MTX-23 free base · Synonyms: MTX 23 · MTX23

MTX-23 is a PROTAC degrader targeting androgen receptor splice variant 7 (AR-V7) and full-length androgen receptor (AR-FL), with DC50 values of 0.37…

For research use only. Not for human or veterinary use.

Target PROTACs Androgen Receptor Apoptosis

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

MTX-23 structure

CAS No.: 2488296-74-6

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
5 mg	USD 480.00	BP-02426-5mg	In stock	Get quote
10 mg	USD 770.00	BP-02426-10mg	In stock	Get quote
25 mg	USD 1,540.00	BP-02426-25mg	In stock	Get quote
50 mg	USD 2,450.00	BP-02426-50mg	In stock	Get quote
100 mg	USD 3,930.00	BP-02426-100mg	In stock	Get quote
250 mg	Inquire	BP-02426-250mg	In stock	Inquire

Need another size or custom synthesis? Request a quote.

Description

MTX-23 is a PROTAC degrader targeting androgen receptor splice variant 7 (AR-V7) and full-length androgen receptor (AR-FL), with DC50 values of 0.37 μM and 2 μM, respectively. MTX-23 binds to the DNA-binding domains of AR-V7 and AR-FL, recruits the VHL E3 ubiquitin ligase (E3 ubiquitin ligase) and induces their degradation. MTX-23 reduces the proliferation of prostate cancer cells, promotes their apoptosis (apoptosis), and also inhibits tumor growth in mouse models. MTX-23 can be used for the research of prostate cancer .

Biological activity

In Vitro MTX-23 degrades AR-V7 with a DC50 of 0.37 μmol/L and AR-FL with a DC50 of 2 μmol/L as measured by immunoblot analysis. MTX-23 inhibits proliferation and increases apoptosis in androgen-responsive prostate cancer cells, with this antiproliferative effect dependent on the presence of AR-V7 and AR-FL. MTX-23 inhibits proliferation in 12 human prostate cancer cell lines resistant to second-line antiandrogen therapies.

Identifiers

SMILES: O=C(N1[C@@H](C[C@H](C1)O)C(N[C@H](C2=CC=C(C3=C(N=CS3)C)C=C2)C)=O)[C@H](C(C)(C)C)NC(CCCCNC(COC4=C(C5=CSC(N6CCOCC6)=N5)C=CC(F)=C4F)=O)=O
InChIKey: JOZGICGAZBMCJF-JMSDHYLISA-N

Specifications

MW (average): 882.0500
Formula: C₄₃H₅₃F₂N₇O₇S₂
CAS No.: 2488296-74-6
Physical state: Solid
Color: Off-white to light yellow
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20°C, 3 years , 4°C, 2 years ; In solvent -20°C, 1 month

Solubility

Soluble in DMSO : 100 mg/mL

Documents

References

[1].Lee GT, et al. Effects of MTX-23, a Novel PROTAC of Androgen Receptor Splice Variant-7 and Androgen Receptor, on CRPC Resistant to Second-Line Antiandrogen Therapy. Mol Cancer Ther. 2021 Mar;20(3):490-499.

Same target

Search PROTACs

Same research area

Search Cancer