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產(chǎn)品描述：布格替尼，也稱為AP-26113，是一種口服活性、有效和選擇性的雙ALK/EGFR抑制劑。AP26113結(jié)合并抑制ALK激酶和ALK融合蛋白以及EGFR和突變體形式。這導(dǎo)致ALK激酶和EGFR激酶的抑制，破壞其信號(hào)通路，最終抑制易感腫瘤細(xì)胞中的腫瘤細(xì)胞生長。此外，AP26113似乎可以克服基于突變的抗性。ALK屬于胰島素受體超家族，在神經(jīng)系統(tǒng)發(fā)育中起重要作用；ALK失調(diào)和基因重排與一系列腫瘤有關(guān)。EGFR在多種癌細(xì)胞類型中過表達(dá)。

用途:AP26113是一種有效的ALK抑制劑，IC50為0.62 nM，可克服由于L1196M突變介導(dǎo)的Crizotinib抵抗作用。

產(chǎn)品名稱: Brigatinib (AP-26113)
CAS#: 1197953-54-0
分子式: C29H39ClN7O2P
分子量: 584.10176
元素分析: C, 59.63; H, 6.73; Cl, 6.07; N, 16.79; O, 5.48; P, 5.30

Synonym: AP26113; AP-26113; AP 26113, Brigatinib; Alunbrig.

IUPAC/Chemical Name: (2-((5-chloro-2-((2-methoxy-4-(4-(4-methylpiperazin-1-yl)piperidin-1-yl)phenyl)amino)pyrimidin-4-yl)amino)phenyl)dimethylphosphine oxide

InChi Key: AILRADAXUVEEIR-UHFFFAOYSA-N

InChi Code: InChI=1S/C29H39ClN7O2P/c1-35-15-17-37(18-16-35)21-11-13-36(14-12-21)22-9-10-24(26(19-22)39-2)33-29-31-20-23(30)28(34-29)32-25-7-5-6-8-27(25)40(3,4)38/h5-10,19-21H,11-18H2,1-4H3,(H2,31,32,33,34)

SMILES Code: CN1CCN(C2CCN(C3=CC=C(NC4=NC=C(Cl)C(NC5=CC=CC=C5P(C)(C)=O)=N4)C(OC)=C3)CC2)CC1

Appearance: Light yellow solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO (2 mg /mL) or ethanol (10mg/mL)

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001