CAS 75629-57-1|Oncrasin-1

Introduction：Basic information about CAS 75629-57-1|Oncrasin-1, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. Oncrasin-1 BiologicalActivity
3. Chemical & Physical Properties
4. Safety Information
5. Customs
6. Synonyms

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

Names

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

Oncrasin-1 BiologicalActivity

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	Signaling Pathways >>GPCR/G Protein >>RasResearch Areas >>Cancer
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.

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

Signaling Pathways >>GPCR/G Protein >>RasResearch Areas >>Cancer

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

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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