BIBR 1532

Name: BIBR 1532
Brand: MedChemExpress
SKU: HY-17353
Rating: 5.0 (5 reviews)

Cat. No.: HY-17353 Purity: 99.86%: FAQs
Data Sheet SDS COA Handling Instructions

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BIBR 1532 is a potent, selective and non-competitive telomerase inhibitor with IC₅₀ of 100 nM in a cell-free assay.

For research use only. We do not sell to patients.

BIBR 1532 Chemical Structure

CAS No. : 321674-73-1

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10 mM * 1 mL in DMSO ready for reconstitution	USD 119	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	USD 119	In-stock	Estimated Time of Arrival: December 31
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5 mg	USD 69	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 108	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 248	In-stock	Estimated Time of Arrival: December 31
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Based on 5 publication(s) in Google Scholar

5 Publications Citing Use of MCE BIBR 1532

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Description

BIBR 1532 is a potent, selective and non-competitive telomerase inhibitor with IC₅₀ of 100 nM in a cell-free assay.

IC₅₀ & Target

IC50: 100 nM (telomerase)

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	0.73 μM Compound: BIBR1532	Antiproliferative activity against human A549 cells by CCK8 assay Antiproliferative activity against human A549 cells by CCK8 assay	[PMID: 34922028]
Calu-3	IC₅₀	0.21 μM Compound: BIBR1532	Antiproliferative activity against human Calu-3 cells by CCK8 assay Antiproliferative activity against human Calu-3 cells by CCK8 assay	[PMID: 34922028]
HeLa	IC₅₀	0.012 μM Compound: BIBR1532	Antiproliferative activity against human HeLa cells by CCK8 assay Antiproliferative activity against human HeLa cells by CCK8 assay	[PMID: 34922028]
HeLa	IC₅₀	0.093 μM Compound: 13, BIBR1532	Inhibition of human telomerase isolated from human HeLa cells nuclear extracts expressed in insect cells assessed as [33P]dCMP incorporation after 30 mins by liquid scintillation counting analysis Inhibition of human telomerase isolated from human HeLa cells nuclear extracts expressed in insect cells assessed as [33P]dCMP incorporation after 30 mins by liquid scintillation counting analysis	[PMID: 24053596]
HeLa	IC₅₀	0.093 μM Compound: 2, BIBR-1532	Inhibition of telomerase in human HeLa cells after 2 hrs by [alpha-32P]dGTP incorporation assay Inhibition of telomerase in human HeLa cells after 2 hrs by [alpha-32P]dGTP incorporation assay	[PMID: 22413845]
HeLa	IC₅₀	3.6 μM Compound: 2, BIBR-1532	Inhibition of telomerase in human HeLa cells using 5'-AAT CCG TCG AGC AGA GTT-3' as substrate incubated for 15 mins prior to extension reaction by telomeric repeat amplification protocol Inhibition of telomerase in human HeLa cells using 5'-AAT CCG TCG AGC AGA GTT-3' as substrate incubated for 15 mins prior to extension reaction by telomeric repeat amplification protocol	[PMID: 22413845]
HeLa	IC₅₀	4.6 μM Compound: 2, BIBR-1532	Inhibition of telomerase in human HeLa cells using 5'-AAT CCG TCG AGC AGA GTT-3' as substrate incubated for 15 mins prior to extension reaction followed by compound washout by spin-telomeric repeat amplification protocol Inhibition of telomerase in human HeLa cells using 5'-AAT CCG TCG AGC AGA GTT-3' as substrate incubated for 15 mins prior to extension reaction followed by compound washout by spin-telomeric repeat amplification protocol	[PMID: 22413845]
L02	IC₅₀	80.45 μM Compound: BIBR1532	Cytotoxicity against human L02 cells by CCK8 assay Cytotoxicity against human L02 cells by CCK8 assay	[PMID: 34922028]
MCF7	IC₅₀	0.52 μM Compound: BIBR1532	Antiproliferative activity against human MCF7 cells by CCK8 assay Antiproliferative activity against human MCF7 cells by CCK8 assay	[PMID: 34922028]
MDA-MB-231	IC₅₀	0.17 μM Compound: BIBR1532	Antiproliferative activity against human MDA-MB-231 cells by CCK8 assay Antiproliferative activity against human MDA-MB-231 cells by CCK8 assay	[PMID: 34922028]
MDA-MB-231	IC₅₀	0.17 μM Compound: BIBR1532	Inhibition of telomerase in human MDA-MB-231 cells after 24 hrs by TRAP-PCR-ELISA Inhibition of telomerase in human MDA-MB-231 cells after 24 hrs by TRAP-PCR-ELISA	[PMID: 25965778]
MGC-803	IC₅₀	0.28 μM Compound: BIBR1532	Inhibition of telomerase in human MGC803 cells after 24 hrs by TRAP-PCR-ELISA Inhibition of telomerase in human MGC803 cells after 24 hrs by TRAP-PCR-ELISA	[PMID: 25554922]
MGC-803	IC₅₀	0.28 μM Compound: BIBR1532	Inhibition of telomerase in human MGC803 cell extracts after 24 hrs by TRAP-PCR-ELISA Inhibition of telomerase in human MGC803 cell extracts after 24 hrs by TRAP-PCR-ELISA	[PMID: 24119869]
MGC-803	IC₅₀	0.41 μM Compound: BIBR1532	Inhibition of telomerase in human MGC803 cell extracts after 24 hrs by TRAP-PCR-ELISA Inhibition of telomerase in human MGC803 cell extracts after 24 hrs by TRAP-PCR-ELISA	[PMID: 25812966]
NCI-H1650	IC₅₀	0.52 μM Compound: BIBR1532	Antiproliferative activity against human H1650 cells by CCK8 assay Antiproliferative activity against human H1650 cells by CCK8 assay	[PMID: 34922028]
NCI-H460	IC₅₀	0.39 μM Compound: BIBR1532	Antiproliferative activity against human H460 cells by CCK8 assay Antiproliferative activity against human H460 cells by CCK8 assay	[PMID: 34922028]

In Vitro

BIBR 1532 non-competitively inhibits telomerase activity^[1]. BIBR 1532 inhibits the proliferation of JVM13 leukemia cells with an IC₅₀ of 52 μM, and similar effect also occurs in other leukemia cell lines such as Nalm-1, HL-60, and Jurkat. BIBR 1532 exerts antiproliferative effect on acute myeloid leukemia (AML) with IC₅₀ of 56 μM with no effect on the proliferative capacity of normal hematopoietic progenitor cells^[2]. BIBR 1532 (2.5 μM) reduces colony-forming ability, induces telomere length shortening and causes chemotherapeutic sensitization via inhibiting telomerase activity in MCF-7/WT and melphalan-resistant MCF-7/MlnR cell lines^[3]. BIBR 1532 is cytotoxic in a dose-dependent manner in T-cell prolymphocytic leukemia (T-PLL)^[4]. BIBR 1532 in combination with carboplatin (a chemotherapeutic agent) eliminates ovarian cancer spheroid-forming cells in ES2, SKOV3, and TOV112D cell lines^[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

331.36

Formula

C₂₁H₁₇NO₃

CAS No.

321674-73-1

Appearance

Solid

Color

White to light yellow

SMILES

O=C(O)C1=CC=CC=C1NC(/C=C(C2=CC=C3C=CC=CC3=C2)\C)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL (301.79 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.0179 mL	15.0893 mL	30.1787 mL
5 mM	0.6036 mL	3.0179 mL	6.0357 mL
10 mM	0.3018 mL	1.5089 mL	3.0179 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.54 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (7.54 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.86%

Select Batch:

Data Sheet (280 KB) SDS (392 KB)

COA (248 KB) LCMS (97 KB)

Handling Instructions (2659 KB)

References

[1]. Pascolo E, et al. Mechanism of human telomerase inhibition by BIBR1532, a synthetic, non-nucleosidic drug candidate. J Biol Chem. 2002 May 3;277(18):15566-72. [Content Brief]

[2]. El-Daly H, et al. Selective cytotoxicity and telomere damage in leukemia cells using the telomerase inhibitor BIBR1532. Blood. 2005 Feb 15;105(4):1742-9. [Content Brief]

[3]. Ward RJ, et al. Pharmacological telomerase inhibition can sensitize drug-resistant and drug-sensitive cells to chemotherapeutic treatment. Mol Pharmacol. 2005 Sep;68(3):779-86. [Content Brief]

[4]. A Röth, et al. Short telomeres and high telomerase activity in T-cell prolymphocytic leukemia. Leukemia. 2007 Dec;21(12):2456-62. [Content Brief]

[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 Mar;124(3):598-605. [Content Brief]

Kinase Assay ^[1]	For the direct telomerase assay with the endogenous telomerase, 10 μL of telomerase-enriched extract is mixed with different concentrations of BIBR1532 in a final volume of 20 μL. After 15-minute preincubation on ice, 20 μL of the reaction mixture is added, and the reaction is initiated by transferring the tubes to 37°C. The final concentrations in the reaction mixture are 25 mM Tris-Cl (pH 8.3), 1 mM MgCl₂, 1 mM EGTA, 1 mM dATP, 1 mM dTTP, 6.3 μM cold dGTP, 15 μCi [α-³²P]dGTP (3000 Ci/mmol; NEN), 1.25 mM spermidine, 10 units of RNasin, 5 mM 2-mercaptoethanol, and 2.5 μM TS-primer (5'-AATCCGTCGAGCAGAGTT). For the recombinant enzyme, 1-7 μL of affinity-purified telomerase (containing less than 0.025 μM hTERT) are assayed in a final volume of 40 μL containing 50 mM Tris acetate (pH 8.5), 50 mM KCl, 1 mM MgCl₂, 1 mM spermidine, 5 mM 2-mercaptoethanol, 1 mM dATP, 1 mM dTTP, 2.5 μM dGTP, 15 μCi of [α-³²P]dGTP (3000 Ci/mmol) and 2.5 μM (TTAGGG)3. The reaction is initiated by incubation at 37°C for 2 hours and stopped by addition of 50 μL of RNase mix (0.1 mg/mL RNaseA-100 u/mL RNaseT1 in 10 mM Tris-Cl (pH 8.3) and 20 mm EDTA) and incubation for 20 min at 37°C. Samples are deproteinated by adding 50 μL of 0.3 mg/m proteinase K in 10 mM Tris-Cl (pH 8.3) and 0.5% w/v SDS, for a 30-minute incubation at 37°C. DNA is recovered by phenol extraction and ethanol precipitation, and the extension products are analyzed on an 8% (endogenous telomerase) or 12% (recombinant telomerase) polyacrylamide-urea gel. Dried gels are exposed to a Kodak phosphorimager screen, and the results are analyzed. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay ^[1]	Cells are plated as triplicates in complete RPMI 1640 medium with various concentrations of BIBR1532. After 24 to 72 hours, water-soluble tetrazolium (WST-1) is added, which is transformed into formazan by mitochondrial reductase systems. The increase in the number of viable cells results in an increase of activity of mitochondrial dehydrogenases, leading to an increase of formazan dye formed, which is quantified by ELISA reader after 2, 3, and 4 hours of incubation. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Pascolo E, et al. Mechanism of human telomerase inhibition by BIBR1532, a synthetic, non-nucleosidic drug candidate. J Biol Chem. 2002 May 3;277(18):15566-72. [Content Brief] [2]. El-Daly H, et al. Selective cytotoxicity and telomere damage in leukemia cells using the telomerase inhibitor BIBR1532. Blood. 2005 Feb 15;105(4):1742-9. [Content Brief] [3]. Ward RJ, et al. Pharmacological telomerase inhibition can sensitize drug-resistant and drug-sensitive cells to chemotherapeutic treatment. Mol Pharmacol. 2005 Sep;68(3):779-86. [Content Brief] [4]. A Röth, et al. Short telomeres and high telomerase activity in T-cell prolymphocytic leukemia. Leukemia. 2007 Dec;21(12):2456-62. [Content Brief] [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 Mar;124(3):598-605. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.0179 mL	15.0893 mL	30.1787 mL	75.4466 mL
	5 mM	0.6036 mL	3.0179 mL	6.0357 mL	15.0893 mL
	10 mM	0.3018 mL	1.5089 mL	3.0179 mL	7.5447 mL
	15 mM	0.2012 mL	1.0060 mL	2.0119 mL	5.0298 mL
	20 mM	0.1509 mL	0.7545 mL	1.5089 mL	3.7723 mL
	25 mM	0.1207 mL	0.6036 mL	1.2071 mL	3.0179 mL
	30 mM	0.1006 mL	0.5030 mL	1.0060 mL	2.5149 mL
	40 mM	0.0754 mL	0.3772 mL	0.7545 mL	1.8862 mL
	50 mM	0.0604 mL	0.3018 mL	0.6036 mL	1.5089 mL
	60 mM	0.0503 mL	0.2515 mL	0.5030 mL	1.2574 mL
	80 mM	0.0377 mL	0.1886 mL	0.3772 mL	0.9431 mL
	100 mM	0.0302 mL	0.1509 mL	0.3018 mL	0.7545 mL

BIBR 1532 Related Classifications

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Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BIBR 1532321674-73-1BIBR1532BIBR-1532TelomeraseApoptosisInhibitorinhibitorinhibit

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BIBR 1532

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BIBR 1532 Related Antibodies

5 Publications Citing Use of MCE BIBR 1532

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Complete Stock Solution Preparation Table

BIBR 1532 Related Classifications

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