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JSH-150 纯度: 98.01%
JSH-150 是一种高效的选择性 CDK9 抑制剂, IC50 为 1 nM。
JSH-150 Chemical Structure
CAS No. : 2247481-21-4
规格 | 价格 | 是否有货 | 数量 |
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5 mg | ¥4800 | In-stock | |
10 mg | ¥8000 | In-stock | |
25 mg | ¥16500 | In-stock | |
50 mg | ¥25500 | In-stock | |
100 mg | ¥38000 | In-stock | |
200 mg | 询价 | ||
500 mg | 询价 |
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JSH-150 相关产品
•相关化合物库:
- Covalent Screening Library Plus
- Bioactive Compound Library Plus
- Cell Cycle/DNA Damage Compound Library
- Kinase Inhibitor Library
- Anti-Cancer Compound Library
- Anti-Aging Compound Library
- Covalent Screening Library
- Anti-Breast Cancer Compound Library
- Anti-Blood Cancer Compound Library
- Targeted Diversity Library
生物活性 |
JSH-150 is a highly selective and potent CDK9 inhibitor with an IC50 of 1 nM. |
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IC50 & Target |
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体外研究 (In Vitro) |
The antiproliferative effect of JSH-150 is examined ton a panel of established cancer cell lines. JSH-150 exhibits potent antiproliferative activities in solid tumor cell lines such as A375 (melanoma), A431 (squamous), BE(2)M17 (neuroblastoma), GIST-T1 (GIST) and COLO205 (colon cancer) with GI50 values from 0.002 to 0.044 µM. In the leukemia cell lines including acute myeloid leukemia (AML), chronic lymphocytic leukemia (CLL) and B cell lymphoma cell lines, JSH-150 also displays strong growth inhibition efficacies with GI50s ranging from single to double digit nM. In addition, JSH-150 is much less sensitive in normal CHO cells (GI50: 1.1 µM) compared with the cancer cell lines[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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体内研究 (In Vivo) |
Treatment of JSH-150 at all dosages, i.e., 10, 20 and 30 mg/kg/day, can almost completely suppress the tumor progression in the first two weeks and does not affect the animal’s weight indicating that there is no general cytotoxicity at these doses. After stopping the treatment of JSH-150, the tumors of the animals treated with 10 mpk drug dosage start to grow again. However, this tumor recurrence is not observed in the 20 and 30 mpk dosage groups during the following week after administration of JSH-150 is stopped and p values are quantified on the 21st day, which are 0.042, 0.0035 and 0.0028, respectively. The PK properties of JSH-150 are evaluated in different species including mice, Sprague-Dawley rats and beagle dogs through intravenous injection and oral administration. JSH-150 is absorbed rapidly in dogs and mice (Tmax=1.33 h and 2.00 h respectively) but slowly in rats (Tmax=3.33 h). JSH-150 also displays different half-lives in three different species via oral administration (T1/2=1.55 h in mice, 3.37 h in rats and 20.37 h in dogs), which indicates that it is metabolized very slowly in dogs compared with mice and rats. In addition, JSH-150 exhibits acceptable bioavailability in mice, rats and dogs (F=45.01%, 45.10% and 39.15%, respectively). The PK properties indicated that JSH-150 is suitable for oral administration[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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分子量 |
505.08 |
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Formula |
C24H33ClN6O2S |
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CAS 号 |
2247481-21-4 |
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运输条件 |
Room temperature in continental US; may vary elsewhere. |
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储存方式 |
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溶解性数据 |
In Vitro:
DMSO : 100 mg/mL (197.99 mM; Need ultrasonic) 配制储备液
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
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参考文献 |
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Cell Assay [1] |
The A375 (melanoma), A431 (squamous), BE(2)M17 (neuroblastoma), BE(2)M17 (neuroblastoma), CRL-2234 (hepatoma), COLO205 (colon cancer), A549 (lung adenocarcinoma), Ramos (B cell lymphoma), MV4-11 (AML), Ramos (B cell lymphoma), U937 (AML), CHL (hamster lung cell), and CHO (hamster ovary cell) cell lines are used. OCI-AML-3 (AML), SKM-1 (AML), MEC-1 (CLL), MEC-2 (CLL) and HL-60 (human promyelocytic leukemia cells) are used. Human GIST-T1 cells are used. MOLM-13 and MOLM14 cell lines are used. All the cells are grown in a humidified incubator at 37°C under 5% CO2. A375, A431, GIST-T1, A549, Colo205 and CHO cells are maintained in DMEM supplemented with 10% FBS, 1% Penicillin/Streptomycin. BE(2)M17 cells are cultured with 1:1 mixture of ATCC-formulated Eagle’s minimum essential medium, and F12 Medium. MV4-11, MEC-1 and MEC-2 are grown in IMDM supplemented with 10% FBS, 1% Penicillin/Streptomycin. CRL-2234, U2932, U937, Ramos, MOLM13, MOLM14, OCI-AML-3, SKM-1, HL-60 and CHL are grown in RPMI 1640 medium supported with 10% FBS and 1% Penicillin/Streptomycin. Adherent cells are grown in tissue culture flasks until they are 85-95% confluent prior to use. For suspension cells, cells are collected by spin down at 800 rpm/min for 5 min before use. Cells are grown in 96-well culture plates (3000 cells/well). The compounds (e.g., JSH-150) at various concentrations are added into the plates. Cell proliferation is determined after treatment with compounds (e.g., JSH-150) for 72 h. Cell viability is measured using the Cell Titer-Glo assay and luminescence is measured in a multilabel reader[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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Animal Administration [1] |
Mice[1] 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
参考文献 |
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