Art. -Nr.: HY-104044

Pamiparib

(Synonyms: BGB-290)

3 Cited Publications

Kundenbewertung

Based on 3 publication(s) in Google Scholar

Pamiparib (BGB-290) is an orally active, potent, highly selective PARP inhibitor, with IC₅₀ values of 0.9 nM and 0.5 nM for PARP1 and PARP2, respectively. Pamiparib has potent PARP trapping, and capability to penetrate the brain, and can be used for the research of various cancers including the solid tumor.

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Reinheit: 99.96%
CAS. Nr.: 1446261-44-4
Formel: C₁₆H₁₅FN₄O
Molecular Weight:298.32

Speicherung:

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

Pamiparib Chemical Structure

CAS. Nr.: 1446261-44-4

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (3)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

PARP

Alle PARP Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HCC1395	EC₅₀	42.5 nM Compound: 139; BGB-290	Antiproliferation activity against human HCC1395 cells expressing BRCA1 mutant incubated for 7 days by CellTiter-Glo luminescent cell viability assay Antiproliferation activity against human HCC1395 cells expressing BRCA1 mutant incubated for 7 days by CellTiter-Glo luminescent cell viability assay	[PMID: 33264017]
MDA-MB-231	EC₅₀	>10000 nM Compound: 139; BGB-290	Antiproliferation activity against human MDA-MB-231 cells incubated for 7 days by CellTiter-Glo luminescent cell viability assay Antiproliferation activity against human MDA-MB-231 cells incubated for 7 days by CellTiter-Glo luminescent cell viability assay	[PMID: 33264017]
MDA-MB-436	EC₅₀	10.6 nM Compound: 139; BGB-290	Antiproliferation activity against human MDA-MB-436 cells expressing BRCA1 mutant incubated for 7 days by CellTiter-Glo luminescent cell viability assay Antiproliferation activity against human MDA-MB-436 cells expressing BRCA1 mutant incubated for 7 days by CellTiter-Glo luminescent cell viability assay	[PMID: 33264017]
SK-BR-3	EC₅₀	>10000 nM Compound: 139; BGB-290	Antiproliferation activity against human SK-BR-3 cells incubated for 7 days by CellTiter-Glo luminescent cell viability assay Antiproliferation activity against human SK-BR-3 cells incubated for 7 days by CellTiter-Glo luminescent cell viability assay	[PMID: 33264017]

In Vitro

Pamiparib shows potent DNA-trapping activity with an IC₅₀ of 13 nM. In the cellular assays, Pamiparib inhibits intracellular PAR formation with an IC₅₀ of 0.24 nM. Tumor cell lines with homologous recombination defects are profoundly sensitive to Pamiparib. Pamiparib is highly active both in vitro and in vivo in BRCA mutant tumors^[3].

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

In Vivo

Pamiparib suppresses PARP activity in patient-derived glioblastoma multiforme and small-cell-lung cancer xenografts, and potentiates the effects of Temozolamide. In vivo activities of Pamiparib, and its combination activity with chemotherapies in patient biopsy derived small cell lung cancer (SCLC) xenograft models^[4].

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 1446261-44-4
Appearance Solid
Molecular Weight 298.32
Formel C₁₆H₁₅FN₄O
Color Light yellow to yellow
SMILES

O=C1NN=C2CN(CCC3)[C@@]3(C)C(N4)=C2C5=C4C=C(F)C=C51
Synonyms

BGB-290
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Publications (3)

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Journal Impact Factor

Nature

The molecular landscape of ETMR at diagnosis and relapse. [Abstract]

2019 Dec;576(7786):274-280. PMID: 31802000
Neoplasia

Targeting BARD1 suppresses a Myc-dependent transcriptional program and tumor growth in pancreatic ductal adenocarcinoma. [Abstract]

2025 May:63:101152. PMID: 40096771
bioRxiv

April 22, 2021.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 50 mg/mL (167.60 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.3521 mL

16.7605 mL

33.5209 mL

5 mM

0.6704 mL

3.3521 mL

6.7042 mL

10 mM

0.3352 mL

1.6760 mL

3.3521 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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: ≥ 2.25 mg/mL (7.54 mM); Clear solution

This protocol yields a clear solution of ≥ 2.25 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.5 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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Changyou Zhou, et al. Fused tetra or penta-cyclic dihydrodiazepinocarbazolones as parp inhibitors. WO 2013097225 A1.

[2]. Friedlander M, et al. Pamiparib in combination with tislelizumab in patients with advanced solid tumours: results from the dose-escalation stage of a multicentre, open-label, phase 1a/b trial. Lancet Oncol. 2019 Sep;20(9):1306-1315. [Content Brief]

[3]. Zhiyu Tang, et al. Abstract 1653: BGB-290: A highly potent and specific PARP1/2 inhibitor potentiates anti-tumor activity of chemotherapeutics in patient biopsy derived SCLC models. Cancer Research. August 2015, Volume 75, Issue 15.

[4]. Shiv K. Gupta, et al. Abstract 3505: Inhibition of PARP activity by BGB-290 potentiates efficacy of NSC 362856 in patient derived xenografts of glioblastoma multiforme. Cancer Research. August 2015, Volume 75, Issue 15

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.3521 mL	16.7605 mL	33.5209 mL	83.8023 mL
	5 mM	0.6704 mL	3.3521 mL	6.7042 mL	16.7605 mL
	10 mM	0.3352 mL	1.6760 mL	3.3521 mL	8.3802 mL
	15 mM	0.2235 mL	1.1174 mL	2.2347 mL	5.5868 mL
	20 mM	0.1676 mL	0.8380 mL	1.6760 mL	4.1901 mL
	25 mM	0.1341 mL	0.6704 mL	1.3408 mL	3.3521 mL
	30 mM	0.1117 mL	0.5587 mL	1.1174 mL	2.7934 mL
	40 mM	0.0838 mL	0.4190 mL	0.8380 mL	2.0951 mL
	50 mM	0.0670 mL	0.3352 mL	0.6704 mL	1.6760 mL
	60 mM	0.0559 mL	0.2793 mL	0.5587 mL	1.3967 mL
	80 mM	0.0419 mL	0.2095 mL	0.4190 mL	1.0475 mL
	100 mM	0.0335 mL	0.1676 mL	0.3352 mL	0.8380 mL

Keywords

Pamiparib

3 Cited Publications

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Pamiparib

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Publications Citing Use of MedChemExpress (MCE) Pamiparib

Alle PARP Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (3)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Pamiparib Related Classifications

HY-104044 Related Classifications