장기간 또는 반복 노출되면 장기(또는, 영향을 받은 알려진 모든 장기를 명시)에 손상을 일으킴
특정 표적장기 독성 - 반복 노출
구분 1
위험
P260, P264, P270, P314, P501
예방조치문구:
P260
분진·흄·가스·미스트·증기·...·스프레이를 흡입하지 마시오.
P264
취급 후에는 손을 철저히 씻으시오.
P264
취급 후에는 손을 철저히 씻으시오.
P270
이 제품을 사용할 때에는 먹거나, 마시거나 흡연하지 마시오.
P301+P312
삼켜서 불편함을 느끼면 의료기관(의사)의 진찰을 받으시오.
P314
불편함을 느끼면 의학적인 조치·조언을 구하시오.
P330
입을 씻어내시오.
P501
...에 내용물 / 용기를 폐기 하시오.
pilaralisib C화학적 특성, 용도, 생산
용도
Pilaralisib is a pan-PI3K inhibitor used in the treatment of patients with chronic lymphocytic leukemia or relapsed or refractory lymphoma.
효소 저해제
This selective, reversible, and ATP-competitive Class I PI3K inhibitor (FW = 541.02 g/mol; CAS 934526-89-3; Solubility: 100 mg/mL DMSO, when warmed; < 1 mg/mL H2O), also known as XL147, SAR245408, and N-(3- {[(3-{[2-chloro-5-(methoxy)phenyl]-amino}quinoxalin-2- yl)amino]sulfonyl}phenyl)-2-methylalaninamide, targets PI3Kα (IC50 = 39 nM, PI3Kδ (IC50 = 36 nM), and PI3Kγ (IC50 = 23 nM), but only weakly for PI3Kβ. Pilaralisib is active against human breast cancer cell lines with constitutive PI3K activation. PI3K inhibitors reduce AKT activity and relieves suppression of receptor tyrosine kinase expression and activity. XL147 shows dose-dependent inhibition of cell growth and levels of pAKT and pS6, signal transducers in the PI3K/AKT/TOR pathway. In HER2- overexpressing cells, pilaralisib inhibition of PI3K is attended by upregulation of expression and phosphorylation of multiple receptor tyrosine kinases, including HER3. Knockdown of FoxO1 and FoxO3a transcription factors suppressed the induction of HER3, InsR, IGF1R, and FGFR2 mRNAs upon inhibition of PI3K. In HER2(+) cells, knockdown of HER3 with siRNA or cotreatment with the HER2 inhibitors trastuzumab or lapatinib enhance XL147-induced cell death and inhibition of pAKT and pS6. When tested separately, trastuzumab and lapatinib synergized with XL147 for inhibition of pAKT and growth of established BT474 xenografts. Compared with XL147 alone, the combination exhibited a superior antitumor effect against trastuzumab-resistant tumor xenografts.
