Dinaciclib

カタログ番号 T1912 CAS 779353-01-4

別名: SCH 727965, PS-095760

Dinaciclib (SCH 727965) is a CDK inhibitor that selectively inhibits CDK1, CDK2, CDK5, and CDK9 (IC50 score = 3/1/1/4 nM). Dinaciclib has potential antitumor activity and inhibits the incorporation of thoracic glycan (dThd) DNA.

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Dinaciclib, CAS 779353-01-4

パッケージサイズ	在庫状況	単価(税別)
サンプルについてお問い合わせ
2 mg	在庫あり	￥ 11,000
5 mg	在庫あり	￥ 17,500
10 mg	在庫あり	￥ 28,000
50 mg	在庫あり	￥ 89,000
1 mL * 10 mM (in DMSO)	在庫あり	￥ 17,500

バルクのお問い合わせ

バッチを選択

純度: 99.75%

COA DATASHEET SDS HNMR HPLC

純度: 99.73%

COA DATASHEET SDS HNMR HPLC

純度: 99.65%

COA DATASHEET SDS HNMR HPLC

純度: 99.22%

COA DATASHEET SDS HNMR HPLC

純度: 99.18%

COA DATASHEET SDS HPLC

純度: 98.99%

COA DATASHEET SDS HNMR HPLC

純度: 98.21%

COA DATASHEET SDS HPLC HNMR

COA DATASHEET SDS

COA DATASHEET SDS HNMR

バッチの詳細情報はお問い合わせください

生物学的特性に関する説明

化学的特性

保存条件 & 溶解度情報

説明	Dinaciclib (SCH 727965) is a CDK inhibitor that selectively inhibits CDK1, CDK2, CDK5, and CDK9 (IC50 score = 3/1/1/4 nM). Dinaciclib has potential antitumor activity and inhibits the incorporation of thoracic glycan (dThd) DNA.
ターゲット＆IC50	CDK1:3 nM (cell free), CDK9:4 nM (cell free), CDK5:1 nM (cell free), CDK2:1 nM (cell free)
In vitro	METHODS: Human pancreatic cancer cell lines MIAPaCa-2 and Pa20C were treated with Dinaciclib (0.5-128 nM) for 72 h. Cell viability was assayed using MTT Assay. RESULTS: Dinaciclib inhibited the growth of MIAPaCa-2 and Pa20C cells in a dose-dependent manner, with a GI50 of approximately 10 and 20 nM, respectively.[1] METHODS: Human osteosarcoma cell lines SaOs-2 and U2OS were treated with Dinaciclib (5-62 nmol/L) for 4-24 h, and the expression levels of target proteins were detected using Western Blot. RESULTS: Dinaciclib eliminated the phosphorylation of CDK substrates in osteosarcoma cells. [2]
In vivo	METHODS: To assay antitumor activity in vivo, Dinaciclib (40 mg/kg, 20% (w/v) HPBCD) was injected intraperitoneally twice weekly for four weeks into CD1 nu/nu athymic mice harboring human pancreatic cancer tumors, JH033 or Panc286. RESULTS: Dinaciclib inhibited the in vivo growth of a group of hypo-permeable cancer xenografts. [1] METHODS: To assay antitumor activity in vivo, Dinaciclib (8-48 mg/kg) was injected intraperitoneally into BALB/c mice harboring ovarian cancer tumor A2780 once daily for ten days. RESULTS: Dinaciclib had dose-dependent antitumor activity in vivo and almost completely inhibited tumor growth at dose levels below MTD. [3]
キナーゼ試験	Recombinant cyclin/CDK holoenzymes were purified from Sf9 cells engineered to produce baculoviruses that express a specific cyclin or CDK. Cyclin/CDK complexes were typically diluted to a final concentration of 50 μg/mL in a kinase reaction buffer containing 50 mmol/L Tris-HCl (pH 8.0), 10 mmol/L MgCl2, 1 mmol/L DTT, and 0.1 mmol/L sodium orthovanadate. For each kinase reaction, 1 μg of enzyme and 20 μL of a 2-μmol/L substrate solution (a biotinylated peptide derived from histone H1) were mixed and combined with 10 μL of diluted SCH 727965. The reaction was started by the addition of 50 μL of 2 μmol/L ATP and 0.1 μCi of 33P-ATP. Kinase reactions were incubated for 1 hour at room temperature and were stopped by the addition of 0.1% Triton X-100, 1 mmol/L ATP, 5 mmol/L EDTA, and 5 mg/mL streptavidin-coated SPA beads. SPA beads were captured using a 96-well GF/B filter plate and a Filtermate universal harvester. Beads were washed twice with 2 mol/L NaCl and twice with 2 mol/L NaCl containing 1% phosphoric acid. The signal was then assayed using a TopCount 96-well liquid scintillation counter. Dose-response curves were generated from duplicate, eight-point serial dilutions of inhibitory compounds. IC50 values were derived by nonlinear regression analysis [1].
細胞研究	A2780 cells were plated into six-well tissue culture dishes and allowed to adhere. Cells were then exposed to differing concentrations of SCH 727965 or a DMSO control vehicle for 24 hours, followed by a brief (30 min) pulsed exposure to bromodeoxyuridine (BrdUrd). Cells were then harvested, immunostained using FITC-conjugated antibodies specific for BrdUrd, counter-stained with propidium iodide/RNase A solution, and analyzed using flow cytometry. Fluorescence-activated cell sorting analyses were done on a FACSCalibur instrument. FITC-positive BrdUrd staining and propidium iodide signal allowed assessment of ongoing DNA replication and the cell cycle stage. Percentages of the cell population in each cell cycle stage were plotted for each test article concentration [1].
動物実験	For tumor implantation, specific cell lines were grown in vitro, washed once with PBS, and resuspended in 50% Matrigel in PBS to a final concentration of 4 × 10^7 to 5 × 10^7 cells per milliliter. Nude mice were injected with 0.1 mL of this suspension s.c. in the flank region. Tumor length (L), width (W), and height (H) were measured by a caliper twice weekly on each mouse and then used to calculate tumor volume using the formula (L × W × H)/2. When the tumor volume reached ～100 mm^3, the animals were randomized to treatment groups (10 mice/group) and treated i.p. with either SCH 727965 or individual chemotherapeutic agents according to the dosing schedule indicated in table and figure legends. Tumor volumes and body weights were measured during and after the treatment periods. Data were expressed as means ± SEM. Animals were euthanized according to the Institutional Animal Care and Use Committee guidelines [1].

別名	SCH 727965, PS-095760
分子量	396.49
分子式	C21H28N6O2
CAS No.	779353-01-4

保存条件

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度情報

DMSO: 50 mg/mL (126.11 mM)

Ethanol: 8 mg/mL (20.17 mM), Heating is recommended.

5% DMSO+95% Saline: 1.25 mg/mL (3.15 mM, suspension)

参考文献

1. Feldmann G, et al. Cyclin-dependent kinase inhibitor Dinaciclib (SCH727965) inhibits pancreatic cancer growth and progression in murine xenograft models. Cancer Biol Ther. 2011 Oct 1;12(7):598-609. 2. Fu W, et al. The cyclin-dependent kinase inhibitor SCH 727965 (dinacliclib) induces the apoptosis of osteosarcoma cells. Mol Cancer Ther. 2011 Jun;10(6):1018-27. 3. Parry D, et al. Dinaciclib (SCH 727965), a novel and potent cyclin-dependent kinase inhibitor. Mol Cancer Ther. 2010 Aug;9(8):2344-53. 4. Lin B, Li Y, Wang T, et al. CRMP2 is a therapeutic target that suppresses the aggressiveness of breast cancer cells by stabilizing RECK[J]. Oncogene. 2020, 39(37): 6024-6040.

引用文献

1. Wang Z, Chen D, Guan D, et al. Material properties of phase-separated TFEB condensates regulate the autophagy-lysosome pathway. Journal of Cell Biology. 2022, 221(5): e202112024 2. Zhang G M, Huang S S, Ye L X, et al. Reciprocal positive regulation between BRD4 and YAP in GNAQ-mutant uveal melanoma cells confers sensitivity to BET inhibitors. Pharmacological Research. 2022: 106464. 3. Lin B, Li Y, Wang T, et al. CRMP2 is a therapeutic target that suppresses the aggressiveness of breast cancer cells by stabilizing RECK. Oncogene. 2020, 39(37): 6024-6040 4. Ly T T G, Yun J, Ha J S, et al. Inhibitory Effect of Etravirine, a Non-Nucleoside Reverse Transcriptase Inhibitor, via Anterior Gradient Protein 2 Homolog Degradation against Ovarian Cancer Metastasis. International Journal of Molecular Sciences. 2022, 23(2): 944. 5. Pu Y, Yan D, Tu L, et al. CDK Inhibition Reverses Acquired 5-Fluorouracil Resistance in Hepatocellular Carcinoma Cells. Disease Markers. 2022 6. Jiang L, Yu Y, Li Z, et al.BMS-265246, a Cyclin-Dependent Kinase Inhibitor, Inhibits the Infection of Herpes Simplex Virus Type 1.Viruses.2023, 15(8): 1642.

投与量変換

You can also refer to dose conversion for different animals. 詳細

In vivo投与量計算 (透明溶液)

ステップ1: 以下の情報を入力してください

投与量

mg/kg

動物の平均体重

動物あたりの投与量

動物数

溶媒の組成を入力してください

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

計算するリセット

計算結果:

作業濃度: mg/ml;

DMSO溶液の作成方法: mg あらかじめ溶解した薬剤 μL DMSO (マスター溶液の濃度 mg/mL)，濃度がそのバッチの薬剤のDMSO溶解度を超える場合は、まずご連絡ください。

生体内薬剤の調合法：取る μL DMSO マスター溶液、次に追加 μL PEG300，確実に混ぜてから加える μL Tween 80，確実に混ぜてから加える μL ddH₂O, 確実に混ぜる

お問合せ内容:

必ず順番通りに溶媒を加えてください。ボルテックスミキサーや超音波、湯煎することで溶解しやすくなります

計算器

モル濃度計算機

希釈計算機

再構成計算

分子量計算機

質量

濃度

体積

分子量

モル度計算機では以下の計算が可能です

既知の体積と濃度の溶液を調製するために必要な化合物の質量
質量が既知の化合物を目的の濃度まで溶解させるのに必要な溶液の量
特定の体積の中に既知の質量の化合物を入れて得られる溶液の濃度

参考例

モル濃度計算機を使用したモル濃度計算の例
化合物の分子量が197.13g/molである場合、10mlの水に10mMのストック溶液を作るのに必要な化合物の質量はどれくらいですか？
［分子量（MW）］の欄に［197.13］と入力してください
[濃度]ボックスに10と入力し、正しい単位（millimolar）を選択します
[容量]ボックスに10と入力し、正しい単位（milliliter）を選択します
計算を押します
答えの19.713mgが質量欄に表示されます

濃度 (開始)

体積 (開始)

濃度 (終了)

体積 (終了)

溶液を作るのに必要な希釈率の計算

溶液の調製に必要な希釈率の算出
希釈計算機は、既知の濃度の原液をどのように希釈するかを計算することができる便利なツールです。V1を計算するためにC1、C2＆V2を入力します。

参考例

Tocrisの希釈計算器を用いた希釈計算の一例
50μMの溶液を20ml作るためには、10mMの原液を何ml必要ですか？
C1V1=C2V2という式を用いて、C1=10mM、C2=50μM、V2=20ml、V1を未知数とします。
濃度（開始）ボックスに10を入力し正しい単位(millimolar)を選択してください
濃度（終了）ボックスに50を入力し正しい単位(millimolar)を選択してください
体積（終了）ボックスに20を入力し正しい単位(millimolar)を選択してください
計算を押します
100 microliter (0.1 ml) という答えが体積（開始）ボックスに表示されます。

分子式

分子量 g/mol

化合物の化学式を入力して、そのモル質量や元素組成を計算します

Tヒント：化学式は大文字と小文字を区別します。: C10H16N2O2 c10h16n2o2

化合物のモル質量（分子量）を計算する手順:
化学物質のモル質量を計算するには、その化学式を入力し、「計算」をクリックしてください。.
分子質量、分子量、モル質量、モル重量の定義:
分子質量（分子量）とは、物質の1分子の質量であり、統一された原子質量単位（u）で表されます。(1uは炭素12の1原子の質量の1/12に等しい）
モル質量（molar weight）とは、ある物質の1モルの質量のことで、単位はg/molです。

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技術サポート

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Dinaciclib 779353-01-4 Apoptosis Cell Cycle/Checkpoint CDK inhibit Inhibitor SCH 727965 SCH727965 PS-095760 Cyclin dependent kinase PS095760 PS 095760 SCH-727965 inhibitor

本ウェブサイトに掲載されている製品は全て研究用試薬です。研究目的以外の用途にはご使用できません。

Dinaciclib

保存条件

溶解度情報

参考文献

引用文献

関連化合物ライブラリー

関連製品

投与量変換

In vivo投与量計算 (透明溶液)

計算器

モル度計算機では以下の計算が可能です

溶液を作るのに必要な希釈率の計算

バイアルを再構成するのに必要な溶媒の量を計算する.

化合物の化学式を入力して、そのモル質量や元素組成を計算します

技術サポート

Keywords