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Merck
CN

529584

PTK/PI 3-K/mTOR Inhibitor, PP121

The PTK/PI 3-K/mTOR Inhibitor, PP121, also referenced under CAS 1092788-83-4, controls the biological activity of PTK/PI 3-K/mTOR. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

别名:

PTK/PI 3-K/mTOR Inhibitor, PP121, 1-Cyclopentyl-3-(1H-pyrrolo[2,3-b]pyridin-5-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine, PI 3-K/mTOR Inhibitor II, PDGFR Tyrosine Kinase Inhibitor XVIII, Abl Inhibitor IV, mTOR Inhibitor VII, VEGFR Tyrosine Kinase Inhibitor XXXII, VEGFR2 Kinase Inhibitor XXX, PI 3-K Inhibitor XIII

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关于此项目

经验公式（希尔记法）:
C17H17N7
化学文摘社编号:
1092788-83-4
分子量:
319.36
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
MFCD12912434

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产品名称

PTK/PI 3-K/mTOR Inhibitor, PP121, The PTK/PI 3-K/mTOR Inhibitor, PP121, also referenced under CAS 1092788-83-4, controls the biological activity of PTK/PI 3-K/mTOR. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

SMILES string

[n]2(nc(c5c2ncnc5N)c3cnc4[nH]ccc4c3)C1CCCC1

InChI

1S/C17H17N7/c18-15-13-14(11-7-10-5-6-19-16(10)20-8-11)23-24(12-3-1-2-4-12)17(13)22-9-21-15/h5-9,12H,1-4H2,(H,19,20)(H2,18,21,22)

InChI key

NVRXTLZYXZNATH-UHFFFAOYSA-N

assay

≥98% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

white

solubility

DMSO: 100 mg/mL

shipped in

ambient

storage temp.

−20°C

Quality Level

100

相关类别

Disclaimer

Toxicity: Standard Handling (A)

General description

A cell-permeable pyrazolopyrimidine compound that effectively targets the ATP pocket of both protein tyrosine kinases (IC50<0.26 M against Abl, EGFR, EphB4, Hck, PDGFR, RET, Src, SrcT338I, and VEGFR2) and PI 3-K family kinases (IC50<1.4 M against p110α/ β/ δ/ γ, mTOR, and DNA-PK). PP121 is less effective against ser/thr kinases and exhibits significant inhibition of only 14 ser/thr kinases (≥70% inhibition with 1 M inhibitor and 10 M ATP) in a 219 kinase panel screening. Individually targeting Ret by sorafenib (IC50 = 780 nM) or PI 3-K/mTOR pathway by PI-103 (IC50 = 800 nM) is shown to be less effective than PP121 treatment (IC50 = 50 nM) in inhibiting the proliferation of Ret C634W-expressing TT thyroid carcinoma cultures.

Other Notes

Apsel, B., et al. 2008. Nat. Chem. Biol.4, 691.

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

存储类别

10 - Combustible liquids

wgk

WGK 1

flash_point_f

Not applicable

flash_point_c

Not applicable

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