CAS 221243-82-9|1-Naphthyl PP1

Introduction：Basic information about CAS 221243-82-9|1-Naphthyl PP1, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. 1-Naphthyl PP1 BiologicalActivity
3. Chemical & Physical Properties
4. Synonyms

Common Name	1-Naphthyl PP1
CAS Number	221243-82-9	Molecular Weight	317.388
Density	1.3±0.1 g/cm3	Boiling Point	527.8±45.0 °C at 760 mmHg
Molecular Formula	C₁₉H₁₉N₅	Melting Point	219-222ºC
MSDS	/	Flash Point	273.0±28.7 °C

Names

Name	1-na-pp1
Synonym	More Synonyms

1-Naphthyl PP1 BiologicalActivity

Description	1-Naphthyl PP1(1-NA-PP 1) is a selective inhibitor of src family kinases v-Src and c-Fyn as well as the tyrosine kinase c-Abl (IC50 values are 1.0, 0.6, 0.6, 18 and 22 μM for v-Src, c-Fyn, c-Abl, CDK2 and CAMK II respectively).IC50 Value:1.0 uM (v-Src); 0.6 uM (c-Fyn); 18 uM (c-Abl) [1]Target: Src Family kinase1-NA-PP1 was considerably more potent and showed distinct substituent effects at the pyrazolopyrimidine core. 1-NA-PP1 was cell-active, and potently blocked prostate cancer cell proliferation by inducing G2/M arrest. Overexpression of PKD1 or PKD3 almost completely reversed the growth arrest and the inhibition of tumor cell invasion caused by 1-NA-PP1, indicating that its anti-proliferative and anti-invasive activities were mediated through the inhibition of PKD. Interestingly, a 12-fold increase in sensitivity to 1-NA-PP1 could be achieved by engineering a gatekeeper mutation in the active site of PKD1, suggesting that 1-NA-PP1 could be paired with the analog-sensitive PKD1(M659G) for dissecting PKD-specific functions and signaling pathways in various biological systems [2].
Related Catalog	Signaling Pathways >>Protein Tyrosine Kinase/RTK >>SrcResearch Areas >>Cancer
References	[1]. Bishop AC, et al. A chemical switch for inhibitor-sensitive alleles of any protein kinase. Nature. 2000 Sep 21;407(6802):395-401. [2]. Tandon M, et al. New pyrazolopyrimidine inhibitors of protein kinase d as potent anticancer agents for prostate cancer cells. PLoS One. 2013 Sep 23;8(9):e75601.

Description

1-Naphthyl PP1(1-NA-PP 1) is a selective inhibitor of src family kinases v-Src and c-Fyn as well as the tyrosine kinase c-Abl (IC50 values are 1.0, 0.6, 0.6, 18 and 22 μM for v-Src, c-Fyn, c-Abl, CDK2 and CAMK II respectively).IC50 Value:1.0 uM (v-Src); 0.6 uM (c-Fyn); 18 uM (c-Abl) [1]Target: Src Family kinase1-NA-PP1 was considerably more potent and showed distinct substituent effects at the pyrazolopyrimidine core. 1-NA-PP1 was cell-active, and potently blocked prostate cancer cell proliferation by inducing G2/M arrest. Overexpression of PKD1 or PKD3 almost completely reversed the growth arrest and the inhibition of tumor cell invasion caused by 1-NA-PP1, indicating that its anti-proliferative and anti-invasive activities were mediated through the inhibition of PKD. Interestingly, a 12-fold increase in sensitivity to 1-NA-PP1 could be achieved by engineering a gatekeeper mutation in the active site of PKD1, suggesting that 1-NA-PP1 could be paired with the analog-sensitive PKD1(M659G) for dissecting PKD-specific functions and signaling pathways in various biological systems [2].

Related Catalog

Signaling Pathways >>Protein Tyrosine Kinase/RTK >>SrcResearch Areas >>Cancer

References

[1]. Bishop AC, et al. A chemical switch for inhibitor-sensitive alleles of any protein kinase. Nature. 2000 Sep 21;407(6802):395-401.

[2]. Tandon M, et al. New pyrazolopyrimidine inhibitors of protein kinase d as potent anticancer agents for prostate cancer cells. PLoS One. 2013 Sep 23;8(9):e75601.

Chemical & Physical Properties

Density	1.3±0.1 g/cm3
Boiling Point	527.8±45.0 °C at 760 mmHg
Melting Point	219-222ºC
Molecular Formula	C₁₉H₁₉N₅
Molecular Weight	317.388
Flash Point	273.0±28.7 °C
Exact Mass	317.164032
PSA	69.62000
LogP	3.88
Vapour Pressure	0.0±1.4 mmHg at 25°C
Index of Refraction	1.688
InChIKey	XSHQBIXMLULFEV-UHFFFAOYSA-N
SMILES	CC(C)(C)n1nc(-c2cccc3ccccc23)c2c(N)ncnc21
Storage condition	2-8℃

Synonyms

1-(2-Methyl-2-propanyl)-3-(1-naphthyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine

1-tert-butyl-3-naphthalen-1-ylpyrazolo[3,4-d]pyrimidin-4-amine

4-Amino-1-tert-butyl-3-(1,-naphthyl)pyrazolo[3,4-d]pyrimidine

1-NA-PP1

1H-Pyrazolo[3,4-d]pyrimidin-4-amine, 1-(1,1-dimethylethyl)-3-(1-naphthalenyl)-

1-tert-butyl-3-(1-naphthyl)-1h-pyrazolo[3,4-d]pyrimidin-4-amine

1-Naphthyl PP1

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