Camonsertib

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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。

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.

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.

Animal Model:Female mice (6-8 weeks old) bearing LoVo xenograftsDosage: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.

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Cell Cycle/DNA Damage

ATM/ATR

ATM/ATR

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2417489-10-0

410.47

C21H26N6O3

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 50 mg/mL (121.81 mM; 超声助溶 )

C[C@@H]1COCCN1c1cc(c2cnn(-c3cc[nH]n3)c2n1)[C@@]1(O)C[C@@H]2CC[C@H](C1)O2

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(-20℃)

With Ice Pack

≥ 2 years