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Cat. No.: HY-159570

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XD2-149

XD2-149 is a PROTAC targeting STAT3. XD2-149 consists of PROTAC target protein ligand Napabucasin (HY-13919) (red part), E3 ligase Thalidomide (HY-14658) (black part), and linker NH2-C5-Azacyclohexane-N-Boc (HY-159572) (blue part). The E3 ligase + linker conjugate is Thalidomide-NH-C5-azacyclohexane-N-Boc (HY-159571), and the active control of the target protein ligand is Thalidomide acid (HY-159573)^{[1]^{.

(Pink: STAT3 ligand (HY-13919); Blue: Cereblon ligand (HY-14658); Black: linker (HY-159572)).}}

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

CAS No.: 2710221-08-0
Formula: C₃₈H₃₉N₅O₈
Molecular Weight:693.74

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (265 KB)

XD2-149 Chemical Structure

CAS No.: 2710221-08-0

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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
- Cellular Effect
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Bioz

Biological Activity

Description

XD2-149 is a PROTAC targeting STAT3. XD2-149 consists of PROTAC target protein ligand Napabucasin (HY-13919) (red part), E3 ligase Thalidomide (HY-14658) (black part), and linker NH2-C5-Azacyclohexane-N-Boc (HY-159572) (blue part). The E3 ligase + linker conjugate is Thalidomide-NH-C5-azacyclohexane-N-Boc (HY-159571), and the active control of the target protein ligand is Thalidomide acid (HY-159573)^{[1]^{.
(Pink: STAT3 ligand (}HY-13919); Blue: Cereblon ligand (HY-14658); Black: linker (HY-159572)).}

IC₅₀ & Target

STAT3^[1]

All PROTACs Isoforms :

All STAT Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
BXPC-3	IC₅₀	0.8 μM Compound: 3-6d; XD2-149	Antiproliferative activity against human BxPC-3 cells assessed as reduction in cell viability incubated for 3 days by MTT assay Antiproliferative activity against human BxPC-3 cells assessed as reduction in cell viability incubated for 3 days by MTT assay	[PMID: 33506674]
BXPC-3	IC₅₀	1.2 μM Compound: 3-6d; XD2-149	Antiproliferative activity against human BxPC-3 cells harboring ZFP91siRNA assessed as reduction in cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human BxPC-3 cells harboring ZFP91siRNA assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 33506674]
BXPC-3	IC₅₀	2.1 μM Compound: 3-6d; XD2-149	Antiproliferative activity against ZFP91 knockdown human BxPC-3 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against ZFP91 knockdown human BxPC-3 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 33506674]
HEK293	IC₅₀	8.7 μM Compound: 3-6d; XD2-149	Antiproliferative activity against human HEK293 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay Antiproliferative activity against human HEK293 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay	[PMID: 33506674]
MIA PaCa-2	IC₅₀	1 μM Compound: 3-6d; XD2-149	Antiproliferative activity against human MIA PaCa-2 cells assessed as reduction in cell viability incubated for 3 days by MTT assay Antiproliferative activity against human MIA PaCa-2 cells assessed as reduction in cell viability incubated for 3 days by MTT assay	[PMID: 33506674]

Chemical Information

CAS No. 2710221-08-0
Molecular Weight 693.74
Formula C₃₈H₃₉N₅O₈
SMILES

O=C(C1=CC2=C(C(C3=C(C2=O)C=CC=C3)=O)O1)NCCN4CCC(CCCCCNC5=CC=CC(C(N6C7C(NC(CC7)=O)=O)=O)=C5C6=O)CC4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (265 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]. Hanafi M, et al. Discovery of a Napabucasin PROTAC as an Effective Degrader of the E3 Ligase ZFP91. J Med Chem. 2021 Feb 11;64(3):1626-1648. [Content Brief]

Calculators

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

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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.

Keywords

100 mg

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Biological Activity
- Description
- IC₅₀ & Target
Chemical Information
Purity & Documentation
References

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XD2-149

All PROTACs Isoforms

All STAT Isoforms