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.)
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Details
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Chemical Formula:
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C27H29NO11.HCl
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CAS No.:
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25316-40-9
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Molecular weight:
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579.88
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Purity:
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> 98%
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Appearance:
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Red Orange
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Chemical name:
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(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
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Solubility:
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Up to 100 mM in DMSO
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Synonyms:
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Adriablastin, Adriblastin, Adriblastina, Adriamycin, Doxorubicine, Rubex,
Doxorubicinum, Doxorubicina, Doxil
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Storage:
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For longer shelf life, store solid powder at 4oC desiccated, or DMSO solution
at -20oC
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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
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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]
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Details
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Chemical Formula:
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C19H18FN3O.O3PO4
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CAS No.:
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459868-92-9
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Molecular weight:
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421.36
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Purity:
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> 98%
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Appearance:
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Yellow
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Chemical name:
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8-Fluoro-2-(4-methylaminomethyl-phenyl)-1,3,4,5-tetrahydro-azepino[5,4,3-cd]
indol-6-one phosphate
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Solubility:
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Up to 100 mM in DMSO
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Synonyms:
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AG-014699, AG014699, AG-14699, AG14699, AG-014447, PF-01367338, PF01367338,
Rucaparib phosphate, Rucaparib
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Storage:
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For longer shelf life, store solid powder at 4oC desiccated, or DMSO solution
at -20oC
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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
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Product Name: AG-1024 | IGF-1R inhibitor (#C2102)
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]
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Details
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Chemical Formula:
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C14H13BrN2O
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CAS No.:
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65678-07-1
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Molecular weight:
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305.17
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Purity:
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> 98%
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Appearance:
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Orange
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Chemical name:
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2-(3-bromo-5-(tert-butyl)-4-hydroxybenzylidene)malononitrile
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Solubility:
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Up to 100 mM in DMSO
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Synonyms:
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AG1024, AG 1024, Tyrphostin AG-1024,
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Storage:
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For longer shelf life, store solid powder or DMSO solution at -20oC desiccated
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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
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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
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Details
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Chemical Formula:
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C27H31FN4O2
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CAS No.:
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1355326-35-0
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Molecular weight:
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462.56
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Purity:
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> 98%
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Appearance:
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White
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Chemical name:
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N-cyclohexyl-2-(N-(3-fluorophenyl)-2-(2-methyl-1H-imidazol-1-yl)acetamido)-2-(o-tolyl)acetamide
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Solubility:
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Up to 25 mM in DMSO
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Synonyms:
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AGl-5198, AGI5198, lDH-C35
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Storage:
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For longer shelf life, store solid powder or DMSO solution at -20oC desiccated
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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
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