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ICC1401 MK-1775
MK-1775,>99%
【英文同義名】:MK 1775, MK1775
訂購(gòu)信息:(*,常備現(xiàn)貨)
品 牌 | 產(chǎn)品名稱 | 產(chǎn)品貨號(hào) | 規(guī) 格 | 目錄價(jià)(元) |
Gene Operation | ICC1401-0005MG | 5 mg | ¥1,299.00 | |
ICC1401-0010MG | 10 mg | ¥2,299.00 | ||
ICC1401-0025MG | 25 mg | ¥3,839.00 | ||
ICC1401-0050MG | 50 mg | ¥6,439.00 |
產(chǎn)品描述
是一種有效的WEE1選擇性抑制劑,其IC50為5.2nM。與其他223種激酶相比,該藥物選擇性作用于wee1,例如,其對(duì)wee1的選擇性是Myt1(另外一種通過(guò)磷酸化蘇氨酸抑制cdc2的激酶)的100倍[1]。可以抑制cdc2 Tyr15的磷酸化,破壞G2檢查點(diǎn),加強(qiáng)DNA損傷試劑如gemcitabine, carboplatin and cisplatin 的細(xì)胞毒性作用。可以聯(lián)合多種DNA損傷試劑,如5-FU, capecitibine, camptothecin, mitomycin C, doxorubicin,和pemetrexed等 以多種方式發(fā)揮抗腫瘤效應(yīng)[2]。目前已進(jìn)入臨床II期試驗(yàn)階段,與gemcitabine, Irinotecan Hydrochloride, cisplatin, or carboplatin等共同用于實(shí)體瘤的治療[3]。
靶點(diǎn)
靶點(diǎn) | WEE1 |
IC50(半數(shù)有效濃度) | 5.2 nM |
化學(xué)特性
Cas No.: 955365-80-7 | M. Wt.: 500.6 |
Formula: C27H32N8O2 | Purity: >99% |
Synonym: MK 1775, MK1775 | |
Chemical Name: 2-allyl-1-(6-(2-hydroxypropan-2-yl)pyridin-2-yl)-6-(4-(4-methylpiperazin-1-yl)phenylamino)-1,2-dihydropyrazolo [3,4-d]pyrimidin-3-one | |
Appearance: almost white powder to yellow powder | |
Solubility: Soluble in DMSO (80mg/ml) | |
Storage:Store powder at -20 ºC for the stability of three years. |
儲(chǔ)存液配制
儲(chǔ)存液 (1 ml DMSO體系) | 1mM | 10mM | 20mM | 40mM |
質(zhì)量(mg) | 0.5006 | 5.006 | 10.012 | 15.018 |
結(jié)構(gòu)式
使用濃度(僅作參考)
的具體使用濃度請(qǐng)參考相關(guān)文獻(xiàn),并根據(jù)自身實(shí)驗(yàn)條件(如實(shí)驗(yàn)?zāi)康?,?xì)胞種類,培養(yǎng)特性等)進(jìn)行摸索和優(yōu)化。
參考文獻(xiàn)
[1] Mueller PR, et al. Myt1: a membrane-associated inhibitory kinase that phosphorylates Cdc2 on both threonine-14 and tyrosine-15. Science,270:86–90( 1995).
[2] Hirai H, et al. , a small molecule Wee1 inhibitor, enhances anti-tumor efficacy of various DNA-damaging agents, including 5-fluorouracil. Cancer Biol, 9:514–522(2010).
[3] Leijen S, et al. A phase I pharmacological and pharmacodynamic study of , a Wee1 tyrosine kinase inhibitor, in monotherapy and combination with gemcitabine, cisplatin, or carboplatin in patients with advanced solid tumors. J Clin Oncol; 46th Ann Meet Am Soc of Clin Oncol (ASCO),. p. 28:15s.( 2010).