Pamiparib (Synonyms: BGB-290)

Name: Pamiparib
Brand: MedChemExpress
SKU: HY-104044
Rating: 5.0 (3 reviews)

製品番号: HY-104044 純度: 99.96%: Data Sheet SDS COA 取扱説明書
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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.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

Pamiparib 構造式

CAS 番号 : 1446261-44-4

容量	価格（税別）	在庫状況	数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 108	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 108	在庫あり	Estimated Time of Arrival: December 31
Solid
5 mg	$99	在庫あり	Estimated Time of Arrival: December 31
10 mg	$165	在庫あり	Estimated Time of Arrival: December 31
25 mg	$275	在庫あり	Estimated Time of Arrival: December 31
50 mg	$495	在庫あり	Estimated Time of Arrival: December 31
100 mg	$825	在庫あり	Estimated Time of Arrival: December 31
200 mg		お問い合わせ
500 mg		お問い合わせ

or バルクお問い合わせ

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 3 publication(s) in Google Scholar

Other Forms of Pamiparib:

Pamiparib maleate お問い合わせ
Pamiparib (Standard) お問い合わせ

顧客検証

PARP アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

生物活性
純度とドキュメンテーション
参考文献
カスタマーレビュー

製品説明

IC₅₀ & Target^[1]

PARP

Cellular Effect

Cell Line	Type	Value	Description	References
MDA-MB-436	EC₅₀	10.6 1 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]
HCC1395	EC₅₀	42.5 1 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]
HCC1395	EC₅₀	42.5 1 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 1 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]
HCC1395	EC₅₀	42.5 1 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 1 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-231	EC₅₀	>10 3 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 1 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]
MDA-MB-436	EC₅₀	10.6 1 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	>10 3 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]
SK-BR-3	EC₅₀	> 10000 1 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]
SK-BR-3	EC₅₀	> 10000 1 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]

体外実験

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.

体内実験

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.

臨床実験

分子量

298.32

分子式

C₁₆H₁₅FN₄O

CAS 番号

1446261-44-4

Appearance

Solid

Color

Light yellow to yellow

SMILES

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

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶剤 & 溶解度

体外:

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

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.

Molarity Calculator
Dilution Calculator

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

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

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

体内:

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: ≥ 2.25 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.

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.

純度とドキュメンテーション

純度: 99.96%

Select Batch:

データシート (281 KB) SDS (393 KB)

COA (257 KB) HNMR (208 KB) RP-HPLC (291 KB) MS (68 KB)

取扱説明書 (2659 KB)

参考文献

[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

Complete Stock Solution Preparation Table

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

Pamiparib Related Classifications

Molarity Calculator
Dilution Calculator

The molarity calculator equation

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

質量		濃度		体積		分子量 *
	=		×		×

The dilution calculator equation

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

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）	×	体積 _（開始）	=	濃度 _（終了）	×	体積 _（終了）
	×		=		×
C1		V1		C2		V2

Help & FAQs

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:

Pamiparib1446261-44-4BGB-290BGB290BGB 290PARPpoly ADP ribose polymeraseInhibitorinhibitorinhibit

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Pamiparib (Synonyms: BGB-290)

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Other Forms of Pamiparib:

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PARP アイソフォーム固有の製品をすべて表示:

生物活性

純度とドキュメンテーション

参考文献

カスタマーレビュー

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Pamiparib Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

Keywords:

最近チェックした製品:

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Pamiparib (Synonyms: BGB-290)

カスタマーレビュー

Other Forms of Pamiparib:

Pamiparib 関連抗体

顧客検証

おすすめ

•関連スクリーニングライブラリ:

•関連小分子:

•関連タンパク質:

PARP アイソフォーム固有の製品をすべて表示:

生物活性

純度とドキュメンテーション

参考文献

カスタマーレビュー

Pamiparib 関連抗体

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Pamiparib Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

Keywords:

最近チェックした製品:

カスタマーレビュー

Request for HNMR Report

Request for HNMR Report