Camonsertib RP-3500; ATR inhibitor 4|cas:2417489-10-0|西域试剂

Camonsertib RP-3500; ATR inhibitor 4,99.75%

产品编号：Bellancom-139609| CAS NO：2417489-10-0| 分子式：C₂₁H₂₆N₆O₃| 分子量：410.47

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-139609		￥6400.00	杭州北京（现货）
Bellancom-139609		￥10200.00	杭州北京（现货）

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Camonsertib RP-3500; ATR inhibitor 4

产品介绍

Camonsertib (RP-3500) 是一种口服有效的，选择性 ATR 激酶抑制剂 (ATRi)，在生化试验中的 IC₅₀ 为 1.00 nM。Camonsertib 对 ATR 的选择性是 mTOR 的 30 倍 (IC₅₀=120 nM)，是 ATM、DNA-PK 和 PI3Kα 激酶的 > 2,000 倍。Camonsertib 具有有效的抗肿瘤活性。

生物活性

Camonsertib (RP-3500) is an orally active, selective ATR kinase inhibitor (ATRi) with an IC₅₀ of 1.00 nM in biochemical assays. Camonsertib shows 30-fold selectivity for ATR over mTOR (IC₅₀=120 nM) and >2,000-fold selectivity over ATM, DNA-PK, and PI3Kα kinases. Camonsertib has potent antitumor activity.

体外研究

Camonsertib (RP-3500; 1 μM; 1-24 hours) inhibits CHK1(Ser345) phosphorylation from 1 to 3 hours.
Camonsertib inhibits Gemcitabine stimulated ATR phosphorylation of its substrate pCHK1(Ser345) with an IC₅₀ of 0.33 nM in a LoVo cell-based assay.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis

Cell 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.

体内研究
(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.
Camonsertib (5, 10 mg/kg; Orally; once daily) produces statistically significant tumor growth inhibition in the CW-2 colon xenograft model.
Camonsertib (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.
Camonsertib 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.
Camonsertib (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.

西域 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.

体内研究

西域 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.

体内研究

西域 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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 50 mg/mL (121.81 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.4362 mL	12.1812 mL	24.3623 mL
5 mM	0.4872 mL	2.4362 mL	4.8725 mL
10 mM	0.2436 mL	1.2181 mL	2.4362 mL

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。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

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
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 1.25 mg/mL (3.05 mM); Clear solution

此方案可获得 ≥ 1.25 mg/mL (3.05 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 1.25 mg/mL (3.05 mM); Clear solution

此方案可获得 ≥ 1.25 mg/mL (3.05 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 1.25 mg/mL (3.05 mM); Clear solution

此方案可获得 ≥ 1.25 mg/mL (3.05 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。