Cat. No.: HY-154984

JET-209

Name: JET-209
Brand: MedChemExpress
SKU: HY-154984
Price: 540.00 USD
Availability: InStock
Rating: 5 (1 reviews)

고객리뷰

Based on 1 Customer Validation

JET-209 is a potent CBP/p300 PROTAC degrader, with DC₅₀ values of 0.05 nM and 0.2 nM for CBP and p300. JET-209 demonstrates remarkable anti-tumor activity against various acute leukemia cell lines and effectively inhibits tumor growth in xenograft tumor models. JET-209 can be used for the study of acute leukemia.
(Pink: CBP/p300 Target protein ligand; Blue: Cereblon ligand (HY-132248); Black: linker).

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

Purity : 99.27%
CAS No.: 3033714-58-5
화학식: C₄₆H₄₇N₉O₆
분자량:821.92

보관:

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

JET-209 Chemical Structure

CAS No.: 3033714-58-5

사이즈

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재고

수량

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biological Activity
- 제품 설명
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
용액&용해도
- In Vitro
- In Vivo
Protocol (6)
순도&문서
References
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

JET-209 is a potent CBP/p300 PROTAC degrader, with DC₅₀ values of 0.05 nM and 0.2 nM for CBP and p300. JET-209 demonstrates remarkable anti-tumor activity against various acute leukemia cell lines and effectively inhibits tumor growth in xenograft tumor models. JET-209 can be used for the study of acute leukemia^[1]. (Pink: CBP/p300 Target protein ligand; Blue: Cereblon ligand (HY-132248); Black: linker).

IC₅₀ & Target

^[1]

CBP

0.05 nM (DC₅₀)

p300

0.2 nM (DC₅₀)

Cereblon

All Histone Acetyltransferase Isoforms :

All PROTACs Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
HL-60	IC₅₀	0.54 nM Compound: 24; JET-209	Cytotoxicity against human HL-60 cells assessed as inhibition of cell growth incubated for 4 days by cellTiter-Glo assay Cytotoxicity against human HL-60 cells assessed as inhibition of cell growth incubated for 4 days by cellTiter-Glo assay	[PMID: 37276143]
MOLM-13	IC₅₀	2.3 nM Compound: 24; JET-209	Cytotoxicity against human MOLM-13 cells assessed as inhibition of cell growth incubated for 4 days by cellTiter-Glo assay Cytotoxicity against human MOLM-13 cells assessed as inhibition of cell growth incubated for 4 days by cellTiter-Glo assay	[PMID: 37276143]
MV4-11	IC₅₀	0.04 nM Compound: 24; JET-209	Cytotoxicity against human MV4-11 cells assessed as inhibition of cell growth incubated for 4 days by cellTiter-Glo assay Cytotoxicity against human MV4-11 cells assessed as inhibition of cell growth incubated for 4 days by cellTiter-Glo assay	[PMID: 37276143]
RS4-11	IC₅₀	0.1 nM Compound: 24; JET-209	Cytotoxicity against human RS4-11 cells assessed as inhibition of cell growth incubated for 4 days by cellTiter-Glo assay Cytotoxicity against human RS4-11 cells assessed as inhibition of cell growth incubated for 4 days by cellTiter-Glo assay	[PMID: 37276143]

In Vitro

JET-209 exhibits strong antiproliferative activity against MV4;11 (IC₅₀ = 0.04 nM), HL-60 (IC₅₀ = 0.54 nM), MOLM-13 (IC₅₀ = 2.3 nM) and RS4;11 cells (IC₅₀ = 0.1 nM)^[1].
JET-209 (1 nM- 1 μM, 24 h) effectively induces G1 phase arrest in RS4;11 cells^[1].
FIP22 (1 nM- 1 μM, 8 h) potently and effectively suppresses the expression ofMYC and MYB genes in the RS4;11 cell line^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.

Cell Cycle Analysis^[1]

View Protocol

Cell Line:

RS4;11 cells
Concentration:

1, 10, 100, 1000 nM
Incubation Time:

24 h
Result:

Effectively induced G1 arrest at concentrations as low as 1 nM.

RT-PCR^[1]

View Protocol

Cell Line:

RS4;11 cells
Concentration:

1, 10, 100, 1000 nM
Incubation Time:

8 h
Result:

Effectively suppressed the expression ofMYC and MYB genes.

In Vivo

JET-209 (1-3 mg/kg, i.p., single dose) effectively depletes CBP/p300 proteins in RS4;11 xenograft tumors in mice^[1].
JET-209 (0.3-3 mg/kg, i.p., for 2 weeks) achieves strong tumor inhibition in RS4;11 and MV4;11 xenograft tumor mice models^[1].

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

Animal Model:

RS4;11 cells xenograft model established in female immunodeficient (SCID) mice^[1]
Dosage:

1 and 3 mg/kg
Administration:

Intraperitoneal injection (i.p.), single dose, twice a week (1 mg/kg) or once a week (3 mg/kg) for 2 weeks
Result:

Completely eliminated the CBP/p300 protein in the tumor within 3 to 6 hours at a single administration, and the protein level returned to normal 24 hours later.
Achieved 81% long-term tumor growth inhibition with continuous administration at 3 mg/kg.

Animal Model:

MV4;11 cells xenograft model established in female immunodeficient (SCID) mice^[1]
Dosage:

0.3 and 1 mg/kg
Administration:

Intraperitoneal injection (i.p.), 0.3 mg/kg once daily 5 days a week for 2 weeks or 1 mg/kg three times a week for 2 weeks
Result:

Demonstrated potent anti-tumor activity and has good safety profile.

Chemical Information

CAS No. 3033714-58-5
Appearance Solid
분자량 821.92
화학식 C₄₆H₄₇N₉O₆
Color Light yellow to yellow
SMILES

CC(N1CCC2=C(C(C3=CC=CC4=C3C=NC(C5=CN=C(C=C5)C(NC6CCN(CC6)C7=CC8=C(C(N(C8)C9CCC(NC9=O)=O)=O)C=C7)=O)=C4)=NN2C%10CCOCC%10)C1)=O
선적

Room temperature in continental US; may vary elsewhere.

보관

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

용액&용해도

In Vitro:

DMSO : 100 mg/mL (121.67 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

1.2167 mL

6.0833 mL

12.1666 mL

5 mM

0.2433 mL

1.2167 mL

2.4333 mL

10 mM

0.1217 mL

0.6083 mL

1.2167 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.

몰농도 계산기

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

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: 2.5 mg/mL (3.04 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL.

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 (3.04 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL.

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 (3.04 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL. 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

Protocol

All Animals and Diseases

Patient-Derived Xenograft (PDX)
Patient-derived xenograft (PDX) models are generated by engrafting primary human tumor tissue directly into immunodeficient mice, allowing in vivo propagation of patient tumor biology without initial in vitro adaptation. These models are used to preserve key histopathological and molecular characteristics of the original tumor and enable assessment of tumor growth dynamics and therapeutic response in a living organism. The biological readout is tumor engraftment and subsequent growth in the murine host, which reflects the ability of human tumor cells to survive, vascularize, and expand in an immunocompromised microenvironment.
Patient-Derived Orthotopic Xenograft (PDOX)
Patient-derived orthotopic xenograft (PDOX) modeling implants fresh patient tumor tissue or patient-derived tumor cells into the anatomically corresponding organ or tissue site of immunodeficient mice, usually by surgical orthotopic implantation, to preserve patient tumor histology, local microenvironmental context, invasion, metastatic behavior, and treatment-response features better than subcutaneous implantation. PDOX readouts include tumor engraftment, orthotopic tumor growth, local invasion, metastasis, recurrence after resection, histologic similarity to the donor tumor, biomarker retention, molecular concordance, survival, and response or resistance to therapy. PDOX models are used for preclinical drug testing and individualized therapy evaluation, but engraftment success varies by tumor type and specimen quality.
Splenic/Portal-Vein Liver Metastasis Xenograft
Splenic and portal-vein liver metastasis xenograft models deliver tumor cells into the portal circulation so that cells reach the liver first and form hepatic metastatic lesions; splenic injection uses the spleen as an access route to the portal system, while direct portal-vein injection introduces cells into the portal vein without requiring splenectomy. The assay detects liver colonization, intrahepatic tumor growth, tumor distribution, treatment response, survival, and liver-metastasis microenvironment changes; readouts include bioluminescence or fluorescence imaging, gross liver nodule counts, liver weight or tumor burden, histology, and survival.
Subcutaneous Cell-Line-Derived Xenograft
Subcutaneous cell-line-derived xenograft (CDX) models are established by implanting cultured human cancer cell lines into immunodeficient mice, where the injected cells form localized tumors that can be monitored in vivo as a measure of tumorigenic potential, growth kinetics, and treatment response. These models are widely used in oncology research because they allow reproducible tumor formation and enable comparative assessment of tumor growth between different cell lines or genetic manipulations in a controlled in vivo microenvironment. Subcutaneous implantation of cancer cells in immunodeficient mice is a standard approach for evaluating tumor growth behavior and therapeutic response across multiple cancer types, including prostate, esophageal, pancreatic, and colon cancer models.
Orthotopic Cell-Line Xenograft
Orthotopic cell-line xenograft models involve implantation of human cancer cell lines into the anatomically corresponding organ of immunodeficient mice to reproduce tumor growth within a native microenvironment, enabling more clinically relevant tumor behavior compared with subcutaneous models. These models are widely used because orthotopic placement better recapitulates tumor progression, including invasion and metastatic spread, which are often underrepresented in heterotopic implantation systems. Compared with conventional xenografts, orthotopic implantation is described as more technically complex but provides improved simulation of tumor-microenvironment interactions and metastatic behavior, making it particularly valuable for translational oncology research. Surgical orthotopic implantation approaches have been emphasized as enabling faithful reproduction of clinical cancer features, including metastasis and disease progression patterns that align with the tumor’s organ of origi
Intraperitoneal/Peritoneal Dissemination Xenograft
Intraperitoneal (IP) or peritoneal dissemination xenograft models are based on the introduction of human cancer cells into the peritoneal cavity of immunodeficient mice, where they attach to peritoneal surfaces, form multicellular aggregates or spheroids, and progressively generate disseminated tumor nodules that mimic advanced peritoneal metastatic disease. These models are widely used to study ovarian cancer progression, tumor-microenvironment interactions, and intraperitoneal therapeutic responses, often incorporating bioluminescence or fluorescence imaging to longitudinally monitor tumor burden in vivo. The biological principle relies on the capacity of tumor cells such as SKOV3 or related ovarian carcinoma lines to survive in suspension, aggregate within ascites-like fluid, adhere to mesothelial surfaces, and invade peritoneal organs, thereby recapitulating human peritoneal carcinomatosis patterns observed in advanced disease.

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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]. Thomas JE 2nd, et al. Discovery of Exceptionally Potent, Selective, and Efficacious PROTAC Degraders of CBP and p300 Proteins. J Med Chem. 2023 Jun 22;66(12):8178-8199. [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	1.2167 mL	6.0833 mL	12.1666 mL	30.4166 mL
	5 mM	0.2433 mL	1.2167 mL	2.4333 mL	6.0833 mL
	10 mM	0.1217 mL	0.6083 mL	1.2167 mL	3.0417 mL
	15 mM	0.0811 mL	0.4056 mL	0.8111 mL	2.0278 mL
	20 mM	0.0608 mL	0.3042 mL	0.6083 mL	1.5208 mL
	25 mM	0.0487 mL	0.2433 mL	0.4867 mL	1.2167 mL
	30 mM	0.0406 mL	0.2028 mL	0.4056 mL	1.0139 mL
	40 mM	0.0304 mL	0.1521 mL	0.3042 mL	0.7604 mL
	50 mM	0.0243 mL	0.1217 mL	0.2433 mL	0.6083 mL
	60 mM	0.0203 mL	0.1014 mL	0.2028 mL	0.5069 mL
	80 mM	0.0152 mL	0.0760 mL	0.1521 mL	0.3802 mL
	100 mM	0.0122 mL	0.0608 mL	0.1217 mL	0.3042 mL

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JET-209

All Histone Acetyltransferase Isoforms

All PROTACs Isoforms