Ro-3306

製品コードS7747 バッチS774705

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₁₈H₁₃N₃OS₂

分子量

351.45

CAS No.

872573-93-8

Solubility (25°C)*

体外

DMSO (warmed with 50ºC water bath)

35 mg/mL (99.58 mM)

Water

Insoluble

Ethanol

Insoluble

体内（毎回新しく調製した物を用意してください）

Clear solution

5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O

0.44mg/ml

Taking the 1 mL working solution as an example, add 50 μL of 8.75 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to make it clear. Volume up to 1 mL. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	RO-3306 is an ATP-competitive, and selective CDK1 inhibitor with K_i of 20 nM, >15-fold selectivity against a diverse panel of human kinases. RO-3306 enhances p53-mediated Bax activation and mitochondrial apoptosis.
in vitro	RO-3306 inhibits CDK1/cyclin B1, CDK1/cyclin A, CDK2/cyclin E, and CDK4/cyclin D activity with Ki of 35 nM, 110 nM, 340 nM, and over 2000 nM, respectively. Treatment of HCT116, SW480, and HeLa cells with RO-3306 for 20 h leads to a complete block of the cell cycle in the G2/M phase. The proliferation of both HCT116 and SW480 is effectively blocked by RO-3306. RO-3306 appears to be more proapoptotic in cancer cells (HCT116 and SW480) than nontumorigenic cells (MCF 10A and MCF 12A).^[1] RO-3306 effectively arrests oocyte maturation at a concentration of 10 μM.^[2]
in vivo	RO-3306 is an ATP-competitive, and selective CDK1 inhibitor.

製品説明

RO-3306 is an ATP-competitive, and selective CDK1 inhibitor with K_i of 20 nM, >15-fold selectivity against a diverse panel of human kinases. RO-3306 enhances p53-mediated Bax activation and mitochondrial apoptosis.

in vitro

RO-3306 inhibits CDK1/cyclin B1, CDK1/cyclin A, CDK2/cyclin E, and CDK4/cyclin D activity with Ki of 35 nM, 110 nM, 340 nM, and over 2000 nM, respectively. Treatment of HCT116, SW480, and HeLa cells with RO-3306 for 20 h leads to a complete block of the cell cycle in the G2/M phase. The proliferation of both HCT116 and SW480 is effectively blocked by RO-3306. RO-3306 appears to be more proapoptotic in cancer cells (HCT116 and SW480) than nontumorigenic cells (MCF 10A and MCF 12A).^[1]

RO-3306 effectively arrests oocyte maturation at a concentration of 10 μM.^[2]

in vivo

RO-3306 is an ATP-competitive, and selective CDK1 inhibitor.

プロトコル(参考用のみ)

キナーゼアッセイ	CDK assay
キナーゼアッセイ	The activity of CDK1 cyclin B1, CDK1 cyclin A, CDK2 cyclin E, and CDK4 cyclin D is measured by a homogeneous time-resolved fluorescence assay in a 96-well format. The assay buffer contained 25 mM Hepes, 6.25 mM MgCl2, 0.003% Tween 20, 0.3 mg/mL BSA, 1.5 mM DTT, and ATP as follows: 162 μM (CDK1), 90 mM (CDK2), or 135 μM (CDK4). CDK1 and CDK2 buffer contained 10 mM MgCl2. Test compounds are diluted in assay buffer to 3-fold their final concentration in 20 μL, and the reaction is started by the addition of a 40 μL assay buffer containing the pRB substrate (0.185μM). The plates are incubated at 37°C for 30 min with constant agitation, and the reaction is terminated by the addition of 15 μL of 1.6μM anti-phospho pRB antibody (Ser-780) in 25 mM Hepes, 24 mM EDTA, and 0.2 mg/mL BSA. After an additional 30 min of incubation with shaking, 15μL of 3nM Lance-Eu-W1024-labeledanti-rabbitIgG and 60 nM Alophycocyanin-conjugated anti-His-6 antibody in 25 mM Hepes, and 0.5 mg/mL BSA is added and incubated for 1 h. The plates are read in the Victor-V multi- label reader at excitation 340 nm and emission 615 nm and 665 nm. The IC50 values are calculated from the readings at 665 nm and normalized for Europium readings at 615 nm. Ki values are calculated according to the equation: Ki= IC50/(1 + S/Km ), where S is the ATP concentration in the assay and Km is the Michaelis-Menten constant for ATP. The inhibitory activity against the panel of kinases is determined by the IMAP assay technology.
細胞アッセイ	細胞株	MDA-MB-231 cell line
	濃度	20 μM
	反応時間	72 h
	実験の流れ	Log phases cells (25,000) are seeed in 96-well plates and incubated in a 37℃ incubator with CO2, After 24 h, different concentrations of RO-3306 are administered to determine the drug concentrations required to achieve a 50% growth inhibition (IC50). MTT (20 μL, 5mg/mL stock solution in saline) is added to each well and the cells are incubated for 4 h. Supernatants are removed and formazan crystals from viable cells are solubilized with 200 μL anhydrous DMSO. The absorbance is detected with a 550 model microplate reader at the 565 nm wavelength.
動物実験	動物モデル	Female BALB/c mice
	投薬量	1.5 mg/kg
	投与方法	i.n.

参考

[4] Zhao L, et al. Antiviral Res. 2022 May;201:105296.

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カスタマーフィードバック

: Data from [Data independently produced by , , J Cell Biol, 2015, 209(2): 221-34 ]

: Data from [Data independently produced by , , Arthritis Rheumatol, 2016, 68(5):1222-32.]

: Data from [Data independently produced by , , Sci Rep, 2017, 7:41950]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Comprehensive multi-omics analysis reveals WEE1 as a synergistic lethal target with hyperthermia through CDK1 super-activation [ Nat Commun, 2024, 15(1):2089]	PubMed: 38453961
ATR limits Rad18-mediated PCNA monoubiquitination to preserve replication fork and telomerase-independent telomere stability [ EMBO J, 2024, 43(7):1301-1324]	PubMed: 38467834
DIS3 depletion in multiple myeloma causes extensive perturbation in cell cycle progression and centrosome amplification [ Haematologica, 2024, 109(1):231-244]	PubMed: 37439377
Multiple intersecting pathways are involved in the phosphorylation of CPEB1 to activate translation during mouse oocyte meiosis [ bioRxiv, 2024, 2024.01.17.575938]	PubMed: 38293116
Polarized microtubule remodeling transforms the morphology of reactive microglia and drives cytokine release [ Nat Commun, 2023, 14(1):6322]	PubMed: 37813836
Homology directed telomere clustering, ultrabright telomere formation and nuclear envelope rupture in cells lacking TRF2B and RAP1 [ Nat Commun, 2023, 14(1):2144]	PubMed: 37059728
Histone demethylase KDM2A is a selective vulnerability of cancers relying on alternative telomere maintenance [ Nat Commun, 2023, 14(1):1756]	PubMed: 36991019
Polarized microtubule remodeling transforms the morphology of reactive microglia and drives cytokine release [ Nat Commun, 2023, 14(1):6322]	PubMed: 37813836
Master mitotic kinases regulate viral genome delivery during papillomavirus cell entry [ Nat Commun, 2023, 14(1):355]	PubMed: 36683055
Inhibition of CDK1 Overcomes Oxaliplatin Resistance by Regulating ACSL4-mediated Ferroptosis in Colorectal Cancer [ Adv Sci (Weinh), 2023, 10(25):e2301088]	PubMed: 37428466

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。