Product Details
| Product Name:
Camonsertib |
CAS No.:
2417489-10-0 |
| Purity:
99.6% |
Supply Ability:
10g |
| Release date:
2024/11/11 |
Product Introduction
Bioactivity
| 名稱 | Camonsertib |
| 描述 | Camonsertib (RP-3500) is a novel, potent and selective ATR kinase inhibitor (ATRi) that exhibits potent antitumor effects with an IC50: 1.00 nM in biochemical assays.RP-3500 is 30-fold more selective for ATR than mTOR (IC50: 120 nM) and more than 2,000-fold more potent than ATM, DNA-PK and PI3Kα kinases. RP-3500 is 30 times more selective for ATR than mTOR (IC50: 120 nM), and 2,000 times more selective than ATM, DNA-PK and PI3Kα kinases. |
| 體外活性 | METHODS: Characterization of the DNA damage response (DDR) to Camonsertib (RP-3500)-mediated ATR inhibition in LoVo and CW-2 human colon cancer cell lines treated with 1 μmol/L RP-3500 for varying durations up to 24 hours.
RESULTS Camonsertib (RP-3500) inhibits CHK1 (Ser345) phosphorylation 1-3 hours after initiation of treatment. [2]
METHODS: A biochemical assay for ATR/ATRIP inhibition was established using tagged human ATR and ATRIP purified from mammalian cells, with p53 (Ser15) as the phosphorylation substrate.
RESULTS In a LoVo cell-based assay, Camonsertib (RP-3500) inhibited gemcitabine-stimulated phosphorylation of the ATR substrate pCHK1 (Ser345) with an IC50 of 0.33 nM. [2] |
| 體內(nèi)活性 | METHODS: Patients received Camonsertib (RP-3500) at doses ranging from 5-200 mg once daily or 40 to 80 mg twice daily for 5 days/2 days off (5/2) or 3 days/4 days off ( 3/4), hematological parameters were assessed over a range of doses during treatment.
RESULTS Early decrease in monocytes and reticulocytes on day 8 and further decrease in hemoglobin levels on day 15. [1]
METHODS: Camonsertib (RP-3500) was used to treat LoVo tumor xenografts in mice, orally administered once a day at a dose of 3/7/15 mg/kg for 17 days, and the effect on LoVo tumor xenografts in mice was observed.
RESULTS Camonsertib (RP-3500) treatment of LoVo tumor xenografts in mice produced dose-dependent tumor growth inhibition, with a minimum effective dose (MED) of 7 mg/kg. [2]
METHODS: In the CW-2 colon xenograft model, Camonsertib (RP-3500) was administered at doses of 5 and 10 mg/kg to observe the effects on the growth of the mouse CW-2 colon xenograft model.
RESULTS Treatment of xenograft mice with Camonsertib (RP-3500) produced statistically significant tumor growth inhibition. [2] |
| 存儲條件 | store at low temperature,keep away from direct sunlight | Shipping with blue ice. |
| 溶解度 | DMSO : 45.0 mg/mL (109.6 mM), Sonication is recommended.
|
| 關(guān)鍵字 | RP3500 | Camonsertib | RP 3500 |
| 相關(guān)產(chǎn)品 | CP-466722 | Ro 90-7501 | Dactolisib | Berzosertib | Elimusertib | GJ103 sodium salt | KU60019 | Ceralasertib | (Z)-Mirin | NU6027 | Schisandrin B | AZ32 |
| 相關(guān)庫 | 經(jīng)典已知活性庫 | 激酶抑制劑庫 | 藥物功能重定位化合物庫 | 抗衰老化合物庫 | 已知活性化合物庫 |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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Recommended supplier
| Product name |
Price |
|
Suppliers |
Update time |
|
|
$/ |
|
Anhui Ruihan Technology Co., Ltd
|
2023-08-21 |
United States