934526-89-3 Usage
Description
Pilaralisib is a pharmaceutical compound that functions as a pan-PI3K inhibitor, which means it targets multiple isoforms of the phosphoinositol-3 kinase (PI3K) enzyme. This enzyme plays a crucial role in cell growth, proliferation, and survival, and its dysregulation is implicated in various cancers. Pilaralisib's ability to inhibit PI3K activity makes it a potential therapeutic agent for cancer treatment.
Uses
Used in Oncology:
Pilaralisib is used as an anticancer agent for the treatment of patients with chronic lymphocytic leukemia (CLL) or those with lymphoma that has relapsed or become refractory to standard treatments. By inhibiting the PI3K pathway, pilaralisib can help control the growth and spread of cancer cells, offering a targeted approach to managing these diseases.
In the context of different cancer types, pilaralisib's application may vary, but its primary use remains in oncology to target the PI3K pathway and potentially improve patient outcomes. Further research and clinical trials are necessary to explore its full potential and possible combination therapies with other treatments.
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.
Check Digit Verification of cas no
The CAS Registry Mumber 934526-89-3 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 9,3,4,5,2 and 6 respectively; the second part has 2 digits, 8 and 9 respectively.
Calculate Digit Verification of CAS Registry Number 934526-89:
(8*9)+(7*3)+(6*4)+(5*5)+(4*2)+(3*6)+(2*8)+(1*9)=193
193 % 10 = 3
So 934526-89-3 is a valid CAS Registry Number.
InChI:InChI=1/C21H16N6O2S2/c1-13-6-9-15(10-7-13)31(28,29)27-21-20(23-16-4-2-3-5-17(16)24-21)22-14-8-11-18-19(12-14)26-30-25-18/h2-12H,1H3,(H,22,23)(H,24,27)
934526-89-3Relevant articles and documents
CRYSTALLINE COMPOUNDS
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, (2014/04/03)
Provided herein are polymorph E, a mixed DMAC/toluene solvate and a DMSO solvate of N-(3-{[(2Z)-3-[(2-chloro-5- methoxyphenyl)amino]quinoxalin-2(1H)-ylidene]sulfamoyl}phenyl)-2- methylalaninamide.
