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Cat. No. Name Size Price Add Cart
KI3340BIBR 153210 mg$200

Chemical Characteristic

Product NameBIBR 1532
CAS No.321674-73-1
Molecular Weight 331.36
FormulaC21H17NO3
Chemical Name2-[[(2E)-3-(2-Naphthalenyl)-1-oxo-2 -butenyl1-yl]amino]benzoic acid
SmilesC(=O)(c1c(cccc1)NC(=O)/C=C(\C)/c1cc2c(cc1)cccc2)O
Chemical Structure

Biological activities

BIBR 1532 is a potent and selective telomerase inhibitor with an IC50 of 100 nM. Using enzyme-kinetic experiments, BIBR 1532 is showed to be a mixed-type non-competitive inhibitor and has a drug binding site distinct from the sites for deoxyribonucleotides and the DNA primer, respectively.[1] In the p53-deficient HT1080, MDA-MB231, and DU145 in vitro, BIBR 1532 treatment causes progressive telomere shortening with no acute cytotoxicity, but leads to a proliferation arrest after a characteristic lag period with hallmarks of senescence, including morphological, mitotic and chromosomal aberrations and altered patterns of gene expression.[2] In short-term culture assays in vitro, BIBR 1532 (30-80 µ M) shows dose-dependent direct cytotoxicity in different leukemia cell lines and primary cells from patients with acute myeloid leukemia (AML) and chronic lymphocytic leukemia (CLL).[3] Moreover, BIBR 1532 treatment also leads to progressive telomere shortening, decreases proliferative capacity, and sensitizes drug-resistant and drug-sensitive cells to chemotherapeutic treatment in leukemia and breast cancer cells in vitro.[4] BIBR 1532 in combination with carboplatin shows synergy in eliminating ovarian cancer spheroid-forming cells in vitro.[5]

Protocols

In vitro: BIBR 1532 is dissolved in 0.1% DMSO.[2]

References

[1] Sun L, et al. Design, synthesis, and evaluations of substituted 3-[(3- or 4-carboxyethylpyrrol-2-yl)methylidenyl]indolin-2-ones as inhibitors of VEGF, FGF, and PDGF receptor tyrosine kinases. J Med Chem. 1999, 42(25): 5120-5130.
[2] Damm K, et al. A highly selective telomerase inhibitor limiting human cancer cell proliferation. EMBO J. 2001, 20(24): 6958-6968.
[3] El-Daly H, et al. Selective cytotoxicity and telomere damage in leukemia cells using the telomerase inhibitor BIBR1532. Blood. 2005, 105(4): 1742-1749.
[4] Ward RJ, et al. Pharmacological telomerase inhibition can sensitize drug-resistant and drug-sensitive cells to chemotherapeutic treatment. Mol Pharmacol. 2005, 68(3): 779-786.
[5] Meng E, et al. Targeted inhibition of telomerase activity combined with chemotherapy demonstrates synergy in eliminating ovarian cancer spheroid-forming cells. Gynecol Oncol. 2012, 124(3): 598-605.

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KareBayTM provides scientists and clinicians with a wide range of biotechnological products and science lab supplies for chemical research and analyzing life processes. KareBay's extensive capabilities include commercializing reagents and kits, manufacturing biotech products and providing contract research services to organizations worldwide. Our many global labs, offices, and business partners enable KareBay to extend its products and services to its customer base around the world.

Our products are used for research, laboratory and further evaluation purposes. They are not for human use.
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