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2241014-82-2

中文名稱(chēng) NAMPT inhibitor-linker 2
英文名稱(chēng) NAMPT inhibitor-linker 2
CAS 2241014-82-2
分子式 C34H33FN6O5
分子量 624.66
MOL 文件 2241014-82-2.mol
2241014-82-2 結(jié)構(gòu)式 2241014-82-2 結(jié)構(gòu)式

基本信息

中文別名
4-(4-(3-(2,5-二氧代-2,5-二氫-1H-吡咯-1-基)丙?;?哌嗪-1-基)-N-(2-氟-4-((1S,2S)-2-(吡啶-3-基)環(huán)丙烷-1-甲酰胺基)芐基)苯甲酰胺
英文別名
NAMPT inhibitor-linker 2
Benzamide, 4-[4-[3-(2,5-dihydro-2,5-dioxo-1H-pyrrol-1-yl)-1-oxopropyl]-1-piperazinyl]-N-[[2-fluoro-4-[[[(1S,2S)-2-(3-pyridinyl)cyclopropyl]carbonyl]amino]phenyl]methyl]-

物理化學(xué)性質(zhì)

沸點(diǎn)940.2±65.0 °C(Predicted)
密度1.395±0.06 g/cm3(Predicted)
酸度系數(shù)(pKa)13.91±0.70(Predicted)
形態(tài)Solid
顏色Off-white to light yellow
NAMPT inhibitor-linker 2價(jià)格(試劑級(jí))
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
2025/05/22HY-112616NAMPT inhibitor-linker 22241014-82-21 mg1364元
2025/05/22HY-112616NAMPT inhibitor-linker 22241014-82-25 mg3000元
2025/05/22HY-112616NAMPT inhibitor-linker 22241014-82-210 mg4800元

常見(jiàn)問(wèn)題列表

生物活性
NAMPT inhibitor-linker 2 為 ADC 的一部分,由一種 NAMPT 的抑制劑作為有效載荷和一個(gè)連接物組成。ADC-4 由一個(gè) NAMPT inhibitor-linker 2 和一個(gè) anti-c-Kit 單克隆抗體組成,對(duì)表達(dá) c-Kit 的細(xì)胞具有抑制作用,比如 GIST-T1 和 NCI-H526 細(xì)胞,IC50 值分別為 <7 pM 和 40 pM。
靶點(diǎn)

Traditional Cytotoxic Agents

體外研究

ADC-4 exihibits potent activity against c-Kit expressing cell lines such as GIST-T1 and NCI-H526, with IC 50 s of <7 pM and 40 pM, respectively.
ADC-4 (0.01 nM-10 nM, 144 hours) inhibits cell proliferation of GIST-T1 cells, but does not affect the cell cycle.

Cell Proliferation Assay

Cell Line: GIST-T1 cells
Concentration: 0.1 pM-10 nM
Incubation Time: 144 hours
Result: Inhibited the cell proliferation of GIST-T1 cells at 0.01-10 nM, and the inhibition remained unchanged after 1 nM.
體內(nèi)研究

ADC-4 (20 mg/kg, i.v. for 28 days) is tolerated, and causes tumor stasis in mice bearing GIST-T1 cells.

Animal Model: Female scid-beige (SCID bg) mice
Dosage: 20 mg/kg
Administration: A single intravenous injection (i.v.) for 28 days
Result: Significantly inhibited the growth of tumor in mice.
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