Cat. No.: HY-125542

DCZ3301

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DCZ3301 is an apoptosis inducer. DCZ3301 modulates JAK2/STAT3, ERK1/2, and PI3K/AKT pathways. DCZ3301 induces G2/M and M phase cell cycle arrest and inhibits cell proliferation and viability. DCZ3301 enhances DNA damage, inhibits DNA repair, and suppresses angiogenesis. DCZ3301 can be used for the research of diffuse large B-cell lymphoma, multiple myeloma and leukemia/lymphoma.

For research use only. We do not sell to patients.

Purity: 99.73%
CAS No.: 2136278-38-9
Formula: C₂₀H₁₆ClF₃N₆O₂
Molecular Weight:464.83

Storage:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

DCZ3301 Chemical Structure

CAS No.: 2136278-38-9

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

JAK2

p-STAT3

ERK1

ERK2

All JAK Isoforms :

All STAT Isoforms :

All ERK Isoforms :

All PI3K Isoforms :

All Akt Isoforms :

In Vitro

DCZ3301 (1-32 μM; 48 h) potently inhibits proliferation of OCI-LY8, NU-DUL-1, SUDHL-4, DB, and TMD8 DLBCL cell lines^[1].
DCZ3301 (1-32 μM; 24-72 h) inhibits proliferation of OCI-LY8 and NU-DUL-1 DLBCL cell lines in a time-dependent manner^[1].
DCZ3301 (2-20 μM; 48 h) inhibits proliferation of OCI-LY8 and NU-DUL-1 DLBCL cell lines in the presence of IL-6 or IGF-1, with its growth-inhibitory effect unaffected by these protumorigenic cytokines^[1].
DCZ3301 (4-20 μM; 24-72 h) induces dose- and time-dependent apoptosis in OCI-LY8 and NU-DUL-1 DLBCL cell lines^[1].
DCZ3301 (8-16 μM; 48 h) induces apoptosis in OCI-LY8 and NU-DUL-1 DLBCL cell lines via both extrinsic and intrinsic caspase-dependent pathways^[1].
DCZ3301 (4 μM; 8-24 h) induces time-dependent G2/M phase cell cycle arrest in OCI-LY8 and NU-DUL-1 DLBCL cell lines when treated with 4 μM for 8, 12, or 24 h^[1].
DCZ3301 (4-8 μM; 24 h) modulates cell cycle-related proteins (upregulating p-CHK2 and p21, downregulating cdc25A, cdc25C, and cyclinB1) in OCI-LY8 and NU-DUL-1 DLBCL cell lines^[1].
DCZ3301 (8-16 μM; 48 h) regulates the Akt, ERK1/2, and JAK2/STAT3 signaling pathways^[1].
DCZ3301 (4-8 μM; 48 h) has its antiproliferative effect enhanced in STAT3-knockdown OCI-LY8 and NU-DUL-1 DLBCL cell lines^[1].
DCZ3301 (8-16 μM; 12-48 h) inhibits Lyn phosphorylation (Y507) in a dose- and time-dependent manner, with a corresponding decrease in STAT3 phosphorylation, in OCI-LY8 and NU-DUL-1 DLBCL cell lines^[1].
DC₅₀Z3301 (8-16 μM; 48 h) modulates DNA repair-related protein expression in NCI-H929R and RPMI-8226R5 BTZ-resistant multiple myeloma cells after 48 hours of treatment^[2].
DCZ3301 (8 μM; 48 h) upregulates γ-H2A.X expression and induces γ-H2A.X foci formation in NCI-H929R and RPMI-8226R5 BTZ-resistant multiple myeloma cells, confirming enhanced DNA damage^[2].
DCZ3301 (5 μM; 24 h) suppresses the migration of human umbilical vein endothelial cells (HUVECs) in a wound healing assay^[5].

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

Cell Proliferation Assay^[1]

Cell Line:

OCI-LY8, NU-DUL-1, SUDHL-4, DB, TMD8 (diffuse large B-cell lymphoma cell lines)
Concentration:

1 μM; 2 μM; 4 μM; 8 μM; 16 μM; 32 μM
Incubation Time:

48 h
Result:

Caused a dose-dependent decrease in DLBCL cell proliferation.
Achieved IC₅₀ values of 7.1 μM (OCI-LY8), 9.7 μM (NU-DUL-1), 6.67 μM (SUDHL-4), 8.04 μM (DB), and 9.66 μM (TMD8).

Cell Proliferation Assay^[1]

Cell Line:

OCI-LY8, NU-DUL-1 (diffuse large B-cell lymphoma cell lines)
Concentration:

1 μM; 2 μM; 4 μM; 8 μM; 16 μM; 32 μM
Incubation Time:

24 h; 48 h; 72 h
Result:

Inhibited proliferation of OCI-LY8 and NU-DUL-1 cells in a time-dependent manner, with greater inhibition observed at longer incubation times.

Cell Proliferation Assay^[1]

Cell Line:

OCI-LY8, NU-DUL-1 (diffuse large B-cell lymphoma cell lines)
Concentration:

2 μM; 4 μM; 6 μM; 8 μM; 10 μM; 12 μM; 16 μM; 20 μM
Incubation Time:

48 h
Result:

Induced growth inhibition that was not altered by the presence of IL-6 or IGF-1, despite these cytokines alone stimulating DLBCL cell growth.

Apoptosis Analysis^[1]

Cell Line:

OCI-LY8, NU-DUL-1 (diffuse large B-cell lymphoma cell lines)
Concentration:

4 μM; 5 μM; 8 μM; 10 μM; 12 μM; 15 μM; 16 μM; 20 μM
Incubation Time:

24 h; 48 h; 72 h
Result:

Induced apoptosis in OCI-LY8 and NU-DUL-1 cells in a dose- and time-dependent manner.
Increased apoptosis rates with higher concentrations and longer incubation times, with statistically significant increases compared to controls.

Western Blot Analysis^[1]

Cell Line:

OCI-LY8, NU-DUL-1 (diffuse large B-cell lymphoma cell lines)
Concentration:

8 μM; 16 μM
Incubation Time:

48 h
Result:

Caused a dose-dependent increase in cleaved caspase-3, caspase-8, caspase-9, and PARP, while downregulating Bcl-2 and Bcl-xL and upregulating Bax.
Suppressed apoptosis in NU-DUL-1 cells when pre-incubated with pan-caspase inhibitor Z-VAD-FMK.

Cell Cycle Analysis^[1]

Cell Line:

OCI-LY8, NU-DUL-1 (diffuse large B-cell lymphoma cell lines)
Concentration:

4 μM
Incubation Time:

8 h; 12 h; 24 h
Result:

Caused a time-dependent accumulation of cells in the G2/M phase in both OCI-LY8 and NU-DUL-1 cell lines, with statistically significant increases (P < 0.05, P < 0.001) compared to controls at 12 and 24 h.

Western Blot Analysis^[1]

Cell Line:

OCI-LY8, NU-DUL-1 (diffuse large B-cell lymphoma cell lines)
Concentration:

4 μM; 8 μM
Incubation Time:

24 h
Result:

Increased p-CHK2 and p21 protein expression, while decreasing protein levels of cdc25A, cdc25C, and cyclinB1 in both OCI-LY8 and NU-DUL-1 cells.

Western Blot Analysis^[1]

Cell Line:

OCI-LY8, NU-DUL-1 (diffuse large B-cell lymphoma cell lines)
Concentration:

8 μM; 16 μM
Incubation Time:

48 h
Result:

Upregulated phosphorylated ERK1/2, downregulated phosphorylated Akt, phosphorylated JAK2, and phosphorylated STAT3, and reduced c-Myc expression in a dose-dependent manner in both OCI-LY8 and NU-DUL-1 cells.

Cell Proliferation Assay^[1]

Cell Line:

OCI-LY8, NU-DUL-1 (diffuse large B-cell lymphoma cell lines, STAT3 knockdown)
Concentration:

4, 8 μM
Incubation Time:

48 h
Result:

Enhanced antiproliferative efficacy in STAT3-knockdown OCI-LY8 and NU-DUL-1 cells compared to negative control siRNA-transfected cells, with statistically significant differences (P < 0.05) observed at both concentrations.

Western Blot Analysis^[1]

Cell Line:

OCI-LY8, NU-DUL-1 (diffuse large B-cell lymphoma cell lines)
Concentration:

8 μM; 16 μM
Incubation Time:

12 h; 24 h; 36 h; 48 h
Result:

Downregulated phosphorylated Lyn (Y507) in a dose- and time-dependent manner, while having no effect on phosphorylated Syk.
Decreased phosphorylated Lyn correlated with a synchronous decrease in phosphorylated STAT3.

Western Blot Analysis^[1]

Cell Line:

OCI-LY8, NU-DUL-1 (diffuse large B-cell lymphoma cell lines, Lyn-overexpressing)
Concentration:

16 μM
Incubation Time:

24 h
Result:

Caused a greater suppression of phosphorylated STAT3 in Lyn-overexpressing cells compared to control cells after 24 h, despite Lyn-overexpressing cells exhibiting higher levels of phosphorylated STAT3 than control cells without treatment.

Immunofluorescence^[2]

Cell Line:

BTZ-resistant multiple myeloma cell lines NCI-H929R and RPMI-8226R5
Concentration:

8 μM
Incubation Time:

48 h
Result:

Increased γ-H2A.X expression and formation of γ-H2A.X foci, indicating increased DNA double-strand breaks.\nInduced the formation of multipolar mitotic spindles, a hallmark of mitotic catastrophe.

In Vivo

DCZ3301 (40 mg/kg; i.p.; daily; 12 days) significantly inhibits diffuse large B-cell lymphoma xenograft tumor growth in BALB/c nude mice^[1].
DCZ3301 (50 mg/kg; i.p.; 2 consecutive days followed by 1 day of vehicle; for 20 days) significantly inhibits tumor growth in a BTZ-resistant multiple myeloma xenograft model, reduces tumor cell proliferation^[2].
DCZ3301 (50 mg/kg; i.p.; daily; 14 days) does not induce significant acute liver or kidney toxicity in healthy BALB/C nude mice^[2].
DCZ3301 (30 mg/kg; i.p.; daily; 14 days) significantly inhibits T-cell leukemia/lymphoma xenograft tumor growth in BALB/c nude mice^[3].
Treatment with DCZ3301 (30 mg/kg; i.p.; daily; 14 days) significantly inhibits tumor growth and reduces tumor weight in a Jurkat cell xenograft model of T-cell leukemia^[4].
DCZ3301 (50-200 μM; topical eye drops; three times daily; 7 days) significantly reduces corneal neovascularization area and attenuates corneal stroma edema in alkali-burned mice, with 200 μM producing a larger reduction in CNV area compared to vehicle control^[5].
DCZ3301 (200 μM; topical eye drops; three times daily; 7 days) does not significantly affect corneal epithelial thickness or endothelial cell density in healthy BALB/c mice^[5].

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

Animal Model:

BALB/c nude (6-week-old male, athymic, nu/nu, subcutaneous xenograft model)^[1]
Dosage:

40 mg/kg
Administration:

i.p.; daily; 12 days
Result:

Reduced tumor volume significantly compared to controls by day 12 (P < 0.05).
Showed no significant difference in mouse body weight compared to controls.
Increased cell necrosis in tumor tissues via H&E staining.
Increased apoptotic cells in tumor tissues via TUNEL staining.
Downregulated phosphorylated STAT3 expression in tumor tissues via immunohistochemistry.
Showed no evidence of organ dysfunction or growth disorder in functional organs.

Animal Model:

BALB/C nude mice (weight monitored during study)^[2]
Dosage:

50 mg/kg
Administration:

i.p.; 2 consecutive days followed by 1 day of vehicle; for 20 days
Result:

Significantly reduced tumor volume compared to control group on day 20.
Did not cause changes in mouse body weight or significant differences in serum levels of ALT, AST, Cr, or BUN.
Increased tumor cell shrinkage and fragmentation relative to controls.
Reduced Ki-67 expression in tumor tissue.
Increased cleaved-caspase 3 expression in tumor tissue.
Upregulated γ-H2A.X, phospho-ATM, and phospho-CHK1 expression in tumor tissue.
Increased percentage of TUNEL-positive cells in tumors.

Animal Model:

BALB/C nude mice (weight monitored during study)^[2]
Dosage:

50 mg/kg
Administration:

i.p.; daily; 14 days
Result:

Showed no significant differences in serum levels of ALT, AST, Cr, or BUN compared to vehicle-treated controls.

Animal Model:

BALB/c nude (5-week-old male, subcutaneous xenograft with Jurkat cells)^[3]
Dosage:

30 mg/kg
Administration:

i.p.; daily; 14 days
Result:

Reduced final tumor volumes to statistically significant levels (P < 0.01).
Reduced final tumor weights to statistically significant levels (P < 0.001).
Caused no significant change in mouse body weight compared to vehicle controls.

Animal Model:

BALB/c nude (5-week-old male, subcutaneous xenograft model)^[4]
Dosage:

30 mg/kg
Administration:

i.p.; daily; 14 days
Result:

Reduced tumor volume by a statistically significant margin on days 12 and 14 of treatment (P < 0.01).
Lowered final tumor weight significantly compared to controls (P < 0.001).
Caused no significant change in mouse body weight compared to vehicle-treated groups.

Animal Model:

BALB/c (6-8 week old male, alkali-burn induced corneal neovascularization)^[5]
Dosage:

50 μM; 200 μM
Administration:

topical eye drops; three times daily; 7 days
Result:

Significantly reduced the ratio of corneal neovascularization (CNV) area compared to vehicle control (P < 0.01).
Significantly reduced the ratio of CNV area compared to vehicle control (P < 0.0001).
Greatly reduced corneal stroma thickness compared to vehicle control (P < 0.001).
Greatly reduced corneal stroma thickness compared to vehicle control (P < 0.0001).

Animal Model:

BALB/c^[5]
Dosage:

200 μM
Administration:

topical eye drops; three times daily; 7 days
Result:

Did not cause a significant difference in central corneal epithelial thickness compared to saline-treated controls (P > 0.05).
Did not cause a significant difference in corneal endothelial cell density compared to saline-treated controls (P > 0.05).
Maintained regular shape of corneal endothelial cells.

Chemical Information

CAS No. 2136278-38-9
Appearance Solid
Molecular Weight 464.83
Formula C₂₀H₁₆ClF₃N₆O₂
Color White to off-white
SMILES

O=C(C1=NC=CC(OC2=CC=C(NC(NC3=CC=C(Cl)C(C(F)(F)F)=C3)=N)N=C2)=C1)NC
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (107.57 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

2.1513 mL

10.7566 mL

21.5132 mL

5 mM

0.4303 mL

2.1513 mL

4.3026 mL

10 mM

0.2151 mL

1.0757 mL

2.1513 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

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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 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.38 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.

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (297 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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)

References

[1]. Sun X, et al. DCZ3301, a novel cytotoxic agent, inhibits proliferation in diffuse large B-cell lymphoma via the STAT3 pathway. Cell Death Dis. 2017;8(10):e3111. Published 2017 Oct 12. [Content Brief]

[2]. Hu L, et al. A novel M phase blocker, DCZ3301 enhances the sensitivity of bortezomib in resistant multiple myeloma through DNA damage and mitotic catastrophe. J Exp Clin Cancer Res. 2020;39(1):105. Published 2020 Jun 9. [Content Brief]

[3]. Xiao W, et al. DCZ3301, a novel aryl-guanidino inhibitor, induces cell apoptosis and cell cycle arrest via suppressing the PI3K/AKT pathway in T-cell leukemia/lymphoma. Acta Biochim Biophys Sin (Shanghai). 2018;50(7):643-650. [Content Brief]

[4]. Xu K, et al. DCZ3301, an aryl-guanidino agent, inhibits ocular neovascularization via PI3K/AKT and ERK1/2 signaling pathways. Exp Eye Res. 2020;201:108267. [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

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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.1513 mL	10.7566 mL	21.5132 mL	53.7831 mL
	5 mM	0.4303 mL	2.1513 mL	4.3026 mL	10.7566 mL
	10 mM	0.2151 mL	1.0757 mL	2.1513 mL	5.3783 mL
	15 mM	0.1434 mL	0.7171 mL	1.4342 mL	3.5855 mL
	20 mM	0.1076 mL	0.5378 mL	1.0757 mL	2.6892 mL
	25 mM	0.0861 mL	0.4303 mL	0.8605 mL	2.1513 mL
	30 mM	0.0717 mL	0.3586 mL	0.7171 mL	1.7928 mL
	40 mM	0.0538 mL	0.2689 mL	0.5378 mL	1.3446 mL
	50 mM	0.0430 mL	0.2151 mL	0.4303 mL	1.0757 mL
	60 mM	0.0359 mL	0.1793 mL	0.3586 mL	0.8964 mL
	80 mM	0.0269 mL	0.1345 mL	0.2689 mL	0.6723 mL
	100 mM	0.0215 mL	0.1076 mL	0.2151 mL	0.5378 mL

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DCZ3301

Apoptosis Compound Library

Epigenetics Compound Library

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

MAPK Compound Library

PI3K/Akt/mTOR Compound Library

Protein Tyrosine Kinase Compound Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

Autophagy Compound Library

Small Molecule Immuno-Oncology Compound Library

Anti-Aging Compound Library

Differentiation Inducing Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Glycolysis Compound Library

Cytoskeleton Compound Library

Glutamine Metabolism Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Transcription Factor-Targeted Library

Glucose Metabolism Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Pain-Related Compound Library

Membrane Protein-targeted Compound Library

Autoimmune Disease Compound Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Fibrosis Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Lactylation Compound Library

All JAK Isoforms

All STAT Isoforms

All ERK Isoforms

All PI3K Isoforms

All Akt Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

DCZ3301 Related Classifications

Cat. No.: HY-125542