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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-DNA/RNA Synthesis-RP-6685
RP-6685

Chemical Structure : RP-6685

CAS No.: 2832047-80-8

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RP-6685 (RP6685, RP 6685)

货号: PC-49348Not For Human Use, Lab Use Only.

RP-6685 (RP6685) is a potent, selective and orally bioavailable inhibitor of DNA polymerase theta (Polθ) with IC50 of 5.8 nM in PicoGreen assay (0.3 nM Polθ enzyme).

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5 mg ￥1380 In stock
10 mg ￥2180 In stock
25 mg ￥3580 In stock
50 mg ￥5580 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: 99.5% (HPLC) Select Batch:

生物&药学活性

RP-6685 (RP6685) is a potent, selective and orally bioavailable inhibitor of DNA polymerase theta (Polθ) with IC50 of 5.8 nM in PicoGreen assay (0.3 nM Polθ enzyme). 
RP-6685 displays no inhibition against Pols α, ε, γ, ν (IC50 values >100 uM).
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 treated cells isolated from tumors showed a modest trend toward increased micronuclei and γH2AX, which are hallmarks of DNA damage.
RP-6685 treatment caused a dosedependent decrease in MMEJ-mediated DNA repair in treated HEK293 cells, RP-6685 exhibited a potency of 0.5 uM in DSB repair of AAVS1 loci.
RP-6685 (80 mg/kg) showed tumor regression in an HCT116 BRCA2−/− mouse tumor xenograft model.

物理化学性质&存储条件

分子量 497.377
分子式 C22H14F7N5O
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

N-(3-(6-aminopyridazin-3-yl)prop-2-yn-1-yl)-2-(3,5-bis(trifluoromethyl)pyridin-2-yl)-N-(4-fluorophenyl)acetamide

参考文献

1. Bubenik M, et al. J Med Chem. 2022 Oct 13;65(19):13198-13215. 

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