RP-6685|cas:2832047-80-8|西域试剂

RP-6685,99.96%

产品编号：Bellancom-151462| CAS NO：2832047-80-8| 分子式：C₂₂H₁₄F₇N₅O| 分子量：497.37

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	包装	价格	库存与货期	购买量	操作
Bellancom-151462		￥6200.00	杭州北京（现货）
Bellancom-151462		￥9800.00	杭州北京（现货）

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RP-6685

产品介绍

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。

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.

体外研究

RP-6685 is extremely potent with an IC₅₀ of 550 pM against the pol activity of full-length Polθ and inactive on the ATPase activity.
RP-6685 inhibits Polθ in HEK293 LIG4^-/- cellswith an IC₅₀ of 0.94 μM.

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

体内研究

RP-6685 (80 mg/kg; p.o.; BID for 21 days) exhibits potent antitumor efficacy in BRCA2-deficient HCT116 mice.

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

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)	V_dss (L/kg)	t_1/2 (h)	F (%)
36.8	1.1	0.4	66

体内研究

RP-6685 (80 mg/kg; p.o.; BID for 21 days) exhibits potent antitumor efficacy in BRCA2-deficient HCT116 mice.

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

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)	V_dss (L/kg)	t_1/2 (h)	F (%)
36.8	1.1	0.4	66

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (201.06 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.0106 mL	10.0529 mL	20.1058 mL
5 mM	0.4021 mL	2.0106 mL	4.0212 mL
10 mM	0.2011 mL	1.0053 mL	2.0106 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。-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 90% corn oil
Solubility: ≥ 2.08 mg/mL (4.18 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.18 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 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。