RP-6685

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

RP-6685是一种有效且具有选择性和口服活性的 DNA 聚合酶 θ (Polθ) 抑制剂，其 IC50 值为5.8 nM (PicoGreen 实验)。RP-6685 在小鼠肿瘤移植模型中表现出抗肿瘤作用。

RP-6685 is a potent, selective and orally active DNA polymerase theta (Polθ) inhibitor with an IC50 value of 5.8 nM (PicoGreen assay). RP-6685 shows antitumor efficacy in mouse tumor xenograft model. RP-6685 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

——

Animal Model:Female CD1 nude mice (HCT116 BRCA2+/+ and BRCA2-/- xenograft tumor models)Dosage:80 mg/kg Administration:p.o.; BID for 21 days Result:Showed tumor regression during the first 8 days of treatment in BRCA2-/- HCT116 model, while did not inhibit tumor growth in BRCA2+/+ HCT116 tumors mice.

——

Cell Cycle/DNA Damage

DNA/RNA Synthesis

DNA/RNA Synthesis

——

——

2832047-80-8

497.37

C22H14F7N5O

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 100 mg/mL (201.06 mM; 超声助溶 )

Nc1ccc(nn1)C#CCN(C(=O)Cc1ncc(cc1C(F)(F)F)C(F)(F)F)c1ccc(F)cc1

——

(-20℃)

With Ice Pack

≥ 2 years