Oncrasin-1
Names
[ CAS No. ]:
75629-57-1
[ Name ]:
Oncrasin-1
[Synonym ]:
Oncrasin 1
1-(4-Chlorobenzyl)-1H-indole-3-carbaldehyde
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]
[Related Small Molecules]
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
MSDS
Safety Information
[ Hazard Codes ]:
Xi
[ RIDADR ]:
NONH for all modes of transport
[ HS Code ]:
2933990090
Synthetic Route
Precursor & DownStream
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%