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    當(dāng)9號(hào)染色體上的ABL基因與22號(hào)染色體上的BCR基因結(jié)合時(shí)，形成BCR-ABL融合基因。BCR-ABL被翻譯成具有致癌性的組成型活性酪氨酸激酶。根據(jù)融合位置的不同，形成了分子量范圍為185-210 kDa的多種蛋白質(zhì)變體。BCR-ABL激活JAK/STAT通路和MAPK信號(hào)。[3]這種基因在大多數(shù)慢性髓性白血病(CML)患者中發(fā)現(xiàn)，在一些急性淋巴細(xì)胞白血病(ALL)或急性髓性白血病(AML)患者中發(fā)現(xiàn)。 Ponatinib是第二代BCR-Abl激酶的pan抑制劑，對(duì)BCR-Abl (T315I)的突變形式也有效。野生型和突變型的[1，2] IC50分別為0.5和11 nM。[4]在體外，Ponatinib還抑制幾種其他臨床相關(guān)激酶(RET、FLT3、KIT、PDGFRα、PDGFRβ和FGFR1)，在Ba/F3細(xì)胞系中的IC50s為5、25、100、5、9和23。[4]

產(chǎn)品性質(zhì)：

Cas No.:943319-70-8

別名:普納替尼; AP24534

化學(xué)名: 3-(2-imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-N-[4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]benzamide

Canonical SMILES CC1=C(C=C(C=C1)C(=O)NC2=CC(=C(C=C2)CN3CCN(CC3)C)C(F)(F)F)C#CC4=CN=C5N4N=CC=C5

分子式:C29H27F3N6O

分子量:532.56

溶解度:≥ 53.3mg/mL in DMSO

儲(chǔ)存條件:Store at -20°C

注意事項(xiàng)：

為了您的安全和健康，請(qǐng)穿實(shí)驗(yàn)服并戴一次性手套操作。

References:

1. Huang WS, Metcalf CA, Sundaramoorthi R, Wang Y, Zou D, Thomas RM, Zhu X, Cai L, Wen D, Liu S, Romero J, Qi J, Chen I, Banda G, Lentini SP, Das S, Xu Q, Keats J, Wang F, Wardwell S, Ning Y, Snodgrass JT, Broudy MI, Russian K, Zhou T, Commodore L, Narasimhan NI, Mohemmad QK, Iuliucci J, Rivera VM, Dalgarno DC, Sawyer TK, Clackson T, Shakespeare WC (June 2010). Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl) methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including the T315I gatekeeper mutant. J. Med. Chem. 53 (12): 4701–19.

2. O'Hare T, Pollock R, Stoffregen EP, Keats JA, Abdullah OM, Moseson EM, Rivera VM, Tang H, Metcalf Ca CA, Bohacek RS, Wang Y, Sundaramoorthi R, Shakespeare WC, Dalgarno D, Clackson T, Sawyer TK, Deininger MW, Druker BJ (2004). Inhibition of wild-type and mutant Bcr-Abl by AP23464, a potent ATP-based oncogenic protein kinase inhibitor: implications for CML. Blood 104 (8): 2532–2539.

3. Cilloni D and Saglio G. Molecular pathways: BCR-ABL. Clinical Cancer Res (2011) 18(4):930-937

4. Gozgit JM, Wong MJ, Zhu X, Schrock AB, Chen T, Clackson T and Rivera VM. Ponatinib, a potent pan-BCR-ABL inhibitor, retains activity against gatekeeper mutants of FLT3, RET, KIT, PDGFR α/β and FGFR1. 2012 AACR poster.