PI-103
- Product Name
- PI-103
- CAS No.
- 371935-74-9
- Chemical Name
- PI-103
- Synonyms
- PI-103;PI 103;PI 103 HYDROCHLORIDE;PI-103, Free Base, >99%;PI-103HydrochlorideSalt;PI-103 - CAS 371935-74-9 - Calbiochem;PI 3-Kinase Inhibitor (PI-103) B-0303;PI-103, 98%, a potent PI3K/Akt and mTOR inhibitor;3-(4-Morpholinopyrido[3',2':4,5]furo[3,2-d]pyrimidin-2-yl)phenol;3-(4-Morpholinopyrido[3',2':4,5] furo[3,2-d]pyriMidin-2-yl)phenol;3-[4-(4-Morpholinylpyrido[3',2',4,5]furo[3,2-d]pyrimidin-2-yl]phenol
- CBNumber
- CB82454333
- Molecular Formula
- C19H16N4O3
- Formula Weight
- 348.36
- MOL File
- 371935-74-9.mol
PI-103 Property
- Density
- 1.409±0.06 g/cm3(Predicted)
- storage temp.
- Keep in dark place,Sealed in dry,Store in freezer, under -20°C
- solubility
- Soluble in DMSO (up to 40 mg/ml)
- form
- White solid
- pka
- 9.06±0.10(Predicted)
- color
- White
- Stability:
- Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months.
N-Bromosuccinimide Price
- Product number
- 528100
- Product name
- PI-103 - CAS 371935-74-9 - Calbiochem<br />A cell-permeable pyridinylfuranopyrimidine compound that acts as a potent and ATP-competitive inhibitor of DNA-PK, PI3-K, and mTOR.
- Packaging
- 1mg
- Price
- $172
- Updated
- 2024/03/01
- Product number
- 528100
- Product name
- PI-103 - CAS 371935-74-9 - Calbiochem<br />A cell-permeable pyridinylfuranopyrimidine compound that acts as a potent and ATP-competitive inhibitor of DNA-PK, PI3-K, and mTOR.
- Packaging
- 5mg
- Price
- $632
- Updated
- 2024/03/01
- Product number
- 10009209
- Product name
- PI-103
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $30
- Updated
- 2024/03/01
- Product number
- 10009209
- Product name
- PI-103
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $113
- Updated
- 2024/03/01
- Product number
- 10009209
- Product name
- PI-103
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $169
- Updated
- 2024/03/01
PI-103 Chemical Properties,Usage,Production
Description
PI-103 (371935-74-9) is a potent inhibitor of PI-3 kinase, mTOR and DNA-PK, IC50 = 8, 88, 150, 48,? 20, 83 and 2 nM for p110α, p110?, p110γ, p110δ, mTORC1, mTORC2 and DNA-PK respectively.1,2 Synergizes with arsenic disulfide to eradicate AML stem cells by induction of differentiation.3 Inhibits the growth of gefitinib-resistant non-small cell lung cancer cell lines.4 Induces autophagy in drug-resistant glioma.5 Protects against a-synuclein-induced toxicity in human neurons by induction of macroautophagy.6
Uses
PI 103 is a dual inhbitor of Class IA phosphatidylinositol 3-kinase and mammalian target of rapaymycin complex 1 (mTORC1), both of which are involved in pathways often activated in myelogenous leukemia. PI 103 also functions to enhance tumour radiosensitivity.
Definition
ChEBI: An organic heterotricyclic compound that is pyrido[3',2':4,5]furo[3,2-d]pyrimidine substituted at positions 2 and 4 by 3-hydroxyphenyl and morpholin-4-yl groups respectively. A dual-kinase inhibitor with anti-cancer properties.
General Description
A cell-permeable pyridinylfuranopyrimidine compound that acts as a potent and ATP-competitive inhibitor of DNA-PK, PI3-K, and mTOR (IC50 = 2, 8, 88, 48, 150, 26, 20, and 83 nM for DNA-PK, p110α, p110β, p110δ, p110γ, PI3-KC2β, mTORC1, and mTORC2, respectively). It inhibits ATR and ATM only at much higher concentrations (IC50 = 850 and 920 nM, respectively) and exhibits little activity towards a panel of more than 40 other kinases even at concentrations as high as 10 μM. Shown to effectively block PI3-K/Akt signaling and cell proliferation in glioma cell lines both in vitro and in vivo. A 10 mM (2 mg/574 μl) solution of PI-103 (Cat. No. 528101) in DMSO is also available.
Biological Activity
Inhibitor of DNA-PK, PI 3-kinase (p110 α ) and mTOR (IC 50 values are 2, 8, 20, 26, 48, 83, 88, 150, 850, 920, ~ 1000 and 2300 nM for DNA-PK, p110 α , mTORC1, PI3KC2 β , p110 δ , mTORC2, p110 β , p110 γ , ATR, ATM, PI3KC2 α and hsVPS34 respectively). Inhibits growth of human tumor xenografts in mice in vivo .
Biochem/physiol Actions
Cell permeable: yes
target
Cell, 2013, 153(4):840-54
References
Knight et al. (2006), A Pharmacological map of the PI3-K family defines a role for p110alpha in insulin signaling; Cell, 125 733 Raynaud et al. (2007), Pharmacologic characterization of a potent inhibitor of a class I phosphatidylinositide 3-kinases; Cancer Res., 67 5840 Hong et al. (2011), Arsenic disulfide synergizes with the phosphoinositide 3-kinase inhibitor PI-103 to eradicate acute myeloid leukemia stem cells by inducing differentiation; Carcinogenesis, 32 1550 Zou et al. (2009), A novel dual PI3Kalpha/mTOR inhibitor PI-103 with high antitumor activity in non-small cell lung cancer cells; Int. J. Mol. Med. 24 97 Fan et al. (2010), Akt and autophagy cooperate to promote survival of drug-resistant glioma; Sci. Signal., 3 ra81 Hollerhage et al. (2019), Multiple molecular pathways stimulating macroautophagy protect from alpha-synuclein-induced toxicity in human neurons; Neuropharmacology, 149 13
PI-103 Preparation Products And Raw materials
Raw materials
Preparation Products
PI-103 Suppliers
- Tel
- 0550-5196001 15000891977
- Fax
- 0550-5196001
- wj520wjxby@126.com
- Country
- China
- ProdList
- 1925
- Advantage
- 55
- Tel
- Fax
- 86-21-57758967
- sales@boylechem.com
- Country
- China
- ProdList
- 2922
- Advantage
- 55
- Tel
- 010-82848833 400-666-7788
- Fax
- 86-10-82849933
- jkinfo@jkchemical.com
- Country
- China
- ProdList
- 96815
- Advantage
- 76
- Tel
- 821-50328103-801 18930552037
- Fax
- 86-21-50328109
- 3bsc@sina.com
- Country
- China
- ProdList
- 15839
- Advantage
- 69
- Tel
- +86-21-20908456
- Fax
- 021-58180499
- sales@BioChemBest.com
- Country
- China
- ProdList
- 6005
- Advantage
- 61
- Tel
- 21-57721279
- Fax
- QQ：14057904
- sales@shydchem.com.cn
- Country
- China
- ProdList
- 990
- Advantage
- 56
- Tel
- +86-21-68182121
- Fax
- +86-21-68182121
- Country
- China
- ProdList
- 882
- Advantage
- 52
- Tel
- 025-83697070
- Fax
- +86-25-83453306
- info@chemlin.com.cn
- Country
- China
- ProdList
- 19182
- Advantage
- 64
- Tel
- 021-50135380
- shchemsky@sina.com
- Country
- China
- ProdList
- 15402
- Advantage
- 60
- Tel
- +86 (531) 88811783
- Fax
- +86 (531) 55696010 QQ 1762738062
- sales@trio-pharmatech.com (International market)
- Country
- China
- ProdList
- 1856
- Advantage
- 62
- Tel
- 029-86538357
- Fax
- 029-87871708
- Country
- China
- ProdList
- 234
- Advantage
- 57
- Tel
- 0411-62910999 13889544652
- sales@meilune.com
- Country
- China
- ProdList
- 4727
- Advantage
- 58
- Tel
- 86-21-34053660
- Fax
- 86-21-34053661
- sale@labgogo.com
- Country
- China
- ProdList
- 9865
- Advantage
- 52
- Tel
- 025-58196018 800028039
- Fax
- 025-83453306
- sales@fartop.net
- Country
- China
- ProdList
- 2229
- Advantage
- 55
- Tel
- 021-58170097
- info@topbiochem.com
- Country
- China
- ProdList
- 9478
- Advantage
- 58
- Tel
- 028-81458053
- Fax
- 028-81458053
- novibiotech@163.com sales@novi-biotech.com
- Country
- China
- ProdList
- 226
- Advantage
- 55
- Tel
- 4000-027-021 |24 +86-13986109188 | +86-15623472865 | +81-08033611988
- Fax
- +86-27-87599188
- Country
- China
- ProdList
- 1493
- Advantage
- 55
- Tel
- +86 (21) 5811-6473 5811-6475
- Fax
- +86 (21) 6129-4103
- sales@koutingchina.com
- Country
- China
- ProdList
- 496
- Advantage
- 60
- Tel
- +86-021-50720296
- Fax
- +86-021-50720297
- service@synkinase.com
- Country
- China
- ProdList
- 266
- Advantage
- 58
- Tel
- 400-400-6206333 18521732826
- Fax
- 021-50323701
- market@aladdin-e.com
- Country
- China
- ProdList
- 25003
- Advantage
- 65
- Tel
- +86-21-38682181 15900741819
- Fax
- +86-21-38682181
- Country
- China
- ProdList
- 282
- Advantage
- 55
- Tel
- 020-39119399 18927568969
- Fax
- 020-39119999
- isunpharm@qq.com
- Country
- China
- ProdList
- 4674
- Advantage
- 55
- Tel
- 021-021-33632979 15002134094
- Fax
- 021-33632979
- marketing@targetmol.com
- Country
- China
- ProdList
- 7783
- Advantage
- 58
- Tel
- 86-21-50700185 13764109623
- Fax
- 86-21-50700185
- sale@inyelchem.com
- Country
- China
- ProdList
- 178
- Advantage
- 55
- Tel
- Mobile:13665161512
- Fax
- +86-510-68873513
- Country
- China
- ProdList
- 1785
- Advantage
- 58
- Tel
- 0086-571-86217390
- Fax
- 0086-571-86217391
- Sales@gihichem.com
- Country
- China
- ProdList
- 860
- Advantage
- 58
- Tel
- 18149758185 18149758185
- sales-cpd@caerulumpharma.com
- Country
- China
- ProdList
- 3466
- Advantage
- 58
- Tel
- 0512-62968256 18550502935
- Fax
- 0512-62968256
- export@laingbiotec.com
- Country
- China
- ProdList
- 1113
- Advantage
- 58
- Tel
- 0512-87182056 18013166090
- Fax
- 0512-87182056
- lingling.qi@yacoo.com.cn
- Country
- China
- ProdList
- 7295
- Advantage
- 60
- Tel
- 025-58849295 18951903616;
- Fax
- 025-68650336
- info@adooq.cn
- Country
- China
- ProdList
- 2990
- Advantage
- 60
- Tel
- 13621943973
- Fax
- -
- sales@shjiyipharmatech.com
- Country
- China
- ProdList
- 1166
- Advantage
- 55
- Tel
- +86 (21) 61124340
- Fax
- +86 (21) 6129-4103
- Country
- China
- ProdList
- 9756
- Advantage
- 58
- Tel
- 027-59599241 18871490274
- Fax
- 027-59599241
- 1400878000@qq.com
- Country
- China
- ProdList
- 9958
- Advantage
- 58
- Tel
- +86-21-5821 5861
- Fax
- +86-21-5106 2861
- sales@letopharm.com
- Country
- China
- ProdList
- 2384
- Advantage
- 58
- Tel
- 021-61415566 800-8193336
- orderCN@merckgroup.com
- Country
- China
- ProdList
- 51456
- Advantage
- 80
- Tel
- 021-52996696，15000506266 15000506266
- Fax
- +86-21-52996696
- Country
- China
- ProdList
- 4574
- Advantage
- 55
- Tel
- 18607101326 15172504745
- Fax
- +86-27-84254680
- aileen@chemfaces.com
- Country
- China
- ProdList
- 6905
- Advantage
- 55
- Tel
- 86-(0)21-31261262 373522135
- Fax
- 86-(0)21-33250524
- sales@novochemy.com
- Country
- China
- ProdList
- 6498
- Advantage
- 58
- Tel
- Fax
- -
- eric_feng1954@126.com
- Country
- China
- ProdList
- 9248
- Advantage
- 55
- Tel
- 17317567081
- info@coreuni.com
- Country
- China
- ProdList
- 201
- Advantage
- 55
- Tel
- 18620099427
- Fax
- +86-20-62619665
- amy@howeipharm.com
- Country
- China
- ProdList
- 17687
- Advantage
- 55
- Tel
- +86-400-851-9921
- Fax
- +86-10-82826195
- sales@pharmacodia.com
- Country
- China
- ProdList
- 2317
- Advantage
- 55
- Tel
- 02781293128
- orders@biochemsafebuy.com
- Country
- China
- ProdList
- 9923
- Advantage
- 55
- Tel
- 021-20242659 18930833303
- Fax
- +86 (21) 2024-2659
- Sales@changyanchem.cn
- Country
- China
- ProdList
- 5010
- Advantage
- 55
- Tel
- 025-83453382-8005
- Fax
- 025-83453382
- sale@parabiochem.com
- Country
- China
- ProdList
- 9595
- Advantage
- 55
- Tel
- 4009903999 13395398332
- Fax
- 0539-6365991
- sales@xiyashiji.com
- Country
- China
- ProdList
- 20806
- Advantage
- 60
- Tel
- 400-1166-196 18502815961
- Fax
- QQ：800101999
- cdhxsj@163.com
- Country
- China
- ProdList
- 14603
- Advantage
- 60
- Tel
- 17754423994 17754423994
- Fax
- QQ:2853530913
- 2853530910@QQ.com
- Country
- China
- ProdList
- 8011
- Advantage
- 62
- Tel
- Fax
- -
- 13006575422@163.com
- Country
- China
- ProdList
- 6355
- Advantage
- 58
- Tel
- 021-QQ：65489617 15618227136
- Fax
- 21-5161 9052
- Sales@ATKchemical.com
- Country
- China
- ProdList
- 7298
- Advantage
- 58
View Lastest Price from PI-103 manufacturers
- Product
- PI-103 371935-74-9
- Price
- US $2.00/kg
- Min. Order
- 1kg
- Purity
- 99%
- Supply Ability
- 100kg
- Release date
- 2018-12-24