BMS-536924

Name: BMS-536924
Brand: MedChemExpress
SKU: HY-10262
Rating: 5.0 (6 reviews)

製品番号: HY-10262 純度: 99.83%: Data Sheet SDS COA 取扱説明書
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BMS-536924 is an orally active, competitive and selective insulin-like growth factor receptor (IGF-1R) kinase and insulin receptor (IR) inhibitor with IC₅₀s of 100 nM and 73 nM, respectively. BMS-536924 has anti-cancer activity.

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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。

BMS-536924 構造式

CAS 番号 : 468740-43-4

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 97	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 97	在庫あり	Estimated Time of Arrival: December 31
Solid
1 mg	$43	在庫あり	Estimated Time of Arrival: December 31
5 mg	$92	在庫あり	Estimated Time of Arrival: December 31
10 mg	$158	在庫あり	Estimated Time of Arrival: December 31
50 mg	$686	在庫あり	Estimated Time of Arrival: December 31
100 mg	$800	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

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* 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.

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Based on 6 publication(s) in Google Scholar

Other Forms of BMS-536924:

BMS-536924 (Standard) お問い合わせ

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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:

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製品説明

IC₅₀ & Target

IC50: 100 nM (IGF-1R) and 73 nM (IR)^[1]^[2]

Cellular Effect

Cell Line	Type	Value	Description	References
COLO 205	IC₅₀	212 nM Compound: 20, BMS-536924	Cytotoxicity against human COLO205 cells Cytotoxicity against human COLO205 cells	[PMID: 19610618]
COLO 205	IC₅₀	212 nM Compound: 3, BMS-536924	In vitro inhibitory concentration against COLO 205 (colon) cell line with ATP concentration at 1/2Km In vitro inhibitory concentration against COLO 205 (colon) cell line with ATP concentration at 1/2Km	[PMID: 16134929]
LS174T	IC₅₀	2.05 μM Compound: BMS-536924	Antiproliferative activity against human LS 174T cells after 48 hrs by MTT assay Antiproliferative activity against human LS 174T cells after 48 hrs by MTT assay	[PMID: 25648298]
MCF7	IC₅₀	1.748 μM Compound: BMS-536924	Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay	[PMID: 25648298]
MCF7	IC₅₀	460 nM Compound: 20, BMS-536924	Cytotoxicity against human MCF7 cells Cytotoxicity against human MCF7 cells	[PMID: 19610618]
MCF7	IC₅₀	460 nM Compound: 3, BMS-536924	In vitro inhibitory concentration against MCF-7(breast) cell line with ATP concentration at 1/2Km In vitro inhibitory concentration against MCF-7(breast) cell line with ATP concentration at 1/2Km	[PMID: 16134929]
RD	IC₅₀	202 nM Compound: 3, BMS-536924	In vitro inhibitory concentration against RD1 (rhabdomyosarcoma) cell line with ATP concentration at 1/2Km In vitro inhibitory concentration against RD1 (rhabdomyosarcoma) cell line with ATP concentration at 1/2Km	[PMID: 16134929]
SGC-7901	IC₅₀	2.893 μM Compound: BMS-536924	Antiproliferative activity against human SGC7901 cells after 48 hrs by MTT assay Antiproliferative activity against human SGC7901 cells after 48 hrs by MTT assay	[PMID: 25648298]
SMMC-7721	IC₅₀	2.555 μM Compound: BMS-536924	Antiproliferative activity against human SMMC7721 cells after 48 hrs by MTT assay Antiproliferative activity against human SMMC7721 cells after 48 hrs by MTT assay	[PMID: 25648298]

体外実験

BMS-536924 inhibits FAK and Lck with IC₅₀s of 150 nM and 341 nM, respectively^[1].
BMS-536924 (1 μM; every four days for 12 days) blocks pBabe-MCF10A and CD8-IGF-IR-MCF10A acinar proliferation^[2].
BMS-536924 (0.01-1 μM; 24 hours) inhibits growth of CD8-IGF-IR-MCF10A cells and has an IC₅₀ of 0.48 μM^[2].
BMS-536924 (1 μM; for 4 days) induces apoptosis in CD8-IGF-IR-MCF10A acini^[2].
BMS-536924 (0.1-1 μM; for 24 hours) decreases in S-phase cells and causes a G0/G1 block^[2].
BMS-536924 (1 μM; 10 min, 1, 8, 24, 48 hours) inhibits IGF-IR signaling in pBabe-MCF10A cells and inhibits phosphorylation of CD8-IGF-IR. BMS-536924 time-dependently inhibits AKT phosphorylation^[2].

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

Cell Proliferation Assay^[2]

Cell Line:	pBabe-MCF10A and CD8-IGF-IR-MCF10A acini
Concentration:	1 μM
Incubation Time:	Every four days for 12 days
Result:	Blocked acinar proliferation.

Cell Viability Assay^[2]

Cell Line:	CD8-IGF-IR-MCF10A cells
Concentration:	0.01, 0.1, 1 μM
Incubation Time:	24 hours
Result:	Has an IC50 of 0.48 μM.

Apoptosis Analysis^[2]

Cell Line:	CD8-IGF-IR-MCF10A acini
Concentration:	1 μM
Incubation Time:	For 4 days
Result:	Resulted in a dramatic induction of apoptosis.

Cell Cycle Analysis^[2]

Cell Line:	CD8-IGF-IR-MCF10A cells and pBabe-MCF10A control cells
Concentration:	0.1, 0.5, 1 μM
Incubation Time:	For 24 hours
Result:	Decreased in S-phase cells and caused a G0/G1 block.

Western Blot Analysis^[2]

Cell Line:	CD8-IGF-IR-MCF10A cells
Concentration:	1 μM
Incubation Time:	10 min, 1, 8, 24, 48 hours
Result:	Caused maximal inhibition of phosphorylated IGF-IR at 10 min and retained its ability to inhibit IGF-IR phosphorylation for up to 48 hours.

体内実験

BMS-536924 (100 mg/kg; gavage; daily; for 35 days) causes regression of xenografts in vivo and an average reduction of 76% tumor volume after 2 weeks^[2].

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

Animal Model:	Athymic nude mice with CD8-IGF-IRMCF10A cells^[2]
Dosage:	100 mg/kg
Administration:	Gavage; daily; for 35 days
Result:	Caused an average reduction of 76% tumor volume after 2 weeks.

分子量

479.96

分子式

C₂₅H₂₆ClN₅O₃

CAS 番号

468740-43-4

Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1C(C2=NC3=CC(N4CCOCC4)=CC(C)=C3N2)=C(C=CN1)NC[C@@H](O)C5=CC=CC(Cl)=C5

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

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

溶剤 & 溶解度

体外:

DMSO : 10 mg/mL (20.84 mM; ultrasonic and warming and heat to 60°C; 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	2.0835 mL	10.4175 mL	20.8351 mL
5 mM	0.4167 mL	2.0835 mL	4.1670 mL
10 mM	0.2084 mL	1.0418 mL	2.0835 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

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: ≥ 3.75 mg/mL (7.81 mM); Clear solution

This protocol yields a clear solution of ≥ 3.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (37.5 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.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.21 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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.25 mg/mL (4.69 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

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: 99.83%

Select Batch:

データシート (285 KB) SDS (252 KB)

COA (256 KB) LCMS (267 KB) OR (62 KB)

取扱説明書 (2659 KB)

参考文献

[1]. Wittman M, et al. Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity. J Med Chem. 2005 Sep 8;48(18):5639-43. [Content Brief]

[2]. Litzenburger BC, et al. BMS-536924 reverses IGF-IR-induced transformation of mammary epithelial cells and causes growth inhibition and polarization of MCF7 cells. Clin Cancer Res. 2009 Jan 1;15(1):226-37. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.0835 mL	10.4175 mL	20.8351 mL	52.0877 mL
	5 mM	0.4167 mL	2.0835 mL	4.1670 mL	10.4175 mL
	10 mM	0.2084 mL	1.0418 mL	2.0835 mL	5.2088 mL
	15 mM	0.1389 mL	0.6945 mL	1.3890 mL	3.4725 mL
	20 mM	0.1042 mL	0.5209 mL	1.0418 mL	2.6044 mL

BMS-536924 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:

BMS-536924468740-43-4BMS536924BMS 536924IGF-1RInsulin ReceptorApoptosisInsulin-like growth factor-1 receptorOrallyinsulin-likegrowthfactorbreastcancer,Inhibitorinhibitorinhibit

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BMS-536924

カスタマーレビュー

Other Forms of BMS-536924:

BMS-536924 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:

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

BMS-536924 関連抗体

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

BMS-536924 Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

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