ZSTK474

Product Name: ZSTK474
CAS No.: 475110-96-4
Chemical Name: ZSTK474
Synonyms: CS-438;ZSTK 474;ZSTK474 BASE;ZSTK474/ZSTK-474;ZSTK474 USP/EP/BP;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;1-[BIS(MORPHOLIN-4-YL)-1,3,5-TRIAZIN-2-YL]-2-(DIFLUOROMETHYL)-1,3-BENZODIAZOLE;2-(difluoromethyl)-1-(4,6-dimorpholino-1,3,5-triazin-2-yl)-1H-benzo[d]imidazole
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.

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Safety

HS Code: 29349990

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

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

TRC

Product number: Z701000
Product name: ZSTK474
Packaging: 50mg
Price: $235
Updated: 2021/12/16

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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.

target

PI3Kδ

References

1) Kong and Yamori et al. (2007), ZSTK474 is an ATP-competitive inhibitor of class I phosphatidylinositol 3 kinase isoforms; Cancer Sci., 98 1638 2) Yaguchi et al. (2006), Antitumor activity of ZST474, a new phosphatidylinositol 3-kinase inhibitor; J. Natl. Cancer Inst., 98 545 3) Xue et al. (2014), ZSTK474, a novel PI3K inhibitor, modulates human CD14+ monocyte-derived dendritic cell functions and suppresses experimental autoimmune encephalomyelitis; J. Mol. Med. (Berl.), 92 1057 4) Haruta et al. (2012), Inhibitory effects of ZST474, a phosphatidylinositol 3-kinase inhibitor, on adjuvant-induced arthritis in rats; Inflamm. Res., 61 551

ZSTK474 Preparation Products And Raw materials

Raw materials

Preparation Products

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ZSTK474 Suppliers

China 133 India 1 Switzerland 1 United Kingdom 1 United States 23 Global 159

Shanghai Yuanding Chem. Sci. & Tech. Co., Ltd.

Tel: 21-57721279
Fax: QQ：14057904
Email: sales@shydchem.com.cn
Country: China
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Shanghai Boyle Chemical Co., Ltd.

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J & K SCIENTIFIC LTD.

Tel: 010-82848833 400-666-7788
Fax: 86-10-82849933
Email: jkinfo@jkchemical.com
Country: China
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Chembest Research Laboratories Limited

Tel: +86-21-20908456
Fax: 021-58180499
Email: sales@BioChemBest.com
Country: China
ProdList: 6005
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Shanghai Paulshine Chemical Co., Ltd.

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Fax: +86-021-37788663
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Shanghai Longsheng chemical Co.,Ltd.

Tel: 021-58099652-8005 13585536065
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Email: bin.wu@shlschem.com
Country: China
ProdList: 9810
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Nanjing Chemlin Chemical Co., Ltd

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Email: info@chemlin.com.cn
Country: China
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Chemsky（shanghai）International Co.,Ltd.

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Jinan Trio PharmaTech Co., Ltd.

Tel: +86 (531) 88811783
Fax: +86 (531) 55696010 QQ 1762738062
Email: sales@trio-pharmatech.com (International market)
Country: China
ProdList: 1856
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Xi’an chemsoar Medical Technology Co., ltd

Tel: 029-86538357
Fax: 029-87871708
Country: China
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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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CS-438

2-(DifluoroMethyl)-1-[4,6-di(4-Morpholinyl)-1,3,5-triazin-2-yl]-1H-benziMidazole

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

4,4'-(6-(2-(difluoromethyl)-1H-benzo[d]imidazol-1-yl)-1,3,5-triazine-2,4-diyl)dimorpholine

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)-

4,4'-(6-(2-(Difluoromethyl)-1H-benzo[d]imidazol-1-yl)-1,3,5-triazine-2,4-diyl)dimorpholine

1-[BIS(MORPHOLIN-4-YL)-1,3,5-TRIAZIN-2-YL]-2-(DIFLUOROMETHYL)-1,3-BENZODIAZOLE

ZSTK474, ATP-competitve PI3K inhibitor

475110-96-4

C19H21F2N7O2

Inhibitors

Akt

mTOR

PI3K