Cat. No.: HY-15343

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CEP-33779

5 Cited Publications

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Based on 5 publication(s) in Google Scholar

CEP-33779 is a novel, selective, and orally bioavailable inhibitor of JAK2 with an IC₅₀ of 1.8±0.6 nM.

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

Purity: 99.12%
CAS No.: 1257704-57-6
Formula: C₂₄H₂₆N₆O₂S
Molecular Weight:462.57

Storage:

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

CEP-33779 Chemical Structure

CAS No.: 1257704-57-6

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

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (5)
Solvent & Solubility
- In Vitro
- In Vivo
Protocol
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

CEP-33779 is a novel, selective, and orally bioavailable inhibitor of JAK2 with an IC₅₀ of 1.8±0.6 nM.

IC₅₀ & Target^[1]

JAK2

1.8 nM (IC₅₀)

JAK3

150 nM (IC₅₀)

All JAK Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	IC₅₀	0.289 μM Compound: 4	Antiproliferative activity against human A2780 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay Antiproliferative activity against human A2780 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay	[PMID: 37856840]
A2780/Taxol	IC₅₀	0.394 μM Compound: 4	Antiproliferative activity against human A2780T cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay Antiproliferative activity against human A2780T cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay	[PMID: 37856840]
A549	IC₅₀	0.358 μM Compound: 4	Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay	[PMID: 37856840]
ARPE-19	IC₅₀	4930.5 nM Compound: 4	Cytotoxicity against human ARPE-19 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay Cytotoxicity against human ARPE-19 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay	[PMID: 37856840]
BXPC-3	IC₅₀	0.73 μM Compound: 4	Antiproliferative activity against human BXPC-3 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay Antiproliferative activity against human BXPC-3 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay	[PMID: 37856840]
CHO	IC₅₀	0.172 μM Compound: 4	Antiproliferative activity against Chinese hamster CHO cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay Antiproliferative activity against Chinese hamster CHO cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay	[PMID: 37856840]
CHO-K1	IC₅₀	0.216 μM Compound: 4	Antiproliferative activity against Chinese hamster CHO-K1 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay Antiproliferative activity against Chinese hamster CHO-K1 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay	[PMID: 37856840]
COLO 205	IC₅₀	1548 nM Compound: 4	Cytotoxicity against human COLO 205 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay Cytotoxicity against human COLO 205 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay	[PMID: 37856840]
CWR22R	IC₅₀	5786.5 nM Compound: 4	Cytotoxicity against human 22Rv1 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay Cytotoxicity against human 22Rv1 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay	[PMID: 37856840]
HaCaT	IC₅₀	2825.5 nM Compound: 4	Cytotoxicity against human HaCaT cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay Cytotoxicity against human HaCaT cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay	[PMID: 37856840]
HCT-8	IC₅₀	1.136 μM Compound: 4	Antiproliferative activity against human HCT-8 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay Antiproliferative activity against human HCT-8 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay	[PMID: 37856840]
HeLa	IC₅₀	1.26 μM Compound: 4	Antiproliferative activity against human HeLa cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay Antiproliferative activity against human HeLa cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay	[PMID: 37856840]
HepG2	IC₅₀	2042 nM Compound: 4	Cytotoxicity against human HepG2 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay Cytotoxicity against human HepG2 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay	[PMID: 37856840]
HT-29	IC₅₀	0.961 μM Compound: 4	Antiproliferative activity against human HT-29 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay Antiproliferative activity against human HT-29 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay	[PMID: 37856840]
KP-4	IC₅₀	0.372 μM Compound: 4	Antiproliferative activity against human KP-4 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay Antiproliferative activity against human KP-4 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay	[PMID: 37856840]
L02	IC₅₀	388.5 nM Compound: 4	Cytotoxicity against human L02 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay Cytotoxicity against human L02 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay	[PMID: 37856840]
MCF7	IC₅₀	1.23 μM Compound: 4	Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay	[PMID: 37856840]
NCI/ADR-RES	IC₅₀	3.532 μM Compound: 4	Antiproliferative activity against human MCF7ADR cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay Antiproliferative activity against human MCF7ADR cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay	[PMID: 37856840]
PC-3	IC₅₀	15.11 μM Compound: 4	Antiproliferative activity against human PC-3 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay Antiproliferative activity against human PC-3 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay	[PMID: 37856840]
TF-1	IC₅₀	61 nM Compound: 29, CEP-33779	Inhibition of JAK2 in human TF-1 cells using GM-CSF pretreated for 1 hr prior to GM-CSF addition measured after 5 hrs by FRET based GeneBLAzer assay Inhibition of JAK2 in human TF-1 cells using GM-CSF pretreated for 1 hr prior to GM-CSF addition measured after 5 hrs by FRET based GeneBLAzer assay	[PMID: 22594690]

In Vitro

CEP-33779, at nontoxic concentrations, significantly sensitizes overexpression of P-glycoprotein overexpressing multidrug resistance cells to its anticancer substrates. CEP-33779 significantly increases intracellular accumulation and decreases the efflux of doxorubicin by inhibiting the overexpression of P-glycoprotein transport function^[3].

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

In Vivo

CEP-33779 exhibits a favorable PK profile in nude mice, an iv half-life of 1 h, moderate distribution (Vd=2.6 L/kg), and measurable oral exposure with an estimated bioavailability of 33%. It demonstrates antitumor efficacy in the CWR22 xenograft model; oral dosing for 14 days at 30 mg/kg bid results in tumor stasis and partial regressions in 5/10 animals^[1]. CEP-33779 administration results in an almost complete shrinkage of tumors in most animals; few remaining tumor nodules were small, poorly vascularized, and had a necrotic appearance. CEP-33779 suppressed activation of NF-κB in tumors^[2].

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

Chemical Information

CAS No. 1257704-57-6
Appearance Solid
Molecular Weight 462.57
Formula C₂₄H₂₆N₆O₂S
Color Light yellow to yellow
SMILES

O=S(C1=CC=C(C2=CC=CN3C2=NC(NC4=CC=CC(N5CCN(C)CC5)=C4)=N3)C=C1)(C)=O
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Publications (5)

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Journal Impact Factor

Cell Rep

Macrophage glycine transporter supports IL-1β production by modulating the AKT1/mTOR/NLRP3 pathway. [Abstract]

2026 Jan 3;45(1):116683. PMID: 41485223
Sci Rep

A phenotypic high-content, high-throughput screen identifies inhibitors of NLRP3 inflammasome activation. [Abstract]

2021 Jul 28;11(1):15319. PMID: 34321581
Iran J Immunol

JAK/STAT Signaling Pathway Mediates Anti-Tumor Immunity of CD8+ T Cells in Renal Cancer. [Abstract]

2024 Sep 25;21(3). PMID: 39319693
bioRxiv

2026 Mar 7.
Patent

US20180263995A1.

Solvent & Solubility

In Vitro:

DMSO : 8.33 mg/mL (18.01 mM; ultrasonic and warming and heat to 60°C; 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

2.1618 mL

10.8092 mL

21.6183 mL

5 mM

0.4324 mL

2.1618 mL

4.3237 mL

10 mM

0.2162 mL

1.0809 mL

2.1618 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.

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)

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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 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (5.40 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 (5.40 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 (5.40 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.

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: 10 mg/mL (21.62 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

Protocol

Kinase Assay^[1]

The kinase activity of baculovirus-expressed human JAK1, JAK2, or JAK3 is measured. Each 96-well Costar high binding plate is coated with 100 μL/well of 10 μg/mL neutravidin in TBS at 37 °C for 2 h, followed by 100 μL/well of 1 μg/mL 15-mer peptide substrate at 37 °C for 1 h. The kinase assay mixture (total volume=100 μL/well) consisting of 20 mM HEPES (pH 7.2), ATP (0.2 μM ATP for JAK1 and JAK2 and 0.1 μM ATP for JAK3), 1 mM MnCl₂, 0.1% BSA, and CEP-33779 (diluted in DMSO, 2.5% DMSO final in assay) is added to the assay plate. Enzyme is added and the reaction is allowed to proceed for 20 min at room temperature. Detection of the phosphorylated product is performed by adding 100 μL/well of diluted Eu-N1 labeled PY100 antibody. Samples are incubated at RT for 1 h, followed by addition of 100 μL enhancement solution. Plates are agitated for 10 min, and the fluorescence of the resulting solution is measured. IC₅₀ values are determined^[1].

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

Animal Administration^[1]

Mice: Nude mice bearing CWR22 xenografts are dosed orally with 55 mg/kg of CEP-33779 or a vehicle (PEG400). At 2, 6, and 24 h after dosing animals (3/group) are sacrificed, tumors are excised and plasma samples are prepared. Tumor extracts are prepared using Triton-based extraction buffer supplemented with inhibitors of proteases and phosphatases. Equal amounts of extracts are resolved on SDS-PAGE gels and STAT3 phosphorylation and expression are analyzed by Western blot using specific antibodies^[1].

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Portuguese - PT (396 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]. Dugan BJ, et al. A selective, orally bioavailable 1,2,4-triazolo[1,5-a]pyridine-based inhibitor of Janus kinase 2 for use in anticancer therapy: discovery of CEP-33779. J Med Chem. 2012 Jun 14;55(11):5243-54. [Content Brief]

[2]. Seavey MM, et al. Therapeutic efficacy of CEP-33779, a novel selective JAK2 inhibitor, in a mouse model of colitis-induced colorectal cancer. Mol Cancer Ther. 2012 Apr;11(4):984-93. [Content Brief]

[3]. Tang SJ, et al. CEP-33779 antagonizes ATP-binding cassette subfamily B member 1 mediated multidrug resistance by inhibiting its transport function. Biochem Pharmacol. 2014 Sep 15;91(2):144-56. [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	2.1618 mL	10.8092 mL	21.6183 mL	54.0459 mL
	5 mM	0.4324 mL	2.1618 mL	4.3237 mL	10.8092 mL
	10 mM	0.2162 mL	1.0809 mL	2.1618 mL	5.4046 mL
	15 mM	0.1441 mL	0.7206 mL	1.4412 mL	3.6031 mL

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CEP-33779

Epigenetics Compound Library

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Differentiation Inducing Compound Library

Reprogramming Compound Library

Orally Active Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Obesity Compound Library

Anti-Liver Cancer Compound Library

Human Metabolite Library

Anti-Prostate Cancer Compound Library

Cancer Stem Cells Compound Library

Pain-Related Compound Library

Autoimmune Disease Compound Library

Highly Selective Inhibitors Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Mass Spectrometry Human Metabolite Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) CEP-33779

All JAK Isoforms

Biological Activity

Chemical Information

Publications (5)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

CEP-33779 Related Classifications

Cat. No.: HY-15343