ChemicalBook > CAS DataBase List > VS-5584

VS-5584

Product Name
VS-5584
CAS No.
1246560-33-7
Chemical Name
VS-5584
Synonyms
SB-2343;VS-5584 (SB2343);SB2343;CS-875;SB 2343;VS-5584;VS-5584, >=98%;VS-5584 VS5584;VS-5584 USP/EP/BP;VS-5584, 10 mM in DMSO
CBNumber
CB42666411
Molecular Formula
C17H22N8O
Formula Weight
354.41
MOL File
1246560-33-7.mol
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VS-5584 Property

Boiling point:
687.2±65.0 °C(Predicted)
Density 
1.48±0.1 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
insoluble in H2O; ≥17.7 mg/mL in DMSO; ≥4.71 mg/mL in EtOH with ultrasonic
form 
solid
pka
4.53±0.10(Predicted)
color 
Light yellow to yellow
InChI
InChI=1S/C17H22N8O/c1-10(2)25-11(3)21-14-13(12-8-19-16(18)20-9-12)22-17(23-15(14)25)24-4-6-26-7-5-24/h8-10H,4-7H2,1-3H3,(H2,18,19,20)
InChIKey
QYBGBLQCOOISAR-UHFFFAOYSA-N
SMILES
C1(N)=NC=C(C2=C3C(=NC(N4CCOCC4)=N2)N(C(C)C)C(C)=N3)C=N1
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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

H410Very toxic to aquatic life with long lasting effects

Precautionary statements

P260Do not breathe dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P273Avoid release to the environment.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Cayman Chemical
Product number
16294
Product name
VS-5584
Purity
≥98%
Packaging
1mg
Price
$32
Updated
2024/03/01
Cayman Chemical
Product number
16294
Product name
VS-5584
Purity
≥98%
Packaging
5mg
Price
$139
Updated
2024/03/01
Cayman Chemical
Product number
16294
Product name
VS-5584
Purity
≥98%
Packaging
10mg
Price
$230
Updated
2024/03/01
ChemScene
Product number
CS-1202
Product name
VS-5584
Purity
98.15%
Packaging
5mg
Price
$90
Updated
2021/12/16
ChemScene
Product number
CS-1202
Product name
VS-5584
Purity
98.15%
Packaging
10mg
Price
$120
Updated
2021/12/16
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VS-5584 Chemical Properties,Usage,Production

Description

Phosphatidylinositol 3-kinase (PI3K) signaling through Akt/PKB and the mammalian target of rapamycin (mTOR) controls gene expression related to cell proliferation, differentiation, and apoptosis. Increased activity of this pathway is important in many types of cancer. VS-5584 is a purine analog that inhibits mTOR (IC50 = 37 nM) and PI3K (IC50s = 16, 68, 25, and 42 nM for the α, β, γ, and δ isoforms, respectively) without relevant activity against more than 400 additional lipid and protein kinases. By inhibiting the phosphorylation of substrates downstream of PI3K and mTOR, VS-5584 demonstrates broad anti-proliferative sensitivity leading to tumor growth inhibition in human tumor models.

Uses

VS-5584 is a pan-PI3K/mTOR kinase inhibitor with IC50s of 16 nM, 68 nM, 42 nM, 25 nM, and 37 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ and mTOR, respectively. VS-5584 simultaneously blocks mTORC2 as well as mTORC1.

in vivo

Nude mice bearing MDA-MB-231 human breast cancer tumors are treated for 5 days with once daily oral VS-5584 (25 mg/kg). Oral treatment of tumor bearing mice with VS-5584 reduces cancer atem cells analyzed from extracted tumors. Mice are implanted with tumor fragments from a docetaxel-resistant patient-derived triple negative breast cancer. Mice are treated with VS-5584 (20 mg/kg, po, qd) or Docetaxel (20 mg/kg, i.v.). Oral VS-5584 induces tumor regression in a Docetaxel-resistant patient-derived breast cancer model[1]. A single oral dose of VS-5584 is rapidly absorbed with a tmax of 0.9 hours and an elimination half-life of 10 hours. To determine the pharmacokinetic and pharmacodynamic relationship in tumors, PC3-tumor–bearing mice are treated with a single dose of VS-5584 and plasma and tumors are harvested after 6 hours and analyzed for concentrations of VS-5584 and effects on target efficacy biomarkers. Plasma levels of VS-5584 increase dose-dependently. For evaluation of efficacy in a Rapamycin-sensitive PC3 engraftment model, tumor-bearing mice are treated with VS-5584 for 28 days in comparison with the rapalog Everolimus. VS-5584 is well tolerated at both doses tested (11 and 25 mg/kg) with minimal weight loss (mean 4.7% on day 27). Treatment with VS-5584 leads to significant tumor growth inhibition (TGI) of 79% and 113% for 11 and 25 mg/kg, respectively[1].

target

mTOR

IC 50

PI3Kα: 16 nM (IC50); PI3Kγ: 25 nM (IC50); PI3Kδ: 42 nM (IC50); PI3Kβ: 68 nM (IC50); Vps34: 7470 nM (IC50); mTOR: 37 nM (IC50); mTORC1; mTORC2; DNA-PK: 1270 nM (IC50)

References

[1] Hart S, et al. VS-5584, a novel and highly selective PI3K/mTOR kinase inhibitor for the treatment of cancer. Mol Cancer Ther, 2013, 12(2), 151-161. DOI:10.1158/1535-7163.MCT-12-0466

VS-5584 Preparation Products And Raw materials

Raw materials

Preparation Products

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VS-5584 Suppliers

China 102 India 1 United Kingdom 1 United States 14 Global 118
Chongqing Chemieliva Pharmaceutical Co., Ltd.
Tel
18696571988
Fax
+86 (23) 6777-0220
Email
amy.lei@chemieliva.com
Country
China
ProdList
1553
Advantage
60
Shanghai Boyle Chemical Co., Ltd.
Tel
Fax
86-21-57758967
Email
sales@boylechem.com
Country
China
ProdList
2922
Advantage
55
Jinan Trio PharmaTech Co., Ltd.
Tel
0531-88811783
Fax
+86 (531) 55696010 QQ 1762738062
Email
sales@trio-pharmatech.com
Country
China
ProdList
1856
Advantage
62
Dalian Meilun Biotech Co., Ltd.
Tel
0411-62910999 13889544652
Email
sales@meilune.com
Country
China
ProdList
4747
Advantage
58
Shanghai Topbiochem Technology Co., Ltd
Tel
+86-21-60341587
Fax
+86-21-61294319
Email
sales@topbiochem.com
Country
China
ProdList
6175
Advantage
58
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
Guangzhou Isun Pharmaceutical Co., Ltd
Tel
020-39119399 18927568969
Fax
020-39119999
Email
isunpharm@qq.com
Country
China
ProdList
4720
Advantage
55
ShangHai Caerulum Pharma Discovery Co., Ltd.
Tel
18149758185
Email
sales-cpd@caerulumpharma.com
Country
China
ProdList
3506
Advantage
58
Suzhou yacoo science co.,Ltd
Tel
0512-87182056 18013166090
Fax
0512-87182056
Email
lingling.qi@yacoo.com.cn
Country
China
ProdList
6295
Advantage
60
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View Lastest Price from VS-5584 manufacturers

Career Henan Chemical Co
Product
VS-5584 1246560-33-7
Price
US $2.00/kg
Min. Order
1kg
Purity
99%
Supply Ability
100kg
Release date
2018-12-23

1246560-33-7, VS-5584Related Search:

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  • VS-5584, 10 mM in DMSO
  • VS-5584 (SB2343) ，S7016
  • 1246560-33-7
  • C17H22N8O
  • Akt
  • mTOR
  • PI3K
  • PI3K/Akt/mTOR
  • Inhibitors