产品
编 号：F741827
分子式：C22H14F7N5O
分子量：497.37
分子式：C22H14F7N5O
分子量：497.37
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
询价
询价
5mg
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询价
10mg
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询价
结构图
CAS No: 2832047-80-8
产品详情
生物活性：
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.
体内研究：
RP-6685 (80 mg/kg；口服；BID，持续 21 天) 在 BRCA2 缺陷型 HCT116 小鼠中表现出有效的抗肿瘤功效。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.
Animal Model:CD1 mice (20-30 g)
Dosage:2.5 mg/kg
Administration:i.v. or p.o.; single dosage
Result:CL (mL/min/kg)Vdss (L/kg) t1/2 (h) F (%)
36.81.10.466
体外研究：
RP-6685 对全长 Polθ 的 pol 活性具有 550 pM 的 IC50 并且对 ATP 酶活性无活性。RP-6685 抑制 HEK293 LIG4-/- 细胞中的 Polθ，IC50 为 0.94 μM。
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.
体内研究：
RP-6685 (80 mg/kg；口服；BID，持续 21 天) 在 BRCA2 缺陷型 HCT116 小鼠中表现出有效的抗肿瘤功效。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.
Animal Model:CD1 mice (20-30 g)
Dosage:2.5 mg/kg
Administration:i.v. or p.o.; single dosage
Result:CL (mL/min/kg)Vdss (L/kg) t1/2 (h) F (%)
36.81.10.466
体外研究：
RP-6685 对全长 Polθ 的 pol 活性具有 550 pM 的 IC50 并且对 ATP 酶活性无活性。RP-6685 抑制 HEK293 LIG4-/- 细胞中的 Polθ，IC50 为 0.94 μM。
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