Oncrasin-1

Modify Date: 2025-08-24 07:07:45

Oncrasin-1 Structure
Oncrasin-1 structure
Common Name Oncrasin-1
CAS Number 75629-57-1 Molecular Weight 269.72600
Density 1.21g/cm3 Boiling Point 465.5ºC at 760 mmHg
Molecular Formula C16H12ClNO Melting Point 117 °C
MSDS USA Flash Point 235.3ºC

 Use of Oncrasin-1


Oncrasin-1 is a potent and effective anticancer inhibitor that kills various human lung cancer cells with K-Ras mutations at low or submicromolar concentrations; also led to abnormal aggregationof PKCι in nucleus of sensitive cells but not in resistant cells.IC50 value: 1.0 μM(A549, K-ras 12H and p53 Wt) [1]Target: human lung cancer cells with K-Ras mutation; K-Ras/PKCiota pathway inhibitorin vitro: effectively kills various human lung cancer cells with K-Ras mutations at low or submicromolar concentrations. The cytotoxic effects correlated with apoptosis inductionas was evidenced by increase of apoptotic cells and activation of caspase-3 and caspase-8 upon the treatment of oncrasin-1 in sensitive cells.Treatment with oncrasin-1 also led to abnormal aggregationof PKCι in nucleus of sensitive cells but not in resistant cells. Furthermore, oncrasin-1 induced apoptosis was blocked by siRNA of K-Ras or PKCι suggesting that oncrasin-1 is targeted to a novel K-Ras/PKCι pathway [1]. oncrasin-1 treatment led to coaggregation of PKCiota and splicing factors into megaspliceosomes but had no obvious effects on the DNA repair molecule Rad51. Moreover, oncrasin-1 treatment suppressed the phosphorylation of the largest subunit of RNA polymerase II and the expression of intronless reporter genes in sensitive cells but not in resistant cells [2]. in vivo: The in vivo administration of oncrasin-1 suppressed the growth of K-ras mutant human lung tumor xenografts by >70% and prolonged the survival of nude mice bearing these tumors, without causing detectable toxicity [1].

 Names

Name 1-[(4-chlorophenyl)methyl]indole-3-carbaldehyde
Synonym More Synonyms

 Oncrasin-1 Biological Activity

Description Oncrasin-1 is a potent and effective anticancer inhibitor that kills various human lung cancer cells with K-Ras mutations at low or submicromolar concentrations; also led to abnormal aggregationof PKCι in nucleus of sensitive cells but not in resistant cells.IC50 value: 1.0 μM(A549, K-ras 12H and p53 Wt) [1]Target: human lung cancer cells with K-Ras mutation; K-Ras/PKCiota pathway inhibitorin vitro: effectively kills various human lung cancer cells with K-Ras mutations at low or submicromolar concentrations. The cytotoxic effects correlated with apoptosis inductionas was evidenced by increase of apoptotic cells and activation of caspase-3 and caspase-8 upon the treatment of oncrasin-1 in sensitive cells.Treatment with oncrasin-1 also led to abnormal aggregationof PKCι in nucleus of sensitive cells but not in resistant cells. Furthermore, oncrasin-1 induced apoptosis was blocked by siRNA of K-Ras or PKCι suggesting that oncrasin-1 is targeted to a novel K-Ras/PKCι pathway [1]. oncrasin-1 treatment led to coaggregation of PKCiota and splicing factors into megaspliceosomes but had no obvious effects on the DNA repair molecule Rad51. Moreover, oncrasin-1 treatment suppressed the phosphorylation of the largest subunit of RNA polymerase II and the expression of intronless reporter genes in sensitive cells but not in resistant cells [2]. in vivo: The in vivo administration of oncrasin-1 suppressed the growth of K-ras mutant human lung tumor xenografts by >70% and prolonged the survival of nude mice bearing these tumors, without causing detectable toxicity [1].
Related Catalog
References

[1]. Guo W, et al. Identification of a small molecule with synthetic lethality for K-ras and protein kinase C iota. Cancer Res. 2008 Sep 15;68(18):7403-8.

[2]. Guo W, et al. Interruption of RNA processing machinery by a small compound, 1-[(4-chlorophenyl)methyl]-1H-indole-3-carboxaldehyde (oncrasin-1). Mol Cancer Ther. 2009 Feb;8(2):441-8.

 Chemical & Physical Properties

Density 1.21g/cm3
Boiling Point 465.5ºC at 760 mmHg
Melting Point 117 °C
Molecular Formula C16H12ClNO
Molecular Weight 269.72600
Flash Point 235.3ºC
Exact Mass 269.06100
PSA 22.00000
LogP 4.15550
Index of Refraction 1.62
InChIKey ZDRQMXCSSAPUMM-UHFFFAOYSA-N
SMILES O=Cc1cn(Cc2ccc(Cl)cc2)c2ccccc12

 Safety Information

Hazard Codes Xi
RIDADR NONH for all modes of transport
HS Code 2933990090

 Synthetic Route

~86%

Oncrasin-1 Structure

Oncrasin-1

CAS#:75629-57-1

Literature: Na, Young-Min; Le Borgne, Marc; Pagniez, Fabrice; Le Baut, Guillaume; Le Pape, Patrice European Journal of Medicinal Chemistry, 2003 , vol. 38, # 1 p. 75 - 87

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Oncrasin-1 Structure

Oncrasin-1

CAS#:75629-57-1

Literature: Chemical and Pharmaceutical Bulletin, , vol. 28, # 6 p. 1711 - 1721

~64%

Oncrasin-1 Structure

Oncrasin-1

CAS#:75629-57-1

Literature: Costi, Roberta; Cuzzucoli Crucitti, Giuliana; Pescatori, Luca; Messore, Antonella; Scipione, Luigi; Tortorella, Silvano; Amoroso, Alessandra; Crespan, Emmanuele; Campiglia, Pietro; Maresca, Bruno; Porta, Amalia; Granata, Ilaria; Novellino, Ettore; Gouge, Jeroime; Delarue, Marc; Maga, Giovanni; Di Santo, Roberto Journal of Medicinal Chemistry, 2013 , vol. 56, # 18 p. 7431 - 7441

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Oncrasin-1 Structure

Oncrasin-1

CAS#:75629-57-1

Literature: US5229505 A1, ;

~86%

Oncrasin-1 Structure

Oncrasin-1

CAS#:75629-57-1

Literature: Moriya, Tamon; Hagio, Katsuaki; Yoneda, Naoto Chemical and Pharmaceutical Bulletin, 1980 , vol. 28, # 6 p. 1711 - 1721

~%

Oncrasin-1 Structure

Oncrasin-1

CAS#:75629-57-1

Literature: Bulletin of the Korean Chemical Society, , vol. 32, # 1 p. 307 - 310

~%

Oncrasin-1 Structure

Oncrasin-1

CAS#:75629-57-1

Literature: Chemical and Pharmaceutical Bulletin, , vol. 28, # 6 p. 1711 - 1721

 Customs

HS Code 2933990090
Summary 2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

 Synonyms

Oncrasin 1
1-(4-Chlorobenzyl)-1H-indole-3-carbaldehyde
Oncrasin-1
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