Cat. No.: HY-10524

GSK1904529A

7 Cited Publications

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Based on 7 publication(s) in Google Scholar

GSK1904529A is a potent, selective, orally active, and ATP-competitive inhibitor of insulin-like growth factor-1 receptor (IGF-1R) and insulin receptor (IR), with IC₅₀s of 27 and 25 nM, respectively. GSK1904529A shows poor activity (IC₅₀>1 μM) in 45 other serine/threonine and tyrosine kinases. GSK1904529A exhibits anti-tumor activity.

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Pureté: 99.03%
CAS No.: 1089283-49-7
Formule: C₄₄H₄₇F₂N₉O₅S
Masse moléculaire:851.96

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

GSK1904529A Chemical Structure

CAS No.: 1089283-49-7

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Fluorescent Dye

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

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (7)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

IC50: 27 nM (IGF-1R), 25 nM (IR)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	>20000 nM Compound: 24	Antiproliferative activity against human A549 cells after 72 hrs by Celltiter assay Antiproliferative activity against human A549 cells after 72 hrs by Celltiter assay	[PMID: 19101143]
A549	IC₅₀	>20000 nM Compound: Chemical Probe: GSK1904529A	Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay	[PMID: 19383820]
A673	IC₅₀	>30000 nM Compound: Chemical Probe: GSK1904529A	Antiproliferative activity against human A673 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human A673 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay	[PMID: 19383820]
COLO 205	IC₅₀	124 nM Compound: 24	Antiproliferative activity against human COLO205 cells after 72 hrs by Celltiter assay Antiproliferative activity against human COLO205 cells after 72 hrs by Celltiter assay	[PMID: 19101143]
COLO 205	IC₅₀	124 nM Compound: Chemical Probe: GSK1904529A	Antiproliferative activity against human COLO 205 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human COLO 205 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay	[PMID: 19383820]
EJM	IC₅₀	>30000 nM Compound: Chemical Probe: GSK1904529A	Antiproliferative activity against human EJM cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human EJM cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay	[PMID: 19383820]
HeLa	IC₅₀	>20000 nM Compound: Chemical Probe: GSK1904529A	Antiproliferative activity against human HeLa cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human HeLa cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay	[PMID: 19383820]
HFF	IC₅₀	>20000 nM Compound: 24	Antiproliferative activity against HFF cells after 72 hrs by Celltiter assay Antiproliferative activity against HFF cells after 72 hrs by Celltiter assay	[PMID: 19101143]
HFF	IC₅₀	>20000 nM Compound: Chemical Probe: GSK1904529A	Cytotoxicity against HFF cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay Cytotoxicity against HFF cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay	[PMID: 19383820]
HMEC	IC₅₀	>20000 nM Compound: Chemical Probe: GSK1904529A	Cytotoxicity against HMEC cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay Cytotoxicity against HMEC cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay	[PMID: 19383820]
HN5	IC₅₀	>20000 nM Compound: Chemical Probe: GSK1904529A	Antiproliferative activity against human HN5 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human HN5 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay	[PMID: 19383820]
HT-29	IC₅₀	104 nM Compound: Chemical Probe: GSK1904529A	Antiproliferative activity against human HT-29 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human HT-29 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay	[PMID: 19383820]
HUVEC	IC₅₀	>20000 nM Compound: Chemical Probe: GSK1904529A	Cytotoxicity against HUVEC cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay Cytotoxicity against HUVEC cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay	[PMID: 19383820]
JJN-3	IC₅₀	>30000 nM Compound: Chemical Probe: GSK1904529A	Antiproliferative activity against human JJN-3 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human JJN-3 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay	[PMID: 19383820]
KARPAS-299	IC₅₀	>30000 nM Compound: Chemical Probe: GSK1904529A	Antiproliferative activity against human KARPAS-299 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human KARPAS-299 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay	[PMID: 19383820]
KMS-12-BM	IC₅₀	113 nM Compound: Chemical Probe: GSK1904529A	Antiproliferative activity against human KMS-12-BM cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human KMS-12-BM cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay	[PMID: 19383820]
L-363	IC₅₀	165 nM Compound: Chemical Probe: GSK1904529A	Antiproliferative activity against human L-363 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human L-363 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay	[PMID: 19383820]
LNCaP	IC₅₀	>20000 nM Compound: Chemical Probe: GSK1904529A	Antiproliferative activity against human LNCaP cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human LNCaP cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay	[PMID: 19383820]
LP-1	IC₅₀	104 nM Compound: 24	Antiproliferative activity against human LP-1 cells after 72 hrs by Celltiter assay Antiproliferative activity against human LP-1 cells after 72 hrs by Celltiter assay	[PMID: 19101143]
LP-1	IC₅₀	104 nM Compound: Chemical Probe: GSK1904529A	Antiproliferative activity against human LP-1 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human LP-1 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay	[PMID: 19383820]
MCF7	IC₅₀	137 nM Compound: Chemical Probe: GSK1904529A	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay	[PMID: 19383820]
MDA-MB-468	IC₅₀	>20000 nM Compound: Chemical Probe: GSK1904529A	Antiproliferative activity against human MDA-MB-468 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human MDA-MB-468 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay	[PMID: 19383820]
MHH-ES-1	IC₅₀	>30000 nM Compound: Chemical Probe: GSK1904529A	Antiproliferative activity against human MHH-ES-1 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human MHH-ES-1 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay	[PMID: 19383820]
MOLP-8	IC₅₀	96 nM Compound: Chemical Probe: GSK1904529A	Antiproliferative activity against human MOLP8 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human MOLP8 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay	[PMID: 19383820]
MX1	IC₅₀	189 nM Compound: Chemical Probe: GSK1904529A	Antiproliferative activity against human MX1 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human MX1 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay	[PMID: 19383820]
NCI-H1299	IC₅₀	>20000 nM Compound: Chemical Probe: GSK1904529A	Antiproliferative activity against human NCI-H1299 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human NCI-H1299 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay	[PMID: 19383820]
NCI-H929	IC₅₀	81 nM Compound: 24	Antiproliferative activity against human NCI-H929 cells after 72 hrs by Celltiter assay Antiproliferative activity against human NCI-H929 cells after 72 hrs by Celltiter assay	[PMID: 19101143]
NCI-H929	IC₅₀	81 nM Compound: Chemical Probe: GSK1904529A	Antiproliferative activity against human NCI-H929 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human NCI-H929 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay	[PMID: 19383820]
NIH3T3	IC₅₀	19 nM Compound: 24	Inhibition of human insulin receptor autophosphorylation in transfected mouse NIH3T3 cells Inhibition of human insulin receptor autophosphorylation in transfected mouse NIH3T3 cells	[PMID: 19101143]
NIH3T3	IC₅₀	22 nM Compound: 24	Inhibition of human IGF1R autophosphorylation in transfected mouse NIH3T3 cells Inhibition of human IGF1R autophosphorylation in transfected mouse NIH3T3 cells	[PMID: 19101143]
PrEC	IC₅₀	68 nM Compound: Chemical Probe: GSK1904529A	Cytotoxicity against human PREC cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay Cytotoxicity against human PREC cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay	[PMID: 19383820]
SK-N-MC	IC₅₀	43 nM Compound: Chemical Probe: GSK1904529A	Antiproliferative activity against human SK-N-MC cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human SK-N-MC cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay	[PMID: 19383820]
SK-OV-3	IC₅₀	>20000 nM Compound: Chemical Probe: GSK1904529A	Antiproliferative activity against human SK-OV-3 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human SK-OV-3 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay	[PMID: 19383820]
SU-DHL-1	IC₅₀	>30000 nM Compound: Chemical Probe: GSK1904529A	Antiproliferative activity against human SU-DHL-1 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human SU-DHL-1 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay	[PMID: 19383820]

In Vitro

GSK1904529A displays high affinities for IGF-1R and IR, with K_is of 1.6 and 1.3 nM, respectively^[1].
GSK1904529A (72 h) inhibits tumor cells proliferation with IC₅₀s ranges from 35 nM to >30 μM, and Ewing's sarcoma and multiple myeloma cell lines are greatest sensitive^[1].
GSK1904529A (0.03-3 μM; 24 and 48 h) arrests cells at the G1 phase of the cell cycle^[1].
GSK1904529A (2 h) inhibits phosphorylation of IGF-IR and IR with IC₅₀s of 22 and 19 nM in NIH-3T3/LISN and NIH-3T3-hIR cells, respectively^[1].
GSK1904529A (0.01-3 μM; 4 h) blocks the major downstream signal transduction pathways mediated by IGF-IR and IR in NIH-3T3/LISN and NIH-3T3-hIR cells^[1].

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

Cell Cycle Analysis^[1]

Cell Line:

COLO 205, MCF-7, and NCI-H929 cells
Concentration:

0, 0.03, 0.1, 0.3, 1, 3 μM
Incubation Time:

24 and 48 hours
Result:

Increased the accumulation in G1 and decreased accumulation in S and G2-M phases of the cell cycle.

Western Blot Analysis^[1]

Cell Line:

NIH-3T3/LISN and NIH-3T3-hIR cells
Concentration:

0.01, 0.03, 0.1, 0.3, 1, 3 μM
Incubation Time:

4 hours
Result:

Inhibited the ligand-induced phosphorylation of IGF-IR and IR at concentrations >0.01 μM.
Decreased the phosphorylation of AKT, IRS-1, and ERK.

In Vivo

GSK1904529A (30 mg/kg; p.o. once or twice daily for 21 d) has antitumor activity in mice^[1].
GSK1904529A (1-30 mg/kg; a single p.o.) decreases IGF-I-induced IGF-IR phosphorylation in a dose-dependent manner in mice^[1].
GSK1904529A (30 mg/kg; p.o. once or twice daily for 21 d) has no significant alterations in the blood glucose levels in mice^[1].

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

Animal Model:

Female athymic nu/nu CD-1 mice are bring NIH-3T3/LISN tumor^[1]
Dosage:

30 mg/kg
Administration:

P.o. once or twice daily for 21 d
Result:

Resulted in 56% (once daily) and 98% (twice daily) inhibition of tumor growth.
No significant decrease in body weight on the once-daily schedule.
Observed 11-13% of body weight loss, and recovered to near baseline 6 days after the cessation of treatment in twice-daily group.

Chemical Information

CAS No. 1089283-49-7
Appearance Solid
Masse moléculaire 851.96
Formule C₄₄H₄₇F₂N₉O₅S
Color Light yellow to yellow
SMILES

O=C(C1=CC(C2=C(N3C=CC=CC3=N2)C4=NC(NC5=CC(CC)=C(C=C5OC)N6CCC(CC6)N7CCN(CC7)S(=O)(C)=O)=NC=C4)=CC=C1OC)NC8=C(C=CC=C8F)F
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (7)

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Journal Impact Factor

Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
Clin Cancer Res

Upregulation of IGF1R by mutant RAS in leukemia and potentiation of RAS signaling inhibitors by small-molecule inhibition of IGF1R. [Abstract]

2014 Nov 1;20(21):5483-95. PMID: 25186968

GSK1904529A purchased from MedChemExpress. Usage Cited in: Clin Cancer Res. 2014 Nov 1;20(21):5483-95. [Abstract]

Effects of GSK1904529A as single agents, respectively, on mediators of IGF-1R- and ERK1/ERK2-signaling pathways.(A-B) Effect of GSK1904529A on phosphorylation of IGF-1R (A) and Erk1/Erk2 (B).
Mol Med Rep

Identification of the clinical value and biological effects of TTN mutation in liver cancer. [Abstract]

2025 Jun;31(6):165. PMID: 40242970
J Cell Mol Med

Cardiomyocyte protective effects of thyroid hormone during hypoxia/reoxygenation injury through activating of IGF-1-mediated PI3K/Akt signalling. [Abstract]

2021 Apr;25(7):3205-3215. PMID: 33724692
iScience

Time-restricted feeding entrains long-term behavioral changes through the IGF2-KCC2 pathway. [Abstract]

2022 Apr 18;25(5):104267. PMID: 35521538
Open Biol

Formyl-peptide receptor 2 signalling triggers aerobic metabolism of glucose through Nox2-dependent modulation of pyruvate dehydrogenase activity. [Abstract]

2023 Oct;13(10):230336. PMID: 37875162
Research Square Preprint

2024 Nov 06.

Solvant et solubilité

In Vitro:

DMSO : 50 mg/mL (58.69 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

1.1738 mL

5.8688 mL

11.7376 mL

5 mM

0.2348 mL

1.1738 mL

2.3475 mL

10 mM

0.1174 mL

0.5869 mL

1.1738 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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: ≥ 2.75 mg/mL (3.23 mM); Clear solution

This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 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.

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (281 KB)
SDS (393 KB)
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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)
Instruction de manipulation (2659 KB)

Références

[1]. Sabbatini P, et al. Antitumor activity of GSK1904529A, a small-molecule inhibitor of the insulin-like growth factor-I receptor tyrosine kinase. Clin Cancer Res, 2009, 15(9), 3058-3067. [Content Brief]

[2]. Zhou Q, et, al. GSK1904529A, an insulin-like growth factor-1 receptor inhibitor, inhibits glioma tumor growth, induces apoptosis and inhibits migration. Mol Med Rep. 2015 Sep;12(3):3381-3385. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.1738 mL	5.8688 mL	11.7376 mL	29.3441 mL
	5 mM	0.2348 mL	1.1738 mL	2.3475 mL	5.8688 mL
	10 mM	0.1174 mL	0.5869 mL	1.1738 mL	2.9344 mL
	15 mM	0.0783 mL	0.3913 mL	0.7825 mL	1.9563 mL
	20 mM	0.0587 mL	0.2934 mL	0.5869 mL	1.4672 mL
	25 mM	0.0470 mL	0.2348 mL	0.4695 mL	1.1738 mL
	30 mM	0.0391 mL	0.1956 mL	0.3913 mL	0.9781 mL
	40 mM	0.0293 mL	0.1467 mL	0.2934 mL	0.7336 mL
	50 mM	0.0235 mL	0.1174 mL	0.2348 mL	0.5869 mL

Keywords

GSK1904529A

7 Cited Publications

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GSK1904529A

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Publications Citing Use of MedChemExpress (MCE) GSK1904529A

Activité biologique

Chemical Information

Publications (7)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

GSK1904529A Related Classifications

HY-10524 Related Classifications