Ro-3306

製品コードS7747 バッチS774704

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）

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

* <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

https://pubmed.ncbi.nlm.nih.gov/16818887/
https://pubmed.ncbi.nlm.nih.gov/24374180/
https://pubmed.ncbi.nlm.nih.gov/24378347/

https://pubmed.ncbi.nlm.nih.gov/35367281/

+ 展开

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：

The cAMP-PKA signaling initiates mitosis by phosphorylating Bora [ Nat Commun, 2025, 16(1):7898]	PubMed: 40849432
TRF1 relies on fork reversal to prevent fragility at human telomeres [ Nat Commun, 2025, 16(1):6439]	PubMed: 40645989
Cell cycle progression of under-replicated cells [ Nucleic Acids Res, 2025, 53(1)gkae1311]	PubMed: 39778868
Combined therapy with DR5-targeting antibody-drug conjugate and CDK inhibitors as a strategy for advanced colorectal cancer [ Cell Rep Med, 2025, S2666-3791(25)00231-9]	PubMed: 40449480
SMAD2 linker phosphorylation impacts overall survival, proliferation, TGFβ1-dependent gene expression and pluripotency-related proteins in NSCLC [ Br J Cancer, 2025, 133(1):52-65]	PubMed: 40319202
Genomic context influences translesion synthesis DNA polymerase-dependent mechanisms of micronuclei induction by G-quadruplexes [ Cell Rep, 2025, 44(5):115706]	PubMed: 40349342
An Aurora kinase A-BOD1L1-PP2A B56 axis promotes chromosome segregation fidelity [ Cell Rep, 2025, 44(2):115317]	PubMed: 39970043
CDK2 Inhibition Produces a Persistent Population of Polyploid Cancer Cells [ JCI Insight, 2025, e189901]	PubMed: 40232858
CDK1-mediated phosphorylation of LDHA fuels mitosis through LDHB-dependent lactate oxidation [ EMBO Rep, 2025, 10.1038/s44319-025-00573-8]	PubMed: 40940446
Dynamic SAS-6 phosphorylation aids centrosome duplication and elimination in C. elegans oogenesis [ EMBO Rep, 2025, 10.1038/s44319-025-00485-7]	PubMed: 40410380

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。