Free shipping on all orders over $ 500


Cat. No. M2047
VE-821 Structure
Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
5mg USD 49  USD49 In stock
10mg USD 82  USD82 In stock
25mg USD 139  USD139 In stock
50mg USD 229  USD229 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control
Biological Activity

VE-821 is a novel ATR inhibitor. VE-821 was shown to inhibit ATR-mediated signalling in response to replication arrest induced by severe hypoxia. VE-821 inhibited radiation- and gemcitabine-induced phosphorylation of Chk1, confirming inhibition of ATR signaling. ATR inhibition by VE-821 led to inhibition of radiation-induced G 2/M arrest in cancer cells. Consistently, VE-821 significantly enhanced the sensitivity of PSN-1, MiaPaCa-2 and primary PancM pancreatic cancer cells to radiation and gemcitabine under both normoxic and hypoxic conditions. VE-821 induced DNA damage and consequently increased Ataxia Telangiectasia Mutated-mediated phosphorylation of H2AX and KAP1. Most importantly, VE-821 increased radiation-induced loss of viability in hypoxic conditions. Reduced cancer cell radiosurvival following treatment with VE-821 was also accompanied by increased DNA damage and inhibition of homologous recombination repair, as evidenced by persistence of γH2AX and 53BP1 foci and inhibition of Rad51 foci, respectively.

Customer Product Validations & Biological Datas
Source Radiat Oncol (2015). Figure 2. VE-821
Method Colonies assay
Cell Lines HeLa, U2OS, and 1BR-hTERT cells
Concentrations 1 μM
Incubation Time 8 h or 24 h
Results With 24-hour treatment of VE-821, HeLa and U2OS cells were significantly radiosensitized by both kinds of radiation, while little was observed in irradiated 1BR-hTERT cells by the inhibitor
Cell Experiment
Cell lines MiaPaCa-2, PSN-1 and Panc1 cells
Preparation method Cell viability assays MiaPaCa-2, PSN-1 and Panc1 (5 x 104) were plated in 96-well plates and after 4 h treated with increasing concentrations of VE-821 at 1 h before irradiation with a single dose of 4 Gy. Medium was replaced 72 h post-irradiation at which point viability was measured using the using the Alamar Blue assay (Resazurin substrate, SIGMA). Cells were allowed to proliferate and cell viability was again analyzed at day 10 for the different treatment conditions. Cell viability and surviving fraction were normalized to the untreated (control) group.
Concentrations 0~9µM
Incubation time 72h
Animal Experiment
Animal models mice bearing PSN-1 xenografts
Formulation 10% Vitamin E d-alpha tocopheryl polyethylene glycol 1000 succinate and administered by gavage, in 200 μl.
Dosages 60 mg/Kg on days 0 and 1
Administration oral gavage
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 368.41
Formula C18H16N4O3S
CAS Number 1232410-49-9
Purity 98.27%
Solubility DMSO 60 mg/mL
Storage at -20°C

[1] Prevo R, et al. Cancer Biol Ther. The novel ATR inhibitor VE-821 increases sensitivity of pancreatic cancer cells to radiation and chemotherapy.

[2] Pires IM, et al. Br J Cancer. Targeting radiation-resistant hypoxic tumour cells through ATR inhibition.

Related ATM/ATR Products

Gartisertib (VX-803) is an ATP-competitive, orally active, selective ATR inhibitor with Ki<150 pM. Gartisertib inhibits atR-driven phosphorylation of checkpoint kinase-1 (Chk1) with an IC50 value of 8 nM. It has antitumor activity.


RP-3500 (ATR inhibitor 4) is an orally potent, selective ATR kinase inhibitor (ATRi) in biochemical assays IC50 1.00 nM. The RP-3500 is 30 times more selective to ATR (IC).50=120 nM), which is 2,000 times > ATM, DNA-PK, and PI3Kα kinase.


AZ32 is an orally bioavailable and blood-brain barrier-(BBB)penetrating inhibitor of ATM with IC50 of <6.2 nM and 0.31 μM for ATM enzyme in cell.


AZD0156 is a potent, selective and orally active ATM inhibitor with an IC50 of 0.58 nM. AZD0156 inhibits ATM mediated signal transduction, prevents DNA damage checkpoint activation, damages DNA damage repair, and induces tumor cell apoptosis.


AZD1390 is currently the most effective and highly selective ATM inhibitor with an IC50 of 0.78 nM, oral activity and the ability to cross the blood-brain barrier. In vivo, AZD1390 combined with radiotherapy effectively inhibited tumor growth.

Abmole Inhibitor Catalog

Keywords: VE-821 supplier, ATM/ATR, inhibitors

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.