pilaralisib
- Product Name
- pilaralisib
- CAS No.
- 934526-89-3
- Chemical Name
- pilaralisib
- Synonyms
- CS-1670;pilaralisib;XL147(pilaralisib);Pilaralisib (XL-147);XL-147(Pilaralisib) (new);Pilaralisib, 10 mM in DMSO;XL-147,Pilaralisib, SAR245408;PILARALISIB (XL147);SAR245408;XL 147;XL-147; SAR245408;XL147;XL 147;SAR-245408;SAR 245408;XL-147;SAR245408;XL147;XL 147;SAR-245408;SAR 245408; PILARALISIB
- CBNumber
- CB72666700
- Molecular Formula
- C25H25ClN6O4S
- Formula Weight
- 541.02
- MOL File
- 934526-89-3.mol
pilaralisib Property
- 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
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Danger
- Hazard statements
-
H302Harmful if swallowed
H372Causes damage to organs through prolonged or repeated exposure
- Precautionary statements
-
P260Do not breathe dust/fume/gas/mist/vapours/spray.
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P270Do not eat, drink or smoke when using this product.
P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.
P314Get medical advice/attention if you feel unwell.
P330Rinse mouth.
P501Dispose of contents/container to..…
N-Bromosuccinimide Price
- Product number
- 18011
- Product name
- Pilaralisib
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $81
- Updated
- 2024/03/01
- Product number
- 18011
- Product name
- Pilaralisib
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $153
- Updated
- 2024/03/01
- Product number
- 18011
- Product name
- Pilaralisib
- Purity
- ≥98%
- Packaging
- 25mg
- Price
- $323
- Updated
- 2024/03/01
- Product number
- 18011
- Product name
- Pilaralisib
- Purity
- ≥98%
- Packaging
- 50mg
- Price
- $581
- Updated
- 2023/06/20
- Product number
- P441390
- Product name
- Pilaralisib
- Packaging
- 10mg
- Price
- $120
- Updated
- 2021/12/16
pilaralisib Chemical Properties,Usage,Production
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.
in vivo
The ability of Pilaralisib (XL147) to inhibit this endogenous phosphorylation of AKT, p70S6K, and S6 is examined following a single oral dose of 10, 30, 100, or 300 mg/kg. The tumors are harvested 4, 24, or 48 hours postdose and homogenized in lysis buffer. Tumor lysates from each animal (n=4) are then pooled for each group and analyzed for levels of total and phosphorylated AKT, p70S6K, and S6 by Western immunoblotting. Administration of Pilaralisib (XL147) causes a dose-dependent decrease in phosphorylation of AKT, p70S6K, and S6 in the tumors, reaching a maximum of 81% inhibition of AKT phosphorylation at 300 mg/kg at 4 hours. The dose-response relationships derived from the 4-hour time point predict 50% inhibition of AKT, p70S6K, and S6 phosphorylation at doses of approximately 100 mg/kg (pAKTT308), 54 mg/kg (pAKTS473), 71 mg/kg (p-p70S6K), and 103 mg/kg (pS6). The inhibition of AKT, p70S6K, and S6 phosphorylation in MCF7 tumors following a 100 mg/kg dose of Pilaralisib (XL147) is maximal at 4 hours, reaching 55% to 75%; however, the level of inhibition decreased to 8% to 45% by 24 hours, and only minimal or no inhibition was evident by 48 hours. Following a 300 mg/kg dose of Pilaralisib (XL147), inhibition is also maximal at 4 hours (65%-81%). However, in contrast with the 100 mg/kg dose, inhibition at 24 hours (51%-78%) is almost comparable with that seen at 4 hours, and partial inhibition (25%-51%) persisted through 48 hours[1].
IC 50
PI3Kγ: 23 nM (IC50); PI3Kδ: 36 nM (IC50); PI3Kα: 39 nM (IC50); PI3Kβ: 383 nM (IC50); Vps34: 6974 nM (IC50); DNA-PK: 4750 nM (IC50)
pilaralisib Preparation Products And Raw materials
Raw materials
Preparation Products
pilaralisib Suppliers
- Tel
- --
- Fax
- --
- sales@ajchem.in
- Country
- India
- ProdList
- 6100
- Advantage
- 58
View Lastest Price from pilaralisib manufacturers
- Product
- pilaralisib 934526-89-3
- Price
- US $1.00/g
- Min. Order
- 1g
- Purity
- 99%
- Supply Ability
- 200kg
- Release date
- 2019-12-30