Art. -Nr.: HY-112090

ABBV-744

11 Cited Publications

Kundenbewertung

Based on 11 publication(s) in Google Scholar

ABBV-744 is a first-in-class, orally active and selective inhibitor of the BDII domain of BET family proteins with IC₅₀ values ranging from 4 to 18 nM for BRD2, BRD3, BRD4 and BRDT. ABBV-744 is primarily metabolized by CYP3A4 with agent-like properties enable the investigation of its antitumor efficacy and tolerability.

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Reinheit: 99.97%
CAS. Nr.: 2138861-99-9
Formel: C₂₈H₃₀FN₃O₄
Molecular Weight:491.55

Speicherung:

4°C, stored under nitrogen

* In solvent : -80°C, 1 year; -20°C, 6 months (stored under nitrogen)

ABBV-744 Chemical Structure

CAS. Nr.: 2138861-99-9

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (11)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

BRD2 (BD2)

8 nM (IC₅₀)

BRD3 (BD2)

13 nM (IC₅₀)

BRDT (BD2)

18 nM (IC₅₀)

BRD4 (BD2)

4 nM (IC₅₀)

BRD4 (BD2)

3 nM (Kd)

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Cellular Effect

Cell Line	Type	Value	Description	References
HeLa	IC₅₀	20700 nM Compound: 46; ABBV-744	Inhibition of NanoLuc-tagged BRD4 BD1 (unknown origin) expressed in human HeLa cells after 2 hrs by NanoBRET assay Inhibition of NanoLuc-tagged BRD4 BD1 (unknown origin) expressed in human HeLa cells after 2 hrs by NanoBRET assay	[PMID: 32324999]
HeLa	IC₅₀	27.5 nM Compound: 46; ABBV-744	Inhibition of NanoLuc-tagged BRD4 BD2 (unknown origin) expressed in human HeLa cells after 2 hrs by NanoBRET assay Inhibition of NanoLuc-tagged BRD4 BD2 (unknown origin) expressed in human HeLa cells after 2 hrs by NanoBRET assay	[PMID: 32324999]
MOLM-13	IC₅₀	0.039 μM Compound: 10; ABBV-744	Antiproliferative activity against human MOLM-13 cells assessed as inhibition of cell proliferation incubated for 72 hrs by CellTiterGlo luminescence assay Antiproliferative activity against human MOLM-13 cells assessed as inhibition of cell proliferation incubated for 72 hrs by CellTiterGlo luminescence assay	[PMID: 38175809]
MV4-11	IC₅₀	0.015 μM Compound: 10; ABBV-744	Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell proliferation incubated for 72 hrs by CellTiterGlo luminescence assay Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell proliferation incubated for 72 hrs by CellTiterGlo luminescence assay	[PMID: 38175809]
MV4-11	IC₅₀	0.04 μM Compound: ABBV-744	Antiproliferative activity against human MV4-11 cells assessed as reduction in cell growth Antiproliferative activity against human MV4-11 cells assessed as reduction in cell growth	[PMID: 38964169]
MV4-11	IC₅₀	0.25 μM Compound: ABBV-744	Antiproliferative activity against human MV4-11 cells assessed as cell viability after 72 hrs by CCK8 assay Antiproliferative activity against human MV4-11 cells assessed as cell viability after 72 hrs by CCK8 assay	[PMID: 33077265]
MV4-11	IC₅₀	152.67 nM Compound: ABBV-744	Antiproliferative activity against human MV4-11 cells incubated for 72 hrs by CCK8 assay Antiproliferative activity against human MV4-11 cells incubated for 72 hrs by CCK8 assay	[PMID: 35395439]
NCI-H1299	IC₅₀	1600 nM Compound: 46; ABBV-744	Antiproliferative activity against human H1299 cells assessed as reduction in cell viability after 5 days by CellTiter-Glo assay Antiproliferative activity against human H1299 cells assessed as reduction in cell viability after 5 days by CellTiter-Glo assay	[PMID: 32324999]
SKM-1	IC₅₀	6.7 nM Compound: 46; ABBV-744	Antiproliferative activity against human SKM1 cells assessed as reduction in cell viability after 5 days by CellTiter-Glo assay Antiproliferative activity against human SKM1 cells assessed as reduction in cell viability after 5 days by CellTiter-Glo assay	[PMID: 32324999]

In Vitro

ABBV-744 (90 nM; 0~24 h; LNCaP cells) downregulates the expression of KLK2 and MYC genes^[1].
? ABBV-744 (90 nM; 0~72 h; LNCaP cells) induces cell cycle arrest in G1 followed by senescence^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[1]

Cell Line:

LNCaP cells
Concentration:

90 nM
Incubation Time:

0~24 hours
Result:

Downregulated the expression of KLK2 and MYC genes.

Cell Cycle Analysis^[1]

Cell Line:

LNCaP cells
Concentration:

90 nM
Incubation Time:

0~72 hours
Result:

Induced cell cycle arrest in G1 followed by senescence.

In Vivo

ABBV-744 (4.7 mg/kg; oral gavage; 28 days) causes a delay in tumor growth and displays equivalent or better antitumor activity compared with ABBV-075^[1].
? ABBV-744 (30 mg/kg; 14 days) is able to produce significant antitumor activity. ABBV-744 (30 mg/kg) triggers a reduction in platelets of only 20 %^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Mice
Dosage:

4.7 mg/kg (Pharmacokinetic Analysis)
Administration:

Oral gavage; 28 days
Result:

Caused a delay in tumor growth and displayed equivalent or better antitumor activity compared with ABBV-075.

Animal Model:

Sprague-Dawley rats
Dosage:

30 mg/kg (Pharmacokinetic Analysis)
Administration:

14 days
Result:

Produced significant antitumor activity.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 2138861-99-9
Appearance Solid
Molecular Weight 491.55
Formel C₂₈H₃₀FN₃O₄
Color White to light yellow
SMILES

CC(O)(C)C1=CC(C(C2=C3NC(C(NCC)=O)=C2)=CN(C)C3=O)=C(OC4=C(C)C=C(F)C=C4C)C=C1
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, stored under nitrogen

* In solvent : -80°C, 1 year; -20°C, 6 months (stored under nitrogen)

Publications (11)

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Journal Impact Factor

Science

Selective targeting of BD1 and BD2 of the BET proteins in cancer and immunoinflammation. [Abstract]

2020 Apr 24;368(6489):387-394. PMID: 32193360
Cell

BET inhibition blocks inflammation-induced cardiac dysfunction and SARS-CoV-2 infection. [Abstract]

2021 Apr 15;184(8):2167-2182.e22. PMID: 33811809
Nat Commun

Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]

2026 Feb 12;17(1):1214. PMID: 41680175
Acta Pharmacol Sin

ABBV-744 alleviates LPS-induced neuroinflammation via regulation of BATF2-IRF4-STAT1/3/5 axis. [Abstract]

2024 Oct;45(10):2077-2091. PMID: 38862817

ABBV-744 purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2024 Oct;45(10):2077-2091. [Abstract]

BV-2 cells were pretreated with ABBV-744 (0.003, 0.01, 0.03, 0.1, 0.3, 1, 3, 10 μM) for 2 h and then exposed to LPS (100 ng/mL) for 24 h (n = 5). The production of NO was measured using nitric oxide detection kit.

ABBV-744 purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2024 Oct;45(10):2077-2091. [Abstract]

BV-2 cells were pretreated with ABBV-744 (0.003, 0.01, 0.03, 0.1, 0.3, 1, 3, 10 μM) for 2 h and then exposed to LPS (100 ng/mL) for 24 h (n = 5). The levels of pro-inflammatory factors TNF-α and IL-6 were measured using ELISA.

ABBV-744 purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2024 Oct;45(10):2077-2091. [Abstract]

BV-2 cells were pretreated with ABBV-744 (0.01, 0.03, 0.1 μM) for 2 h and then exposed to LPS (100 ng/mL) for 3 h (n = 5). The mRNA levels of TNF-α, IL-1β and IL-6 were measured by quantitative real-time PCR.

ABBV-744 purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2024 Oct;45(10):2077-2091. [Abstract]

BV-2 cells were pretreated with ABBV-744 (0.01, 0.03, 0.1 μM) for 2 h and then exposed to LPS (100 ng/mL) for 24 h (n = 5). The protein levels of iNOS, COX2 and α-tubulin were measured using immunoblot analysis.

ABBV-744 purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2024 Oct;45(10):2077-2091. [Abstract]

Primary microglial cells were pretreated with ABBV-744 (0.03 μM) for 2 h and then exposed to LPS (100 ng/mL) for 3 h (n = 5). The mRNA levels of TNF-α, IL-1β, and IL-6 were measured by quantitative real-time PCR.

ABBV-744 purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2024 Oct;45(10):2077-2091. [Abstract]

C57BL/6J mice were treated with vehicle (5% DMSO + 40% PEG300 + 55% saline; p.o.) or ABBV-744 (0.05, 0.1, 0.2 mg/kg; p.o.) daily for 2 days, followed by injection with saline or LPS (5 mg/kg; i.p.) for 1 day. Activation of microglia in the CA1 region of mice hippocampus was detected by immunofluorescence staining using an anti-Iba1 antibody.

ABBV-744 purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2024 Oct;45(10):2077-2091. [Abstract]

C57BL/6J mice were treated with vehicle (5% DMSO + 40% PEG300 + 55% saline; p.o.) or ABBV-744 (0.05, 0.1, 0.2 mg/kg; p.o.) daily for 2 days, followed by injection with saline or LPS (5 mg/kg; i.p.) for 1 day. The mRNA levels of TNF-α and IL-1β in the hippocampus were measured by quantitative real-time PCR (n = 7–8).

ABBV-744 purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2024 Oct;45(10):2077-2091. [Abstract]

BV-2 cells were pretreated with ABBV-744 (0.03 μM) for 2 h and then exposed to LPS (100 ng/mL) for 3 h (n = 4–5). The mRNA levels of BATF2 and IRF4 were measured by quantitative real-time PCR.

ABBV-744 purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2024 Oct;45(10):2077-2091. [Abstract]

BV-2 cells were pretreated with ABBV-744 (0.03 μM) for 2 h and then exposed to LPS (100 ng/mL) for 15 min (n = 5). The protein level of BATF2 was measured by Western blot. The quantification of the intensity of BATF2 relative to β-actin is shown.

ABBV-744 purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2024 Oct;45(10):2077-2091. [Abstract]

BV-2 cells were pretreated with ABBV-744 (0.03 μM) for 2 h and then exposed to LPS (100 ng/mL) for 3 h (n = 6–7). Protein levels of p-STAT3 and STAT3, p-STAT5 and STAT5 were measured by Western blot and β-actin or GAPDH were used as a loading control.

ABBV-744 purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2024 Oct;45(10):2077-2091. [Abstract]

C57BL/6J mice were treated with vehicle (5% DMSO + 40% PEG300 + 55% saline; p.o.) or ABBV-744 (0.1 mg/kg; p.o.) daily for 2 days, followed by injection with saline or LPS (5 mg/kg; i.p.) for 1 day. Protein levels of BATF2 and IRF4 were measured by Western blot and β-actin was used as a loading control.
Sci Data

High-throughput drug screening identifies novel therapeutics for Low Grade Serous Ovarian Carcinoma. [Abstract]

2024 Sep 19;11(1):1024. PMID: 39300112
Sci Rep

Epigenetic modulation through BET bromodomain inhibitors as a novel therapeutic strategy for progranulin-deficient frontotemporal dementia. [Abstract]

2024 Apr 20;14(1):9064. PMID: 38643236
Cancer Med

Focal Adhesion Kinase Intersects With the BRD4-MYC Axis and YAP1 to Drive Tumor Cell Growth, Phenotypic Plasticity, Stemness, and Metastatic Potential in Colorectal Cancer. [Abstract]

2025 Sep;14(18):e71227. PMID: 40959971
J Leukoc Biol

BET inhibition curbs macrophage inflammation, lipid accumulation, and atherogenesis by disrupting the YAP/TAZ-BRD4 axis. [Abstract]

2026 Apr 29:qiag017. PMID: 42054500
Anal Sens

22 June 2022.
Harvard University

2026.
bioRxiv

2025 Sep 21.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (203.44 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.0344 mL

10.1719 mL

20.3438 mL

5 mM

0.4069 mL

2.0344 mL

4.0688 mL

10 mM

0.2034 mL

1.0172 mL

2.0344 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (stored under nitrogen). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (5.09 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (5.09 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.09 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Protocol 4

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline

Solubility: ≥ 2 mg/mL (4.07 mM); Clear solution

Protocol 5

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)

Solubility: ≥ 2 mg/mL (4.07 mM); Clear solution

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 50% PEG300 50% Saline

Solubility: 2.5 mg/mL (5.09 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (285 KB)
SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Faivre EJ, et al. Selective inhibition of the BD2 bromodomain of BET proteins in prostate cancer. Nature. 2020;578(7794):306-310. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.0344 mL	10.1719 mL	20.3438 mL	50.8595 mL
	5 mM	0.4069 mL	2.0344 mL	4.0688 mL	10.1719 mL
	10 mM	0.2034 mL	1.0172 mL	2.0344 mL	5.0860 mL
	15 mM	0.1356 mL	0.6781 mL	1.3563 mL	3.3906 mL
	20 mM	0.1017 mL	0.5086 mL	1.0172 mL	2.5430 mL
	25 mM	0.0814 mL	0.4069 mL	0.8138 mL	2.0344 mL
	30 mM	0.0678 mL	0.3391 mL	0.6781 mL	1.6953 mL
	40 mM	0.0509 mL	0.2543 mL	0.5086 mL	1.2715 mL
	50 mM	0.0407 mL	0.2034 mL	0.4069 mL	1.0172 mL
	60 mM	0.0339 mL	0.1695 mL	0.3391 mL	0.8477 mL
	80 mM	0.0254 mL	0.1271 mL	0.2543 mL	0.6357 mL
	100 mM	0.0203 mL	0.1017 mL	0.2034 mL	0.5086 mL

Keywords

ABBV-744

11 Cited Publications

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ABBV-744

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Chemical Probe Library

Anti-Blood Cancer Compound Library

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Anti-Hematopathy Compound Library

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Histone Modification Research Compound Library

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Clinical Compound Library

Antiviral Compound Library

Publications Citing Use of MedChemExpress (MCE) ABBV-744

Alle Epigenetic Reader Domain Isoform-spezifische Produkte anzeigen

Alle HIV Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (11)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

ABBV-744

Reprogramming Compound Library

Orally Active Compound Library

Chemical Probe Library

Anti-Blood Cancer Compound Library

Highly Selective Inhibitors Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Anti-Infection Compound Library

Epigenetics Compound Library

Immunology/Inflammation Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Antiviral Compound Library

Publications Citing Use of MedChemExpress (MCE) ABBV-744

Alle Epigenetic Reader Domain Isoform-spezifische Produkte anzeigen

Alle HIV Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (11)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

ABBV-744 Related Classifications

HY-112090 Related Classifications