Basic information Safety Supplier Related

pilaralisib

Basic information Safety Supplier Related

pilaralisib Basic information

Product Name:
pilaralisib
Synonyms:
  • pilaralisib
  • Pilaralisib (XL-147)
  • 2-Amino-N-[3-[N-[3-[(2-chloro-5-methoxyphenyl)amino]quinoxalin-2-yl]sulfamoyl]phenyl]-2-methylpropanamide
  • 2-amino-N-[3-[[3-(2-chloro-5-methoxyanilino)quinoxalin-2-yl]sulfamoyl]phenyl]-2-methylpropanamide
  • XL147(pilaralisib)
  • XL-147,Pilaralisib, SAR245408
  • PILARALISIB (XL147);SAR245408;XL 147
  • XL-147;SAR245408;XL147;XL 147;SAR-245408;SAR 245408; PILARALISIB
CAS:
934526-89-3
MF:
C25H25ClN6O4S
MW:
541.02
Product Categories:
  • Inhibitors
  • API
Mol File:
934526-89-3.mol
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pilaralisib Chemical Properties

Melting point:
216-220oC
Density 
1.458±0.06 g/cm3(Predicted)
storage temp. 
Refrigerator
solubility 
DMSO (Slightly)
pka
6.33±0.30(Predicted)
form 
Solid
color 
Light Yellow to Yellow
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pilaralisib Usage And Synthesis

Uses

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

Enzyme inhibitor

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.

pilaralisibSupplier

Shanghai Boyle Chemical Co., Ltd.
Tel
Email
sales@boylechem.com
Dalian Meilun Biotech Co., Ltd.
Tel
0411-62910999 13889544652
Email
meilunui@163.com
NCE Biomedical Co.,Ltd.
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4000-027-021 |24 +86-13986109188 | +86-15623472865 | +81-08033611988
Haoyuan Chemexpress Co., Ltd.
Tel
021-58950125
Email
info@chemexpress.com
Shanghai Aladdin Bio-Chem Technology Co.,LTD
Tel
400-400-6206333 18521732826
Email
market@aladdin-e.com