Referencia número: HY-10459

PF-562271

(Synonyms: VS-6062)

32 Cited Publications

Revisión del cliente

Based on 32 publication(s) in Google Scholar

PF-562271 (VS-6062) is a potent, ATP-competitive and reversible FAK and Pyk2 kinase inhibitor with IC₅₀s of 1.5 nM and 13 nM, respectively.

Para uso exclusivo en investigación. No vendemos a pacientes.

Pureza: 99.36%
No. CAS: 717907-75-0
Fòrmula: C₂₁H₂₀F₃N₇O₃S
Peso molecular:507.49

Almacenamiento:

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

PF-562271 Chemical Structure

No. CAS: 717907-75-0

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Fluorescent Dye

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

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (32)
Solvente y solubilidad
- In Vitro
- In Vivo
Protocolo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

PF-562271 (VS-6062) is a potent, ATP-competitive and reversible FAK and Pyk2 kinase inhibitor with IC₅₀s of 1.5 nM and 13 nM, respectively^[1].

IC₅₀ & Target

IC50: 1.5 nM (FAK), 13 nM (Pyk2), 30 nM (CDK2), 47 nM (CDK3), 58 nM (CDK1), 97 nM (CDK7), 97 nM (Flt3)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
A375P	GI₅₀	10.22 μM Compound: PF-562271	Antiproliferative activity against human A375P cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human A375P cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo assay	[PMID: 34324343]
HCT-116	GI₅₀	1.14 μM Compound: PF-562271	Antiproliferative activity against human HCT-116 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human HCT-116 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo assay	[PMID: 34324343]
MDA-MB-231	GI₅₀	1.95 μM Compound: PF-562271	Antiproliferative activity against human MDA-MB-231 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human MDA-MB-231 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo assay	[PMID: 34324343]
Sf21	IC₅₀	13 nM Compound: PF562271	Inhibition of full length recombinant human N-terminal His6-tagged PYK2 expressed in baculovirus infected sf21 cells Inhibition of full length recombinant human N-terminal His6-tagged PYK2 expressed in baculovirus infected sf21 cells	[PMID: 27876318]
Sf9	IC₅₀	1.5 nM Compound: PF562271	Reversible/competitive inhibition of NH2-terminal His6-tagged FAK kinase domain (410 to 689 residues) (unknown origin) expressed in baculovirus infected sf9 cells using p(Glu/Tyr) as substrate in presence of ATP Reversible/competitive inhibition of NH2-terminal His6-tagged FAK kinase domain (410 to 689 residues) (unknown origin) expressed in baculovirus infected sf9 cells using p(Glu/Tyr) as substrate in presence of ATP	[PMID: 27876318]
SMMC-7721	IC₅₀	23.92 μM Compound: PF-562271	Antiproliferative activity against human SMMC-7721 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay Antiproliferative activity against human SMMC-7721 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay	[PMID: 34214842]

In Vitro

PF-562271 (VS-6062) is shown to be a 30- to 120-nM inhibitor of CDK2/E, CDK5/p35, CDK1/B, and CDK3/E in recombinant enzyme assays, in cell-based assays evaluating the role of CDKs, a 48-hour exposure of 3.3 μM PF-562271 is required to alter cell cycle progression. PF-562271 is potent in an inducible cell-based assay measuring phospho-FAK with a IC₅₀ of 5 nM^[1].
PF-562271, a selective inhibitor of both FAK and proline-rich tyrosine kinase 2 (PYK2), a FAK-related family member, on cell growth and colony formation in Ewing sarcoma cell lines. Seven cell lines are treated for 5 days with PF-562271 across a range of concentrations using 2-fold serial dilutions. Treatment with PF-562271 impaires cell viability in all cell lines, with an average IC₅₀ of 2.4 μM after 3 days of treatment. TC32 and A673 are the 2 most sensitive cell lines, with IC₅₀ concentrations of 2.1 and 1.7 μM, respectively^[2].

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

In Vivo

PF-562271 inhibits FAK phosphorylation in vivo in a dose-dependent fashion (calculated EC₅₀ of 93 ng/mL, total) after p.o. administration to tumor-bearing mice^[1]. Rats that receive PF-562271 demonstrate a decrease in tumor growth after 2 weeks of treatment with signs of bone healing as evidenced by the deposition of new bone (cortical and cancellous) at sites previously damaged by the tumor^[3].

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

Chemical Information

No. CAS 717907-75-0
Appearance Solid
Peso molecular 507.49
Fòrmula C₂₁H₂₀F₃N₇O₃S
Color Light yellow to brown
SMILES

CS(=O)(N(C)C1=NC=CC=C1CNC2=NC(NC3=CC4=C(C=C3)NC(C4)=O)=NC=C2C(F)(F)F)=O
Synonyms

VS-6062
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

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

Publications (32)

All WB

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Journal Impact Factor

Nat Biomed Eng

Nonexpansive biodegradable matrix promotes blood vessel organoid development for neurovascular repair and functional recovery in ischaemic stroke. [Abstract]

2025 Nov 3. PMID: 41184604
Cancer Res

High-throughput tyrosine kinase activity profiling identifies FAK as a candidate therapeutic target in Ewing sarcoma. [Abstract]

2013 May 1;73(9):2873-83. PMID: 23536552

PF-562271 purchased from MedChemExpress. Usage Cited in: Cancer Res. 2013 May 1;73(9):2873-83. [Abstract]

FAK inhibition downregulates the AKT/mTOR pathway and CAS activity. A, protein levels measured by Western immunoblotting for AKT/mTOR pathway proteins in A673 and TC32 cells serum-starved overnight, treated with PF-562271 for 6 hours, and then stimulated with IGF-1 for 2 hours. Vinculin is used as the loading control. B, Western immunoblots showing downregulation of phospho-CAS but not phospho-ERK in A673 and TC32 cells after treatment with PF-562271.
Autophagy

PTK2/FAK inhibition triggers TMED9-mediated protective autophagy in pancreatic cancer cell via enhancing ERGIC-ERES contact. [Abstract]

2026 May 29:1-15. PMID: 42144738
Cell Discov

A positive mechanobiological feedback loop controls bistable switching of cardiac fibroblast phenotype. [Abstract]

2022 Sep 6;8(1):84. PMID: 36068215
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
Carbohydr Polym

Inulin-like polysaccharide ABWW may impede CCl4 induced hepatic stellate cell activation through mediating the FAK/PI3K/AKT signaling pathway in vitro & in vivo. [Abstract]

2024 Feb 15:326:121637. PMID: 38142102
Cell Death Dis

Identification of matrix-remodeling associated 5 as a possible molecular oncotarget of pancreatic cancer. [Abstract]

2023 Feb 24;14(2):157. PMID: 36828810

PF-562271 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2023 Feb 24;14(2):157. [Abstract]

PF-562271 (250 nM; 6 h) largely inhibits Akt-S6 phosphorylation in OE-MXRA5 priPC-1 cells.
Cell Death Dis

P130cas-FAK interaction is essential for YAP-mediated radioresistance of non-small cell lung cancer. [Abstract]

2022 Sep 10;13(9):783. PMID: 36088346
Clin Cancer Res

High-throughput Chemical Screening Identifies Focal Adhesion Kinase and Aurora Kinase B Inhibition as a Synergistic Treatment Combination in Ewing Sarcoma. [Abstract]

2019 Jul 15;25(14):4552-4566. PMID: 30979745
Int J Surg

Supervising the recurrence of pancreatic ductal adenocarcinoma using CtDNA-based MIR129-2 methylation detection. [Abstract]

2025 Sep 17. PMID: 40961228
Am J Chin Med

Evodiamine Suppresses Lung Cancer Progression Through Modulating FAK/STAT3/AKT Signaling Pathway. [Abstract]

2025;53(4):1225-1240. PMID: 40582716
World J Gastroenterol

FBP1 as a key regulator of focal adhesion kinase-mediated hepatic stellate cell activation: Multi-omics and experimental validation. [Abstract]

2025 Jul 28;31(28):107361. PMID: 40741470
Cell Rep

Mechanotransduction in response to ECM stiffening impairs cGAS immune signaling in tumor cells. [Abstract]

2023 Oct 5;42(10):113213. PMID: 37804510
Life Sci

Harmine inhibits the proliferation and migration of glioblastoma cells via the FAK/AKT pathway. [Abstract]

2021 Apr 1:270:119112. PMID: 33508300
Breast Cancer Res

TMEM120B strengthens breast cancer cell stemness and accelerates chemotherapy resistance via β1-integrin/FAK-TAZ-mTOR signaling axis by binding to MYH9. [Abstract]

2024 Mar 19;26(1):48. PMID: 38504374
Sci Rep

The mechanical microenvironment regulates ovarian cancer cell morphology, migration, and spheroid disaggregation. [Abstract]

2018 May 8;8(1):7228. PMID: 29740072
Int J Cancer

Targeting FAK scaffold functions inhibits human renal cell carcinoma growth. [Abstract]

2015 Oct 1;137(7):1549-59. PMID: 25809490

PF-562271 purchased from MedChemExpress. Usage Cited in: Int J Cancer. 2015 Oct 1;137(7):1549-59. [Abstract]

786-O (a) and Caki-1 (b) are treated for 24 and 48h with increasing concentrations of PF-562,271 and adherent cells were counted. Cell lysates are evaluated through immunoblotting for total FAK following treatment for 24h.
Cell Signal

Tenvermectin B, a novel macrocyclic lactone antibiotic, suppresses glioblastoma progression by targeting RhoJ. [Abstract]

2025 Sep 10:136:112117. PMID: 40939916
Environ Toxicol Pharmacol

ZC3H4 Governs Epithelial Cell Migration through ROCK/p-PYK2/p-MLC2 Pathway in Silica-induced Pulmonary Fibrosis. [Abstract]

2023 Nov:104:104301. PMID: 37866415
Eur J Cell Biol

The mechanical mechanism of angiotensin II induced activation of hepatic stellate cells promoting portal hypertension. [Abstract]

2024 May 28;103(2):151427. PMID: 38820882
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
Mol Biol Rep

Piperlongumine inhibits the proliferation and migration of non-small cell lung cancer cells through the EGFR/FAK/STAT3 pathway. [Abstract]

2026 May 14;53(1):770. PMID: 42133146
Mol Biol Rep

Ginkgetin inhibits the proliferation and migration of lung cancer cells via FAK/STAT3/AKT pathway. [Abstract]

2025 May 14;52(1):458. PMID: 40366441
J Nat Med

Antiangiogenic effects of AG36, a triterpenoid saponin from Ardisia gigantifolia stapf. [Abstract]

2020 Sep;74(4):732-740. PMID: 32643027
Anticancer Drugs

AZD7762 induces CRBN dependent BAG3 degradation through ubiquitin-proteasome pathway. [Abstract]

2024 Jan 1;35(1):46-54. PMID: 37449977
Res Sq

2025 Jul 11.
University of Washington

2025.
bioRxiv

2025 May 28.
bioRxiv

FAK Differentially Mechanoregulates Cell Migration During Wound Closure. [Abstract]

2025 Apr 7:2025.04.01.646098. PMID: 40291676
Research Square Preprint

2023 May 23.
Research Square Preprint

2021 Dec.
Practical Oncology Journal

2015, 29(5): 444-449.

PF-562271 purchased from MedChemExpress. Usage Cited in: Practical Oncology Journal. 2015, 29(5): 444-449.

Effects and mechanism of Biglycan and FAK signaling pathway on the invasion and metastasis of colon cancer cells.

Solvente y solubilidad

In Vitro:

DMSO : 66.67 mg/mL (131.37 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

1.9705 mL

9.8524 mL

19.7048 mL

5 mM

0.3941 mL

1.9705 mL

3.9410 mL

10 mM

0.1970 mL

0.9852 mL

1.9705 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.

Calculadora de molaridad

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

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: ≥ 1.67 mg/mL (3.29 mM); Clear solution

This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 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% Corn Oil

Solubility: ≥ 1.67 mg/mL (3.29 mM); Clear solution

This protocol yields a clear solution of ≥ 1.67 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 (16.7 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

Protocolo

Cell Assay^[2]

Ewing sarcoma cells are plated in 10-cm dishes, allowed to adhere for 24 hours, and then treated with PF-562271, PD0325901, or BMS-354825. ATP content is measured as a surrogate for cell number using the CellTiter-Glo Luminescent Cell Viability Assay. Luminescence readings are obtained using the FLUOstar Omega microplate reader. For experiments with small-molecule treatment, 1.25×10³ Ewing sarcoma cells are seeded in each well and treated with a range of concentrations. IC₅₀ values are calculated from ATP measurements obtained after 3 days of treatment using log-transformed, normalized data in GraphPad Prism 5.0. Cell lines are also treated with compound in 6-cm dishes, trypsinized, and counted by light microscopy using trypan blue exclusion. For experiments using shRNA-transduced cells, 1.25×10³ cells are seeded per well into 384-well plates on day 3 posttransduction. ATP content is measured on days 3, 6, and 8 posttransduction^[2].

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

Animal Administration^[1]^[3]

Mice^[1]
Athymic female mice (CD-1 Nu/Nu, ~20 grams) are used for all in vivo studies. Exponentially growing cells are trypsinized and resuspended in sterile PBS and inoculated s.c. (1×10⁶ cells per mouse in 200 μL) into the right flank of mice. Animals bearing tumors of 150 mm³ in size are divided into groups receiving either vehicle (5% Gelucire) or PF-562,271 (diluted in vehicle), and dosed by p.o. gavage. Animal body weight and tumor measurements are obtained every 2 d. Tumor volume (mm³) is measured with Vernier calipers and calculated using the formula: length (mm)×width (mm)×width (mm)×0.5. Percent growth inhibition. For all tumor growth inhibition experiments, 8 to 10 mice per dose group are used. A Student's t test is used to determine the P value.
Rats^[3]
Nude (Crl:NIH-rnu) female rats are used. PF-562271 is formulated for oral dosing using 0.5% methyl-cellulose. On the first day of dosing, rats receive a single dose of PF-562271 (10 mg/kg) by oral gavage. Based on the exposure levels at 1 hour after dosing, the dose is reduced to 5 mg/kg. From the second day onward, rats are dosed daily with 5 mg/kg by oral gavage for 28 days. Dosing is initiated 2 weeks after tumor inoculation and only after the presence of tumors is confirmed by radiography. The presence of the tested compound in serum is confirmed during the course of the study.

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

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (280 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Roberts WG, et al. Antitumor activity and pharmacology of a selective focal adhesion kinase inhibitor, PF-562,271. Cancer Res, 2008, 68(6), 1935-1944. [Content Brief]

[2]. Crompton BD, et al. High-throughput tyrosine kinase activity profiling identifies FAK as a candidate therapeutic target in Ewing sarcoma. Cancer Res. 2013 May 1;73(9):2873-83. [Content Brief]

[3]. Bagi CM, et al. Dual focal adhesion kinase/Pyk2 inhibitor has positive effects on bone tumors: implications for bone metastases. Cancer. 2008 May 15;112(10):2313-21. [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	1.9705 mL	9.8524 mL	19.7048 mL	49.2621 mL
	5 mM	0.3941 mL	1.9705 mL	3.9410 mL	9.8524 mL
	10 mM	0.1970 mL	0.9852 mL	1.9705 mL	4.9262 mL
	15 mM	0.1314 mL	0.6568 mL	1.3137 mL	3.2841 mL
	20 mM	0.0985 mL	0.4926 mL	0.9852 mL	2.4631 mL
	25 mM	0.0788 mL	0.3941 mL	0.7882 mL	1.9705 mL
	30 mM	0.0657 mL	0.3284 mL	0.6568 mL	1.6421 mL
	40 mM	0.0493 mL	0.2463 mL	0.4926 mL	1.2316 mL
	50 mM	0.0394 mL	0.1970 mL	0.3941 mL	0.9852 mL
	60 mM	0.0328 mL	0.1642 mL	0.3284 mL	0.8210 mL
	80 mM	0.0246 mL	0.1232 mL	0.2463 mL	0.6158 mL
	100 mM	0.0197 mL	0.0985 mL	0.1970 mL	0.4926 mL

Keywords

PF-562271

32 Cited Publications

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PF-562271

Kinase Inhibitor Library

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Anti-Cancer Compound Library

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Anti-Pancreatic Cancer Compound Library

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High-Throughput Bioactive Compound Library

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Publications Citing Use of MedChemExpress (MCE) PF-562271

Actividad biológica

Chemical Information

Publications (32)

Solvente y solubilidad

Protocolo

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

PF-562271

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Cytoskeleton Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Heterocyclic Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

Kinase Inhibitor Library Mini

MCE Bioactive Compound Library

Clinical Compound Library Plus

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) PF-562271

Actividad biológica

Chemical Information

Publications (32)

Solvente y solubilidad

Protocolo

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

PF-562271 Related Classifications

HY-10459 Related Classifications