Fig. 1 · Structure

Cat. No.: A11243
CAS No.: 1207456-01-6
Formula: C₁₉H₁₄F₂N₆O
Mol. Weight: 380.35

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Talazoparib (BMN673)

Name: Talazoparib (BMN673)
Brand: Adooq Bioscience
SKU: A11243
Availability: InStock
Rating: 5 (2 reviews)

Cat. No. A11243 CAS 1207456-01-6

PARP inhibitor

BMN-673 is an orally bioavailable inhibitor of the nuclear enzyme poly(ADP-ribose) polymerase (PARP) with potential antineoplastic activity.

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Biological Activity

Bioactivity / Mechanism

Talazoparib (BMN 673) inhibits PARP1/2 catalytic activity. Shen et al. reported a PARP1 enzyme IC50 of 0.57 nM and Ki values of 1.20 nM (PARP1) and 0.85 nM (PARP2). In DNA-damaged cells, BMN 673 also promoted chromatin-associated PARP trapping; this cellular effect is distinct from catalytic inhibition. [1,2]

Literature-reported observations and conditions; not Adooq-tested protocols or general treatment recommendations.

Target & Activity

Target	Activity	Value
PARP (Cell-free assay)		0.58 nM

Cellular Effect

Cell Line	Activity	Value	Description	Reference
CAPAN-1	IC50	1.8 nM	Antiproliferative activity against human Capan1 cells after 7 days by CCK8 or SRB assay	[PMID: 28692916]
DLD-1	IC50	0.002 μM	Antiproliferative activity against human DLD-1 deficient in BRCA-2 cells measured after 7 days	[PMID: 34570508]
LoVo	EC50	2.5 nM	Inhibition of PARP in human LoVo cells assessed as inhibition of hydrogen peroxide-induced PARylation treated for 30 mins prior to incubation with H2O2 for 5 mins by fluorescence analysis	[PMID: 25761096]
LoVo	EC50	2.51 nM	Inhibition of PARP in human LoVo cells assessed as inhibition of poly(ADP)-ribose polymerization for 30 mins by fluorescence assay	[PMID: 26652717]
LoVo	GI50	4 nM	Potentiation of temozolomide-induced cytotoxicity in human LoVo cells assessed as temozolomide GI50 at 0.4 uM after 5 days by Celltiter-Glo assay	[PMID: 26652717]
MDA-MB-436	IC50	0.012 nM	Cytotoxicity against human MDA-MB-436 cells assessed as inhibition of cell viability incubated for 14 days with three intermittent intervals by CellTiterGlo luminescence assay	[PMID: 33120078]
MDA-MB-436	IC50	0.38 nM	Cytotoxicity against human MDA-MB-436 cells assessed as inhibition of cell viability incubated for 4 days by CellTiterGlo luminescence assay	[PMID: 33120078]
MDA-MB-436	IC50	0.7 nM	Antiproliferative activity against human MDA-MB-436 cells after 7 days by CCK8 or SRB assay	[PMID: 28692916]
SUM149PT	EC50	1.6 nM	Cytotoxicity against BRCA1-deficient human SUM149 cells measured after 6 days by microscopic analysis	[PMID: 31042381]
SUM149PT	EC50	23.2 nM	Cytotoxicity against BRCA1-proficient human SUM149 cells measured after 6 days by microscopic analysis	[PMID: 31042381]
V79	IC50	5011.4 nM	Cytotoxicity against BRCA2 expressing Chinese hamster V79 cells after 3 days by CCK8 or SRB assay	[PMID: 28692916]

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In Vitro Studies

In MMS-treated DT40 and DU145 cells, 0.1 μM BMN 673 produced PARP trapping comparable to 10 μM olaparib. This comparison reflects a chromatin-fraction assay under induced DNA damage. Single-agent sensitivity remained heterogeneous across NCI60: the authors reported that approximately half the cell lines were resistant even at 100 μM. [2]

PARP1/2 catalytic inhibition

Biochemical assay · PARP1 and PARP2 enzyme assays [1]

BMN 673 inhibited PARP catalytic activity; potency depends on assay and stereochemistry.

Measured endpoints — not treatment concentrations
Endpoint	Reported result	Reference
PARP1 enzyme activity	IC50 0.57 nM	[1]
Enzymatic inhibition constants	Ki PARP1: 1.20 nM; PARP2: 0.85 nM	[1]

Literature-Reported Treatment Conditions

Method: Cell-free catalytic assays
Vehicle: DMSO stock solutions
Reported limits: IC50 assay concentration series and incubation duration are not specified in the retrieved main-text description. Ki assay timing is separate from the IC50 assay.

Methods and source locations

Compound reported in the paper: Talazoparib (BMN 673); Compound label in the paper: BMN 673

Evidence concerns the paper-tested material; it does not validate a current Adooq lot.

Results: BMN 673 discovery; Figure 1A; Table 1; Methods: PARP enzyme assays, Drugs and cell lines

PARP1 enzyme activity: Trevigen PARP assay; Table 1 values average 3–4 independent experiments. — Table 1 (PARP1 enzyme inhibition column), caption; Figure 1A; Methods: PARP enzyme assays

Enzymatic inhibition constants: Radiometric enzyme assay; Ki calculated using substrate concentration and Km. — Results paragraph following Table 1; Methods: PARP enzyme assays

Chromatin-associated PARP trapping

Cell-based study · Chicken DT40 and human DU145 prostate cancer cells [2]

Under MMS-induced DNA damage, BMN 673 trapped PARP on chromatin at lower concentrations than olaparib.

Measured endpoints — not treatment concentrations
Endpoint	Reported result	Reference
Chromatin-bound PARP1 (DT40/DU145) and PARP2 (DU145)	Comparative trapping 0.1 μM BMN 673 produced trapping comparable to 10 μM olaparib (authors’ approximately 100-fold comparison).	[2]

Literature-Reported Treatment Conditions

Treatment concentration: 0.1, 1 and 10 μM BMN 673
Exposure duration: DT40: 30 min; DU145: 4 h
Method: Cell treatment followed by chromatin fractionation and immunoblotting
Vehicle: DMSO stock; final DMSO fraction not specified in the selected description
Co-treatment: 0.01% methyl methanesulfonate (MMS) to induce DNA damage
Reported limits: Exact replicate count and densitometric uncertainty not specified. This is a damage-conditioned trapping assay, not a monotherapy survival IC50.

Methods and source locations

Compound reported in the paper: Talazoparib (BMN 673); Compound label in the paper: BMN 673

Evidence concerns the paper-tested material; it does not validate a current Adooq lot.

Figure 4A-B and caption; Results: BMN 673 traps PARP-DNA complexes; Methods: Immunoblotting, Cell lines and drug treatments

Chromatin-bound PARP1 (DT40/DU145) and PARP2 (DU145): Chromatin fraction immunoblot; histone H3 loading/fraction control; no-PARP-inhibitor lanes. Representative blots from multiple experiments, exact n unspecified. — Figure 4A-B image/caption; adjacent Results

Heterogeneous sensitivity across NCI60

Cell-based study · NCI60 human cancer cell-line panel [2]

BMN 673 sensitivity varied markedly across the panel; biochemical potency did not imply universal cell killing.

Measured endpoints — not treatment concentrations
Endpoint	Reported result	Reference
Cell survival sensitivity across NCI60	IC50 sensitivity pattern Authors report approximately half of NCI60 cell lines resistant even at 100 μM BMN 673.	[2]

Literature-Reported Treatment Conditions

Treatment concentration: Figure 3 extends to 100 μM; individual cell-line IC50 values are not digitized.
Method: Single-agent NCI60 panel sensitivity analysis
Co-treatment: None in this panel
Reported limits: Panel-specific exposure duration, vehicle and replicate count are referenced to standard NCI procedures rather than specified in the selected main text; the separate 72-h ATP assay is not assigned to this panel.

Methods and source locations

Compound reported in the paper: Talazoparib (BMN 673); Compound label in the paper: BMN 673

Evidence concerns the paper-tested material; it does not validate a current Adooq lot.

Figure 3 image/caption; Results following Figure 2D; Discussion: NCI60 resistance; Methods: Measurement of cellular sensitivity

Cell survival sensitivity across NCI60: NCI Developmental Therapeutics Program panel data; Figure 3 defines IC50 as concentration reducing cell survival to 50%; NA denotes unavailable data. — Figure 3/caption; Discussion paragraph beginning “Our results provide relevant information”

In Vivo Studies

In the MX-1 xenograft schedule comparison, oral BMN 673 for 28 days produced complete responses in 4/6 mice at 0.33 mg/kg once daily and 6/6 at 0.165 mg/kg per dose twice daily. Tumors regrew after once-daily treatment ceased; the twice-daily cohort had no regrowth during the displayed follow-up. One twice-daily-treated mouse lost >20% body weight and was sacrificed on day 53. The paper does not resolve the exact post-treatment follow-up duration consistently. [1]

Single-agent dosing schedules in MX-1 xenografts

Animal study · BRCA1-deficient MX-1 mammary tumor xenografts in female athymic nu/nu mice (8–10 weeks) [1]

QD and BID regimens both induced regression; only the BID cohort maintained complete responses through the reported follow-up, with one substantial weight-loss event.

Conditions shared by the study groups

Route: Oral gavage (p.o.)
Treatment course: 28 consecutive days
Vehicle: 10% DMAc, 6% Solutol, 84% PBS

Study groups and reported outcomes
Group / dose	Comparator	Observed result	Reference
Once-daily BMN 673 0.33 mg/kg/dose	Vehicle-QD group in Figure 3C; six mice per active-treatment cohort	4/6 complete responses; tumors eventually re-established after treatment cessation.	[1]
Twice-daily BMN 673 0.165 mg/kg/dose	Vehicle-QD group in Figure 3C; six mice per active-treatment cohort	6/6 complete responses; no tumor re-establishment during the displayed follow-up. One of six mice lost >20% body weight and was sacrificed on day 53.	[1]

Once-daily BMN 673: Model: BRCA1-deficient MX-1 mammary tumor xenografts in female athymic nu/nu mice (8–10 weeks); Frequency: Once daily; Reported limits: Exact animal-level tumor trajectories are not provided in the median-volume plot.

Twice-daily BMN 673: Model: BRCA1-deficient MX-1 mammary tumor xenografts in female athymic nu/nu mice (8–10 weeks); Frequency: Twice daily; Reported limits: Exact animal-level tumor trajectories are not provided in the median-volume plot.

Methods and source locations

Compound reported in the paper: Talazoparib (BMN 673); Compound label in the paper: BMN 673

Evidence concerns the paper-tested material; it does not validate a current Adooq lot.

Figure 3C/caption; Results: Anti-tumor effect of oral BMN 673 (QD versus BID comparison); Methods: Xenograft experiments

Once-daily BMN 673 · Figure 3C image/caption; adjacent QD-versus-BID Results; Methods: Xenograft experiments

Twice-daily BMN 673 · Figure 3C image/caption; adjacent QD-versus-BID Results; Methods: Xenograft experiments

Specifications

Manufacturer	Adooq Bioscience
Actions	Inhibitor
CAS Number	1207456-01-6
Applications	PARP inhibitor
Formula	C₁₉H₁₄F₂N₆O
Molecular Weight	380.35
Synonyms	BMN-673; LT-673
SMILES	CN1C(=NC=N1)[C@@H]2[C@H](N=C3C=C(C=C4C3=C2NNC4=O)F)C5=CC=C(C=C5)F

Storage & Solubility

In Vitro Solubility

Reported Solubility

Solvent	Reported Solubility
DMSO	Warmed: 38 mg/mL (99.9 mM)
Water	Insoluble
Ethanol	Insoluble

Preparing Stock Solutions

Stock preparation is unavailable for this product molecular weight.

Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.

Storage

Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

Research References

[1] Shen Y, Rehman FL, Feng Y, et al. BMN 673, a novel and highly potent PARP1/2 inhibitor for the treatment of human cancers with DNA repair deficiency Clin Cancer Res (2013). PMID: 23881923 DOI: 10.1158/1078-0432.ccr-13-1391 Source material
[2] Murai J, Huang SY, Renaud A, et al. Stereospecific PARP trapping by BMN 673 and comparison with olaparib and rucaparib Mol Cancer Ther (2014). PMID: 24356813 DOI: 10.1158/1535-7163.mct-13-0803 Source material

Publications

2 publications citing this product

Subhajit Chatterjee, .et al. , J Cancer Res Clin Oncol, 2022, Dec;148(12):3521-3535 PMID: 35962813
Charles-André Philip, .et al. , BMC Cancer, 2017, 17: 638 PMID: 28886696

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