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ABT-888 2HCl

(CAS No:912444-00-9)

Veliparib (ABT-888) is a potent inhibitor of PARP1 and PARP2 with Ki of 5.2 nM and 2.9 nM in cell-free assays, respectively. It is inactive to SIRT2. Phase 3.

CAS No:912444-00-9

Molecular Weight(MW):244.29

Purity:98%+

Specification:500mg;1g;5g;10g;50g;100g

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QC Documents

COA	MSDS	HPLC	NMR

ChemicalInfomation

CAS No:	912444-00-9
Molecular formula(MF)	C₁₃H₁₆N₄O
Molecular Weight(MW):	244.29
Alias

Solubility

In vitro	DMSO	17 mg/mL (69.58 mM)
	Water	<1 mg/mL
	Ethanol	<1 mg/mL
In vivo	0.5% methylcellulose+0.2% Tween 80	5 mg/mL

Biological Activity

Description

Veliparib (ABT-888) is a potent inhibitor of PARP1 and PARP2 with K_i of 5.2 nM and 2.9 nM in cell-free assays, respectively. It is inactive to SIRT2. Phase 3.

Features

Increases the efficacy of common cancer therapies such as radiation and alkylating agents.

Targets

PARP2 ^[1] (Cell-free assay)	PARP1 ^[1] (Cell-free assay)
2.9 nM(Ki)	5.2 nM(Ki)

In vitro

ABT-888 is inactive to SIRT2 (>5 μM). ^[1] ABT-888 inhibits the PARP activity with EC50 of 2 nM in C41 cells. ^[2] ABT-888 could decrease the PAR levels in both irradiated and nonirradiated H460 cells. ABT-888 also reduces clonogenic survival and inhibits DNA repair by PARP-1 inhibition in H460 cells. ABT-888 increases apoptosis and autophagy in H460 cells when combination with radiation. ^[3] ABT-888 also inhibits PARP activity in H1299, DU145 and 22RV1 cells and the inhibition is independent of p53 function. ABT-888 (10 μM) suppresses the surviving fraction (SF) by 43% in the clonogenic H1299 cells. ABT-888 shows effective radiosensitivity in oxic H1299 cells. Furthermore, ABT-888 could attenuate the SF of hypoxic-irradiated cells including H1299, DU145 and 22RV1. ^[4]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID
C41	Kinase Assay		30 min		Inhibition of PARP1 with EC50 of 0.002 Î¼M	19888760
Jurkat	Kinase Assay		96 h	DMSO	Inhibition of PARP1 assessed as reduction of cell viability with EC50 of 3 Î¼M	23850199
Capan1	Growth Inhibition Assay		72 h	DMSO	Antiproliferative activity against BRCA2 gene mutated human Capan1 cells with IC50 of 39.7 Î¼M	24398383
DT40	Cytotoxic Assay		72 h	DMSO	Cytotoxicity against chicken BRCA2-deficient DT40 cells	24922587
ML-1	Apoptotic Assay	2.5 Î¼M	24 h	DMSO	Synergistically enhances TRAIL-induced apoptosis in ML-1 cells	24895135
HCT-116	Kinase Assay	0.5 Î¼M	24 h		PARP activity decreases	23054213
UM-SCC1	Cytotoxic Assay	10 Î¼M	24 h		Reduces the cell viability	21912620
FaDu	Cytotoxic Assay	10 Î¼M	24 h		Reduces the cell viability	21912620
PC-3	Growth Inhibition Assay	10 Î¼M			Induces a significant inhibition in colony formationÂ	21571912
EoL-1-cell	Growth Inhibition Assay				IC50=1.0798 Î¼M	SANGER
NCI-SNU-5	Growth Inhibition Assay				IC50=3.12841 Î¼M	SANGER
BV-173	Growth Inhibition Assay				IC50=5.45409 Î¼M	SANGER
HCC1806	Growth Inhibition Assay				IC50=5.75173 Î¼M	SANGER
COLO-680	Growth Inhibition Assay				IC50=6.21406 Î¼M	SANGER
HCC2218	Growth Inhibition Assay				IC50=7.79704 Î¼M	SANGER
SK-MEL-24	Growth Inhibition Assay				IC50=7.81924 Î¼M	SANGER
NCI-H720	Growth Inhibition Assay				IC50=8.43603 Î¼M	SANGER
KASUMI-1	Growth Inhibition Assay				IC50=8.89266 Î¼M	SANGER
HAL-01	Growth Inhibition Assay				IC50=9.8862 Î¼M	SANGER
CAL-33	Growth Inhibition Assay				IC50=10.434 Î¼M	SANGER
SK-MEL-1	Growth Inhibition Assay				IC50=12.4663 Î¼M	SANGER
Ramos-2G6-4C10	Growth Inhibition Assay				IC50=12.4752 Î¼M	SANGER
KY821	Growth Inhibition Assay				IC50=12.485 Î¼M	SANGER
HEC-1	Growth Inhibition Assay				IC50=12.9196 Î¼M	SANGER
SK-NEP-1	Growth Inhibition Assay				IC50=13.166 Î¼M	SANGER
MN-60	Growth Inhibition Assay				IC50=13.5389 Î¼M	SANGER
DU-145	Growth Inhibition Assay				IC50=13.9053 Î¼M	SANGER
EW-3	Growth Inhibition Assay				IC50=14.5565 Î¼M	SANGER
OS-RC-2	Growth Inhibition Assay				IC50=15.9589 Î¼M	SANGER
RPMI-8226	Growth Inhibition Assay				IC50=16.2042 Î¼M	SANGER
ChaGo-K-1	Growth Inhibition Assay				IC50=16.5325 Î¼M	SANGER
DEL	Growth Inhibition Assay				IC50=16.6717 Î¼M	SANGER
GP5d	Growth Inhibition Assay				IC50=17.053 Î¼M	SANGER
COLO-668	Growth Inhibition Assay				IC50=17.6294 Î¼M	SANGER
H9	Growth Inhibition Assay				IC50=18.2833 Î¼M	SANGER
NKM-1	Growth Inhibition Assay				IC50=18.5119 Î¼M	SANGER
KYSE-150	Growth Inhibition Assay				IC50=18.9986 Î¼M	SANGER
Daoy	Growth Inhibition Assay				IC50=19.5649 Î¼M	SANGER
ECC10	Growth Inhibition Assay				IC50=20.7455 Î¼M	SANGER
A388	Growth Inhibition Assay				IC50=21.9091 Î¼M	SANGER
MHH-NB-11	Growth Inhibition Assay				IC50=23.1363 Î¼M	SANGER
HCC1937	Growth Inhibition Assay				IC50=24.746 Î¼M	SANGER
TGBC11TKB	Growth Inhibition Assay				IC50=25.6863 Î¼M	SANGER
CTV-1	Growth Inhibition Assay				IC50=25.8969 Î¼M	SANGER
NCI-H2029	Growth Inhibition Assay				IC50=26.4238 Î¼M	SANGER
HLE	Growth Inhibition Assay				IC50=27.054 Î¼M	SANGER
NCI-H1693	Growth Inhibition Assay				IC50=27.2898 Î¼M	SANGER
HCC70	Growth Inhibition Assay				IC50=27.7246 Î¼M	SANGER
BEN	Growth Inhibition Assay				IC50=27.9566 Î¼M	SANGER
LB771	Growth Inhibition Assay				IC50=28.8373 Î¼M	SANGER
697	Growth Inhibition Assay				IC50=29.0235 Î¼M	SANGER
LU-139	Growth Inhibition Assay				IC50=29.3748 Î¼M	SANGER
EW-13	Growth Inhibition Assay				IC50=29.3814 Î¼M	SANGER
MOLT-13	Growth Inhibition Assay				IC50=29.3814 Î¼M	SANGER
L-363	Growth Inhibition Assay				IC50=29.4798 Î¼M	SANGER
EM-2	Growth Inhibition Assay				IC50=29.4901 Î¼M	SANGER
RS4-11	Growth Inhibition Assay				IC50=30.4241 Î¼M	SANGER
A2780	Growth Inhibition Assay				IC50=30.7457 Î¼M	SANGER
KU812	Growth Inhibition Assay				IC50=32.3642 Î¼M	SANGER
COLO-684	Growth Inhibition Assay				IC50=33.3599 Î¼M	SANGER
MFE-280	Growth Inhibition Assay				IC50=33.3889 Î¼M	SANGER
KG-1	Growth Inhibition Assay				IC50=33.6001 Î¼M	SANGER
JVM-3	Growth Inhibition Assay				IC50=35.5868 Î¼M	SANGER
MV-4-11	Growth Inhibition Assay				IC50=35.8499 Î¼M	SANGER
LAMA-84	Growth Inhibition Assay				IC50=36.7345 Î¼M	SANGER
MOLT-16	Growth Inhibition Assay				IC50=36.952 Î¼M	SANGER
H4	Growth Inhibition Assay				IC50=37.567 Î¼M	SANGER
T47D	Growth Inhibition Assay				IC50=37.7018 Î¼M	SANGER
CAL-54	Growth Inhibition Assay				IC50=37.966 Î¼M	SANGER
SW982	Growth Inhibition Assay				IC50=38.0998 Î¼M	SANGER
IGROV-1	Growth Inhibition Assay				IC50=39.3304 Î¼M	SANGER
NB14	Growth Inhibition Assay				IC50=40.7031 Î¼M	SANGER
HCC1187	Growth Inhibition Assay				IC50=41.2771 Î¼M	SANGER
SBC-1	Growth Inhibition Assay				IC50=41.3063 Î¼M	SANGER
KARPAS-45	Growth Inhibition Assay				IC50=41.4818 Î¼M	SANGER
MOLT-4	Growth Inhibition Assay				IC50=42.2538 Î¼M	SANGER
JVM-2	Growth Inhibition Assay				IC50=42.9207 Î¼M	SANGER
A4-Fuk	Growth Inhibition Assay				IC50=43.5691 Î¼M	SANGER
MDA-MB-361	Growth Inhibition Assay				IC50=43.8414 Î¼M	SANGER
BALL-1	Growth Inhibition Assay				IC50=43.9532 Î¼M	SANGER
T98G	Growth Inhibition Assay				IC50=44.8517 Î¼M	SANGER
Mo-T	Growth Inhibition Assay				IC50=45.6389 Î¼M	SANGER
MHH-PREB-1	Growth Inhibition Assay				IC50=45.7585 Î¼M	SANGER
ALL-PO	Growth Inhibition Assay				IC50=47.3791 Î¼M	SANGER
NCI-H510A	Growth Inhibition Assay				IC50=47.9034 Î¼M	SANGER
ML-2	Growth Inhibition Assay				IC50=49.7856 Î¼M	SANGER

... Click to View More Cell Line Experimental Data

In vivo

The oral bioavailability of ABT-888 is 56%-92% in mice, Sprague-Dawley rats, beagle dogs, and cynomolgus monkeys after oral administration. ^[1] ABT-888 (25 mg/kg i.p.) could improve tumor growth delay in a NCI-H460 xenograft model with well tolerated. Combination with radiation, ABT-888 decreases the tumor vessel formation. ^[3] ABT-888 reduces intratumor PAR levels by more than 95% at a dose of 3 and 12.5 mg/kg in A375 and Colo829 xenograft models and the suppression could be maintained over time. ^[4]