM. Furthermore, MK-4101 displaced a fluorescently-labeled cyclopamine derivative from 293 cells expressing recombinant human SMO with an IC50 = 1.1 μM. MK-4101 arrests cells in G1 and G2 phases[1]. |
| 體內(nèi)活性 | MK-4101 has robust antitumor activity through the inhibition of proliferation and induction of extensive apoptosis in tumor cells. MK-4101 is highly efficacious against primary medulloblastoma and basal cell carcinoma(BCC) developing in the cerebellum and skin of Ptch1+/- mice. Pharmacokinetics of MK-4101 shows that it could be administered orally, showing a good bioavailability (F ≥ 87 %) with low-to-moderate plasma clearance in mice and rats. Moreover, it was well absorbed, and mainly excreted into the bile[1]. |
| 激酶實(shí)驗(yàn) | Luciferase assays: After various compound treatments, cells are lysed in luciferase lysis buffer and assayed for luciferase activity using the ONE-Glo luciferase assay system. All luciferase activities are normalized to protein concentration determined by Bradford assay. |
| 細(xì)胞實(shí)驗(yàn) | BCC cells are treated with MK-4101(10 μM) for 72 h and cell cycle is analyzed by FACS monitoring EdU incorporation. (Only for Reference) |
| 分子量 | 493.47 |
| 分子式 | C24H24F5N5O |
| CAS No. | 935273-79-3 |
存儲(chǔ)
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
Ethanol: 60 mg/mL (121.6 mM)
DMSO: 92 mg/mL (186.4 mM)
H2O: <1 mg/mL
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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西安齊岳生物科技有限公司是集化學(xué)科研和定制與一體的高科技化學(xué)公司。業(yè)務(wù)范圍包括化學(xué)試劑和產(chǎn)品的研發(fā)、生產(chǎn)、銷售等。涉及產(chǎn)品為通用試劑的分銷、非通用試劑的定制與研發(fā)，涵蓋生物科技、化學(xué)品、中間體和化工材料等領(lǐng)域。
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