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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
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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
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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..…

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N-Bromosuccinimide Price

Cayman Chemical
Product number
18011
Product name
Pilaralisib
Purity
≥98%
Packaging
5mg
Price
$81
Updated
2024/03/01
Cayman Chemical
Product number
18011
Product name
Pilaralisib
Purity
≥98%
Packaging
10mg
Price
$153
Updated
2024/03/01
Cayman Chemical
Product number
18011
Product name
Pilaralisib
Purity
≥98%
Packaging
25mg
Price
$323
Updated
2024/03/01
Cayman Chemical
Product number
18011
Product name
Pilaralisib
Purity
≥98%
Packaging
50mg
Price
$581
Updated
2023/06/20
TRC
Product number
P441390
Product name
Pilaralisib
Packaging
10mg
Price
$120
Updated
2021/12/16
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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

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pilaralisib Suppliers

China 84 India 1 United States 12 Global 97
Shanghai Boyle Chemical Co., Ltd.
Tel
Fax
86-21-57758967
Email
sales@boylechem.com
Country
China
ProdList
2922
Advantage
55
Dalian Meilun Biotech Co., Ltd.
Tel
0411-62910999 13889544652
Email
sales@meilune.com
Country
China
ProdList
4729
Advantage
58
NCE Biomedical Co.,Ltd.
Tel
4000-027-021 |24 +86-13986109188 | +86-15623472865 | +81-08033611988
Fax
+86-27-87599188
Country
China
ProdList
1493
Advantage
55
Haoyuan Chemexpress Co., Ltd.
Tel
021-58950125
Fax
(86) 21-58955996
Email
info@chemexpress.com
Country
China
ProdList
7552
Advantage
61
Shanghai Aladdin Bio-Chem Technology Co.,LTD
Tel
400-6206333 13167063860
Fax
021-50323701
Email
anhua.mao@aladdin-e.com
Country
China
ProdList
25003
Advantage
65
MedChemexpress LLC
Tel
021-58955995
Fax
609-228-5909
Email
sales@medchemexpress.cn
Country
United States
ProdList
4861
Advantage
58
Suzhou yacoo science co.,Ltd
Tel
0512-87182056 18013166090
Fax
0512-87182056
Email
lingling.qi@yacoo.com.cn
Country
China
ProdList
7295
Advantage
60
ShangHai KenEn Chemical Technology Co., Ltd.
Tel
13120367189
Fax
021-50315529
Email
mychess007@163.com
Country
China
ProdList
1994
Advantage
55
AdooQ Bioscience CHINA
Tel
025-58849295 18951903616;
Fax
025-68650336
Email
info@adooq.cn
Country
China
ProdList
2990
Advantage
60
Shanghai Lollane Biological Technology Co.,Ltd.
Tel
021-52996696，15000506266 15000506266
Fax
+86-21-52996696
Country
China
ProdList
4613
Advantage
55
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View Lastest Price from pilaralisib manufacturers

Career Henan Chemical Co
Product
pilaralisib 934526-89-3
Price
US $1.00/g
Min. Order
1g
Purity
99%
Supply Ability
200kg
Release date
2019-12-30

934526-89-3, pilaralisibRelated Search:

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  • XL-147(Pilaralisib) (new)
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  • 934526-89-3
  • C25H25ClN6O4S
  • Inhibitors
  • API