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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C18H17ClN4O |
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分子量 | 340.81 | CAS No. | 1883423-59-3 | ||||||||
Solubility (25°C)* | 体外 | DMSO | 68 mg/mL (199.52 mM) | ||||||||
Ethanol | 68 mg/mL (199.52 mM) | ||||||||||
Water | Insoluble | ||||||||||
体内 (毎回新しく調製した物を用意してください) |
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* <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. |
製品説明 | MSC2530818, a CDK8 inhibitor with the IC50 of 2.6 nM, displays excellent kinase selectivity, biochemical and cellular potency, microsomal stability, and is orally bioavailable. |
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in vitro | MSC2530818 binds to CDK8 and CDK19 with similar affinity (4 nM) and shows potent inhibition of phospho-STAT1SER727 in SW620 human colorectal carcinoma cells (IC50=8 ± 2 nM). It also demonstrates potent inhibition of WNT-dependent transcription in human cancer cell lines that have constitutively activated WNT signaling. MSC2530818 is a soluble CDK8 inhibitor with high permeability and low efflux ratio in Caco-2 cells (ER = 1.5) and does not inhibit any cytochrome P450 subtypes (Cyp IC50s > 20 μM)[1]. |
in vivo | MSC2530818 shows acceptable pharmacokinetics (PK) in all tested preclinical species (mouse, rat, dog). It demonstrates reduction of tumor growth rates of established human SW620 colorectal carcinoma xenografts[1]. |
細胞アッセイ | 細胞株 | Pancreatic duct-like organoids |
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濃度 | 0.05 µM | |
反応時間 | ||
実験の流れ | ||
動物実験 | 動物モデル | NCr athymic mice |
投薬量 | 50 mg/kg bid or 100 mg/kg qd | |
投与方法 | p.o. |
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Organoids at the PUB: The Porcine Urinary Bladder serves As A Pancreatic Niche for Advanced Cancer Modelling [ Adv Healthc Mater, 2022, e2102345] | PubMed: 35114730 |
LATS1 is a central signal transmitter for achieving full type-I interferon activity [ Sci Adv, 2022, 8(14):eabj3887] | PubMed: 35394840 |
Single-cell-resolved differentiation of human induced pluripotent stem cells into pancreatic duct-like organoids on a microwell chip [ Nat Biomed Eng, 2021, 10.1038/s41551-021-00757-2] | PubMed: 34239116 |
Modeling plasticity and dysplasia of pancreatic ductal organoids derived from human pluripotent stem cells [ Cell Stem Cell, 2021, 28(6):1105-1124.e19] | PubMed: 33915078 |
Differentiation of human pluripotent stem cells into pancreatic duct-like organoids [ STAR Protoc, 2021, 2(4):100913] | PubMed: 34917972 |
A kinase-independent role for CDK8 in BCR-ABL1+ leukemia. [ Nat Commun, 2019, 10(1):4741] | PubMed: 31628323 |
A kinase-independent role for CDK8 in BCR-ABL1+ leukemia [ Nature Communications, 2019, ] | PubMed: None |
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。