计算溶液所需的质量、体积或浓度。
为什么选择此级别
提供 ≥99% 纯度，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
2-8°C储存,避光,干燥。低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
Camonsertib (RP-3500) is an orally active, selective ATR kinase inhibitor (ATRi) with an IC 50 of 1.00 nM in biochemical assays. Camonsertib shows 30-fold selectivity for ATR over mTOR (IC 50 =120 nM) and >2,000-fold selectivity over ATM , DNA-PK , and PI3Kα kinases. Camonsertib has potent antitumor activity
In Vitro
Camonsertib (RP-3500; 1 μM; 1-24 hours) inhibits CHK1(Ser345) phosphorylation from 1 to 3 hours. ?\nCamonsertib inhibits Gemcitabine stimulated ATR phosphorylation of its substrate pCHK1(Ser345) with an IC 50 of 0.33 nM in a LoVo cell-based assay. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: LoVo and CW-2 human colon cancer cell lines Concentration: 1 μM Incubation Time: 1, 2, 4, 6, 8, 16, 24 hours Result: Inhibited CHK1(Ser345) phosphorylation from 1 to 3 hours. Starting at 4 hours, CHK1(Ser345) became re-phosphorylated as DNA-PKcs became activated in treated cells, along with its substrates KAP1 and H2AX.
In Vivo
Camonsertib (RP-3500; 3, 7, 15 mg/kg; Orally; once daily for 18 days) produces dose-dependent tumor growth inhibition with a minimum effective dose (MED) of 7 mg/kg in LoVo xenografts . ?\nCamonsertib (5, 10 mg/kg; Orally; once daily) produces statistically significant tumor growth inhibition in the CW-2 colon xenograft model . ?\nCamonsertib (7 mg/kg; for 7 days) results in 8.1- and 2.7-fold inductions of KAP1 and DNA-PKcs phosphorylation in mice bearing LoVo tumors . ?\nCamonsertib has a more profound anti-tumor effect occurred at higher doses on the 3 days on/4 days off (30 mg/kg) and 5 days on/2 days off (25 mg/kg) schedules compared with consecutive daily administrations (10 mg/kg) at a lower dose for 14 days . ?\nCamonsertib (15mg/kg) combined PARPi Olaparib (80mg/kg; both agents days 1-3 on/4 days off) or sequential (PARPi for 3 days followed by RP-3500 for 3 days then 1 day off) schedules produces greater antiTumor effects compared with sequential administration without affecting tolerability . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female mice (6-8 weeks old) bearing LoVo xenografts Dosage: 3, 7, 15 mg/kg (0.5% methylcellulose/0.02% SDS vehicle) Administration: Orally; once daily for 18 days Result: Produced dose-dependent tumor growth inhibition with a minimum effective dose (MED) of 7 mg/kg. The maximum tolerated dose (MTD) was 10 mg/kg once daily on a continuous dosing schedule.
Form:Solid
IC50& Target:ATR ATM >30 μM (IC 50 ) mTOR 120 nM (IC 50 )
规格
别名
卡蒙塞蒂布
规格或纯度
≥99%
英文名称
Camonsertib
生化机理
Camonsertib（RP-3500）是一种口服活性、选择性 ATR 激酶抑制剂（ATRi），在生化试验中的 IC 50 为 1.00 nM。Camonsertib 对 ATR 的选择性是 mTOR 的 30 倍（IC 50 =120 nM），是 ATM、DNA-PK 和 PI 的 2,000 倍以上。
储存条件
2-8°C储存,避光,干燥
运输条件
低温运输
纯度
≥99%
名称和识别符
分子类型
小分子
Smiles
C[C@@H]1COCCN1C2=NC3=C(C=NN3C4=CC=NN4)C(=C2)C5(C[C@H]6CC[C@@H](C5)O6)O
Isomeric SMILES
C[C@@H]1COCCN1C2=NC3=C(C=NN3C4=CC=NN4)C(=C2)C5(C[C@H]6CC[C@@H](C5)O6)O
分子量
410.47
技术文档
高级数据
化学和物理性质
溶解性
DMSO : 50 mg/mL (121.81 mM; Need ultrasonic)
分子量
410.500 g/mol
XLogP3
1.600
氢键供体数Hydrogen Bond Donor Count
2
氢键受体数Hydrogen Bond Acceptor Count
7
可旋转键计数Rotatable Bond Count
3
精确质量Exact Mass
410.207 Da
单同位素质量Monoisotopic Mass
410.207 Da
拓扑极表面积Topological Polar Surface Area
101.000 Ų
重原子数Heavy Atom Count
30
形式电荷Formal Charge
0
复杂度Complexity
628.000
同位素原子数Isotope Atom Count
0
定义的原子立体中心计数Defined Atom Stereocenter Count
3
未定义的原子立体中心计数Undefined Atom Stereocenter Count
0
定义的键立体中心计数Defined Bond Stereocenter Count
0
未定义的键立体中心计数Undefined Bond Stereocenter Count
0
所有立体化学键的总数The total count of all stereochemical bonds
0
共价键合单元计数Covalently-Bonded Unit Count
1
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技术文档和文章
溶液计算器
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