Cellagen Technology LLC
 
작성일 : 16-10-12
[Cellagen Technology LLC] Disease Area, Oncology III
Adriamycin (Doxorubicin) l DNA intercalator / AG-014699 (PF-01367338, Rucaparib) l PARP1/2 inhibitor / AG-1024 l IGF-1R inhibitor / AGI-5198 (IDH-C35) | IDH1 inhibitor

 

Disease Area, Oncology III

 

 

Product Name: Adriamycin (Doxorubicin) l DNA intercalator (#C2374)

 

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Adriamycin (Doxorubicin) is an intravenous, anthracycline-based antibiotic and antineoplastic agent derived

from Streptomyces bacterium. Adriamycin enters cancer cell DNA and inhibits cell replication by arresting

protein synthesis.

In HK-2 cells, adriamycin decreases cell viability in a dose-dependent manner and induces an increase in

cells in the sub G1 and G2/M phases. It also increases secretion of TNFa, decreases expression of

phosphorylated PKA and Bcl-2, and increases phosphoryled signal transducer and activator of transcription

3, phospho-ERK,and ATF3. [1]

Due to adriamycin's route of administration and cytotoxic effects, extensive research has been conducted in

the area of assisted delivery of the chemotherapeutic (liposome [2], prodrug [3], polymer, gold-particles,

etc.)

 

Details

Chemical Formula:

 

C27H29NO11.HCl

CAS No.:

 

25316-40-9

Molecular weight:

 

579.88

Purity:

> 98%

Appearance:

 

Red Orange

Chemical name:

  

  

 

(8S,10S)-10-((2R,4S,5S,6S)-4-amino-5-hydroxy-6-methyl-tetrahydro-2H-pyran-2-

yloxy)-6,8,11-trihydroxy-8-(2-hydroxyacetyl)-1-methoxy-7,8,9,10-

tetrahydrotetracene-5,12-dione hydrochloride

Solubility:

 

Up to 100 mM in DMSO

Synonyms:

  

 

Adriablastin, Adriblastin, Adriblastina, Adriamycin, Doxorubicine, Rubex,

Doxorubicinum, Doxorubicina, Doxil

Storage:

  

For longer shelf life, store solid powder at 4oC desiccated, or DMSO solution

at -20oC

 

References

1. Park et al., Doxorubicin induces cytotoxicity through upregulation of pERK-dependent ATF3. PLoSONE,

   2012, 7(9), e44990. Pubmed ID: 23028726   

2. Macmillan and Cancer Backup factsheet

3. Albright et al., Matrix metalloproteinase-activated doxorubicin prodrugs inhibit HT1080 xenograft growth

   better than doxorubicin with less toxicity. Mol. Cancer Ther. 2005, 4, 751-760. Pubmed ID: 15897239

 

 

Product Name: AG-014699 (PF-01367338, Rucaparib) l PARP1/2 inhibitor (#C2401)

 

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AG-014699 (Rucaparib) is an intraveneously-administered, azepinone-indole-based inhibitor of PARP 1 and

2 (Ki = 1.4 nM) [1] AG-014699 induces selective cytotoxicity in tumor cells defective in homologous

recombination repair (HRR) through BRCA1 and 2 mutation and non-BRCA mutated HRR defects. It is a potent

chemosensitizer of temozolomide (3 to 10 fold) and topotecan (1.5 to 2.3 fold) antitumor activity in

neuroblastoma cells. [2, 3]

 

Details

Chemical Formula:

 

C19H18FN3O.O3PO4

CAS No.:

 

459868-92-9

Molecular weight:

 

421.36

Purity:

> 98%

Appearance:

 

Yellow

Chemical name:

   

 

8-Fluoro-2-(4-methylaminomethyl-phenyl)-1,3,4,5-tetrahydro-azepino[5,4,3-cd]

indol-6-one phosphate

Solubility:

 

Up to 100 mM in DMSO

Synonyms:

  

 

AG-014699, AG014699, AG-14699, AG14699, AG-014447, PF-01367338, PF01367338,

Rucaparib phosphate, Rucaparib

Storage:

  

For longer shelf life, store solid powder at 4oC desiccated, or DMSO solution

at -20oC

 

References

1."Phase II trial of the Poly(ADP-ribose) polymerase (PARP) inhibitor AG-014699 in BRCA1 and 2 mutated

   advanced ovarian and breast cancer" Cancer Research UK / Newcastle Univ. Abstract 3104

2. Thomas et al., Preclinical selection of a novel poly(ADP-ribose) polymerase inhibitor for clinical trial. Mol.

   Cancer. Ther. 2007, 6(3), 945-956. Pubmed ID: 17363489   

3. Daniel et al., Inhibition of poly(ADP-ribose) polymerase-1 enhances temozolomide and topotecan activity

   against childhood neuroblastoma. Clin. Cancer Res. 2009, 15(4), 1241-1249. Pubmed ID: 19174487

 

 

Product Name: AG-1024 | IGF-1R inhibitor (#C2102)

 

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AG-1024 is a selective IGF-1R kinase inhibitor with modest activity. It inhibits insulin-stimulated cellular

proliferation with IC50 of 0.4 µM. [1] AG-1024 showed synergistic effect with irradation and inhibited

proliferation and induced apoptosis in human breast cancer MCF-7 cells. [2] AG-1024 also inhibited

autocrine growth of human prostate cancer DU145 cells with an IC50 value of 2.5 µM.[3]

In vivo, daily administration of AG-1024 through i.v. route at 1-2 mg/kg has been shown to increase the

survival rate of mouse injected with Ba/F3-p210 cells. [4]

 

Details

Chemical Formula:

 

C14H13BrN2O

CAS No.:

 

65678-07-1

Molecular weight:

 

305.17

Purity:

> 98%

Appearance:

 

Orange

Chemical name:

 

2-(3-bromo-5-(tert-butyl)-4-hydroxybenzylidene)malononitrile

Solubility:

 

Up to 100 mM in DMSO

Synonyms:

 

AG1024, AG 1024, Tyrphostin AG-1024,

Storage:

 

For longer shelf life, store solid powder or DMSO solution at -20oC desiccated

 

References

1. Párrizas M, et al. Specific inhibition of insulin-like growth factor-1 and insulin receptor tyrosine kinase

   activity and biological function by tyrphostins. Endocrinology. 1997; 138(4):1427-33. Pubmed ID: 9075698

2. Wen B, et al. Tyrphostin AG 1024 modulates radiosensitivity in human breast cancer cells. Br J Cancer.

   2001; 85(12):2017-21. Pubmed ID: 11747348

3. Kisielewska J, et al. The effect of tyrosine kinase inhibitors, tyrphostins: AG1024 and SU1498, on autocrine

   growth of prostate cancer cells (DU145). Folia Histochem Cytobiol. 2008; 46(2):185-91. Pubmed ID: 18519236

4. Deutsch E, et al. Tyrosine kinase inhibitor AG1024 exerts antileukaemic effects on STI571-resistant Bcr-

   Abl expressing cells and decreases AKT phosphorylation. Br J Cancer. 2004; 91(9):1735-41.

   Pubmed ID: 11747348

 

 

Product Name: AGI-5198 (IDH-C35) | IDH1 inhibitor (#C2519)

 

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AGI-5198 (IDH-C35) is a potent and selective isocitrate dehydrogenase 1 (IDH1) inhibitor specifically against

R132H/C mutants (mIDH1) with IC50 at 100 nM range. AGI-5198 does not inhibit wild-type IDH1 or any of the

examined IDH2 isoforms (IC50 > 100 µM).[1] AGI-5198 inhibits R-2-hydroxyglutarate (R-2HG) production by

mIDH1. AGI-5198 also induces demethylation of histone H3K9me3 and expression of genes associated with

gliogenic differentiation.

In both in vitro and in vivo studies, AGI-5198 inhibited the growth of glioma cells carrying mutated but not wild

type IDH1, yet with no appreciable changes in genome-wide DNA methylation. These data suggest that

mIDH1 may promote glioma growth through mechanisms beyond its well-characterized epigenetic effects.

AGI-5198 could serve as a very useful chemical tool to probe the mechanism and treatment of mIDH1-

carrying tumors

 

Details

Chemical Formula:

 

C27H31FN4O2

CAS No.:

 

1355326-35-0

Molecular weight:

 

462.56

Purity:

> 98%

Appearance:

 

White

Chemical name:

  

 

N-cyclohexyl-2-(N-(3-fluorophenyl)-2-(2-methyl-1H-imidazol-1-yl)acetamido)-2-(o-tolyl)acetamide

Solubility:

 

Up to 25 mM in DMSO

Synonyms:

 

AGl-5198, AGI5198, lDH-C35

Storage:

For longer shelf life, store solid powder or DMSO solution at -20oC desiccated

 

Reference

1. Rohle D, et al. An inhibitor of mutant IDH1 delays growth and promotes differentiation of glioma cells.

   Science. 2013; 340(6132):626-30. Pubmed ID:23558169

 



Ordering informations

    

Catalog No.

Product Name

Size

C2374

Adriamycin (Doxorubicin) l DNA intercalator

5 mg, 25 mg & 100 mg

C2401

AG-014699 (PF-01367338, Rucaparib) l PARP1/2 inhibitor

5 mg, 25 mg & 100 mg

C2102

AG-1024 l IGF-1R inhibitor

5 mg, 25 mg & 100 mg

C2519

AGI-5198 (IDH-C35) | IDH1 inhibitor

2 mg, 25 mg & 100 mg

 


 

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