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ZSTK474

Product Name
ZSTK474
CAS No.
475110-96-4
Chemical Name
ZSTK474
Synonyms
CS-438;ZSTK 474;ZSTK474 BASE;ZSTK474 ，S1072;ZSTK474/ZSTK-474;ZSTK474 USP/EP/BP;ZSTK474, 10 mM in DMSO;ZSTK474, ATP-competitve PI3K inhibitor;2-(2-Difluoromethylbenzimidazol-1-yl)-4,6-dimorpholino-1,3,5-triazine;2-(DifluoroMethyl)-1-[4,6-di(4-Morpholinyl)-1,3,5-triazin-2-yl]-1H-benziMidaz
CBNumber
CB0505419
Molecular Formula
C19H21F2N7O2
Formula Weight
417.41
MOL File
475110-96-4.mol
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ZSTK474 Property

Melting point:
217-219 °C(Solv: ethanol (64-17-5))
Boiling point:
640.3±65.0 °C(Predicted)
Density 
1.57
storage temp. 
-20°C
solubility 
Soluble in DMSO (up to 20 mg/ml) or in Ethanol (up to 2.5 mg/ml with warming).
form 
White powder.
pka
5.21±0.10(Predicted)
color 
White or off-white
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 3 months.
InChI
InChI=1S/C19H21F2N7O2/c20-15(21)16-22-13-3-1-2-4-14(13)28(16)19-24-17(26-5-9-29-10-6-26)23-18(25-19)27-7-11-30-12-8-27/h1-4,15H,5-12H2
InChIKey
HGVNLRPZOWWDKD-UHFFFAOYSA-N
SMILES
C1(C(F)F)N(C2=NC(N3CCOCC3)=NC(N3CCOCC3)=N2)C2=CC=CC=C2N=1
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Safety

HS Code 
29349990
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P271Use only outdoors or in a well-ventilated area.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P312Call a POISON CENTER or doctor/physician if you feel unwell.

P321Specific treatment (see … on this label).

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

P362Take off contaminated clothing and wash before reuse.

P403+P233Store in a well-ventilated place. Keep container tightly closed.

P405Store locked up.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

TCI Chemical
Product number
D6342
Product name
ZSTK 474
Packaging
100MG
Price
$267
Updated
2025/07/31
Cayman Chemical
Product number
17381
Product name
ZSTK474
Purity
≥98%
Packaging
5mg
Price
$49
Updated
2024/03/01
Cayman Chemical
Product number
17381
Product name
ZSTK474
Purity
≥98%
Packaging
10mg
Price
$77
Updated
2024/03/01
Cayman Chemical
Product number
17381
Product name
ZSTK474
Purity
≥98%
Packaging
25mg
Price
$168
Updated
2024/03/01
Cayman Chemical
Product number
17381
Product name
ZSTK474
Purity
≥98%
Packaging
50mg
Price
$263
Updated
2024/03/01
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ZSTK474 Chemical Properties,Usage,Production

Description

ZSTK474 (475110-96-4) is a novel Class I phosphatidylinositol 3-kinase (PI3K) inhibitor. ZSTK474 is an ATP-competitive inhibitor of all four Class I PI3K isoforms. However, it inhibits PI3Kδ most potently, with a Ki of 1.8 nM, while inhibiting the α, β and γ isoforms at slightly higher concentrations (6.7 nM, 10.4 nM and 11.7 nM, respectively)1. Displays potent antitumor activity against human cancer xenografts (A549, PC-3 and WiDr) when administered to mice2. ZSTK474 displays potent anti-inflammatory activity via modulation of human CD14+ monocyte-derived dendritic cell functions and suppresses experimental autoimmune encephalomyelitis3. Ameliorates the progression of adjuvant-induced arthritis in a rat model4.

Uses

ZSTK474 is a triazine derivative that acts as an inhibitor of class I phosphatidylinositol 3-kinase (PI3K) isoforms (IC50s = 17, 53, and 6 nM for p110β, -γ, and -δ, respectively). It is selective for PI3K, as it has negligible activity against 139 other kinases when tested at 30 μM. ZSTK474 is orally bioavailable and shows strong antitumor activity against human cancer xenografts in mice. The efficacy of ZSTK474 against certain cancer cells and tumors can be enhanced by combination therapy.

Uses

ZSTK474 is an ATP-competitive inhibitor of class I phosphatidylinositol 3 kinase (PI3K) isoforms. Potent PI3K inhibitor.

Definition

ChEBI: A triamino-1,3,5-triazine that is 1,3,5-triazine in which two of the hydrogens have been replaced by morpholin-4-yl groups while the third hydrogen has been replaced by a 2-(difluoromethyl)benzimidazol-1-yl group. It is an inhibitor of phosphatidylinositol 3-kinase.

in vivo

In mice subjected to MCAO, treatment with ZSTK474 is tested at dosages of 50, 100, 200, and 300 mg/kg. Since the 200 mg/kg dose produces significant improvement and no obvious toxic effects (P<0.01), mice are treated with ZSTK474 at a dose of 200 mg/kg/day daily for three post-MCAO days during the remaining experiments of this study. Neurological function is examined in mice suffered from MCAO followed by 24, 48, and 72 h of reperfusion. In the ZSTK474 group, neurological function scores are significantly better than the control group except the corner test[2].

target

PI3Kδ

IC 50

PI3Kδ: 4.6 nM (IC50); PI3Kα: 16 nM (IC50); PI3Kβ: 44 nM (IC50); PI3Kγ: 49 nM (IC50); Autophagy

References

[1] DEXIN KONG  Takao Y. ZSTK474 is an ATP-competitive inhibitor of class I phosphatidylinositol 3 kinase isoforms[J]. Cancer Science, 2007, 98 10: 1638-1642. DOI:10.1111/j.1349-7006.2007.00580.x
[2] SHIN-ICHI YAGUCHI. Antitumor activity of ZSTK474, a new phosphatidylinositol 3-kinase inhibitor.[J]. JNCI Journal of the National Cancer Institute, 2006, 98 8: 545-556. DOI:10.1093/jnci/djj133
[3] ZHENYI XUE. ZSTK474, a novel PI3K inhibitor, modulates human CD14+ monocyte-derived dendritic cell functions and suppresses experimental autoimmune encephalomyelitis.[J]. Journal of Molecular Medicine-Jmm, 2014, 92 10: 1057-1068. DOI:10.1007/s00109-014-1158-x
[4] KAZUHIKO HARUTA. Inhibitory effects of ZSTK474, a phosphatidylinositol 3-kinase inhibitor, on adjuvant-induced arthritis in rats.[J]. Inflammation Research, 2012: 551-562. DOI:10.1007/s00011-012-0444-8

ZSTK474 Preparation Products And Raw materials

Raw materials

Preparation Products

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ZSTK474 Suppliers

China 167 India 1 Switzerland 1 United Kingdom 1 United States 23 Global 193
Shanghai Yuanding Chem. Sci. & Tech. Co., Ltd.
Tel
21-57721279
Fax
QQ：14057904
Email
sales@shydchem.com.cn
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China
ProdList
998
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56
Shanghai Boyle Chemical Co., Ltd.
Tel
Fax
86-21-57758967
Email
sales@boylechem.com
Country
China
ProdList
2922
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55
J & K SCIENTIFIC LTD.
Tel
18210857532; 18210857532
Fax
86-10-82849933
Email
jkinfo@jkchemical.com
Country
China
ProdList
96815
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Chembest Research Laboratories Limited
Tel
+86-21-20908456
Fax
021-58180499
Email
sales@BioChemBest.com
Country
China
ProdList
6003
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61
Shanghai Paulshine Chemical Co., Ltd.
Tel
+86-021-37788663
Fax
+86-021-37788663
Country
China
ProdList
186
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64
Shanghai Longsheng chemical Co.,Ltd.
Tel
021-58099652-8005 13585536065
Fax
021-58099609
Email
bin.wu@shlschem.com
Country
China
ProdList
9883
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59
Nanjing Chemlin Chemical Co., Ltd
Tel
025-83697070
Fax
+86-25-83453306
Email
info@chemlin.com.cn
Country
China
ProdList
15883
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64
Chemsky（shanghai）International Co.,Ltd.
Tel
021-50135380
Email
shchemsky@sina.com
Country
China
ProdList
32321
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50
Jinan Trio PharmaTech Co., Ltd.
Tel
0531-88811783
Fax
+86 (531) 55696010 QQ 1762738062
Email
sales@trio-pharmatech.com
Country
China
ProdList
1856
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62
Xi’an chemsoar Medical Technology Co., ltd
Tel
029-86538357
Fax
029-87871708
Country
China
ProdList
234
Advantage
57
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View Lastest Price from ZSTK474 manufacturers

Career Henan Chemical Co
Product
ZSTK474 475110-96-4
Price
US $2.00/kg
Min. Order
1kg
Purity
99%
Supply Ability
100kg
Release date
2018-12-23

475110-96-4, ZSTK474Related Search:

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  • 1H-BenziMidazole, 2-(difluoroMethyl)-1-(4,6-di-4-Morpholinyl-1,3,5-triazin-2-yl)-
  • ZSTK474 BASE
  • ZSTK474/ZSTK-474
  • 2-(difluoromethyl)-1-(4,6-dimorpholino-1,3,5-triazin-2-yl)-1H-benzo[d]imidazole
  • 2-(2-Difluoromethylbenzimidazol-1-yl)-4,6-dimorpholino-1,3,5-triazine ZSTK-474
  • ZSTK 474 2-(2-Difluoromethylbenzimidazol-1-yl)-4,6-dimorpholino-1,3,5-triazine
  • ZSTK 474
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  • 2-(DifluoroMethyl)-1-[4,6-di(4-Morpholinyl)-1,3,5-triazin-2-yl]-1H-benziMidaz
  • 4-[4-[2-(difluoromethyl)benzimidazol-1-yl]-6-morpholin-4-yl-1,3,5-triazin-2-yl]morpholine
  • 2-(2-Difluoromethylbenzimidazol-1-yl)-4,6-dimorpholino-1,3,5-triazine
  • ZSTK474 USP/EP/BP
  • 3-Oxazolidinecarboxylicacid,2,2-dimethyl-4-(2-oxoethyl)-,1,1-dimethylethylester,(8S)-
  • 1-[BIS(MORPHOLIN-4-YL)-1,3,5-TRIAZIN-2-YL]-2-(DIFLUOROMETHYL)-1,3-BENZODIAZOLE
  • ZSTK474, ATP-competitve PI3K inhibitor
  • ZSTK474, 10 mM in DMSO
  • ZSTK474 ，S1072
  • 2-(Difluoromethyl)-1-(4,6-di-morpholin-4-yl-1,3,5-triazin-2-yl)-1H-benzo[d]imidazole
  • 475110-96-4
  • C19H21F2N7O2
  • Inhibitors
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  • mTOR
  • PI3K