pilaralisib Chemische Eigenschaften,Einsatz,Produktion Methoden

Verwenden

Pilaralisib is a pan-PI3K inhibitor used in the treatment of patients with chronic lymphocytic leukemia or relapsed or refractory lymphoma.

Enzyminhibitor

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.

pilaralisib Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte

pilaralisib Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.

Firmenname	Telefon	E-Mail	Land	Produktkatalog	Edge Rate
ATK CHEMICAL COMPANY LIMITED	+undefined-21-51877795	ivan@atkchemical.com	China	32998	60
career henan chemical co	+86-0371-86658258	factory@coreychem.com	China	29780	58
TargetMol Chemicals Inc.	+1-781-999-5354; +1-00000000000	marketing@targetmol.com	United States	32431	58
BOC Sciences	16314854226; +8616314854226	inquiry@bocsci.com	United States	19852	58
Dayang Chem (Hangzhou) Co.,Ltd.	+86-0571-88938639 17705817739	info@dycnchem.com	China	52693	58
Zhejiang J&C Biological Technology Co.,Limited	+1-2135480471	sales@sarms4muscle.com	China	10378	58
InvivoChem	+1-708-310-1919 +1-13798911105	sales@invivochem.cn	United States	6378	58
PT CHEM GROUP LIMITED	+86-85511178; +86-85511178	peter68@ptchemgroup.com	China	35405	58
ShenZhen Trendseen Biological Technology Co.,Ltd.	13417589054	trendseenbio@gmail.com	China	11674	58
Zibo Hangyu Biotechnology Development Co., Ltd	+86-0533-2185556 +86-15965530500	nickzhang@hangyubiotech.com	China	9937	58

934526-89-3()Verwandte Suche:

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• PILARALISIB (XL147);SAR245408;XL 147
• XL-147,Pilaralisib, SAR245408
• XL147(pilaralisib)
• 2-amino-N-[3-[[3-(2-chloro-5-methoxyanilino)quinoxalin-2-yl]sulfamoyl]phenyl]-2-methylpropanamide
• 2-Amino-N-[3-[N-[3-[(2-chloro-5-methoxyphenyl)amino]quinoxalin-2-yl]sulfamoyl]phenyl]-2-methylpropanamide
• Pilaralisib (XL-147)
• pilaralisib
• Propanamide, 2-amino-N-[3-[[[3-[(2-chloro-5-methoxyphenyl)amino]-2-quinoxalinyl]amino]sulfonyl]phenyl]-2-methyl-
• CS-1670
• XL-147; SAR245408;XL147;XL 147;SAR-245408;SAR 245408
• XL-147;SAR245408;XL147;XL 147;SAR-245408;SAR 245408; PILARALISIB
• XL-147(Pilaralisib) (new)
• Pilaralisib, 10 mM in DMSO
• 934526-89-3
• C25H25ClN6O4S
• Inhibitors
• API