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Chemical Structure| 2630904-45-7 Chemical Structure| 2630904-45-7

Structure of MRTX-1719
CAS No.: 2630904-45-7

Chemical Structure| 2630904-45-7

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MRTX-1719 is a selective inhibitor of the PRMT5•MTA complex that effectively binds to and inhibits the PRMT5•MTA complex. It shows anti-tumor activity in cancer research.

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Product Details of MRTX-1719

CAS No. :2630904-45-7
Formula : C23H18ClFN6O2
M.W : 464.88
SMILES Code : N#CC1=C(OC2CC2)C=C(Cl)C(F)=C1C3=C(C=NN3C)C=4C=CC=5C(=O)NN=C(C5C4)CN
MDL No. :N/A
InChI Key :BZKIOORWZAXIBA-UHFFFAOYSA-N
Pubchem ID :156151242

Safety of MRTX-1719

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319
Precautionary Statements:P501-P270-P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313-P301+P312+P330

Related Pathways of MRTX-1719

epigenetics

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Murine CD8+ T cells 0.1 μM and 0.5 μM 3 days Evaluate the effect of MRTX1719 on T cell function. Results showed MRTX1719 reduced SDMA levels at high concentration but had minimal impact on cytokine production and cytotoxicity. J Immunother Cancer. 2024 Sep 23;12(9):e009600
B16 Mtap-KO tumor cells 0.1 μM and 0.5 μM 5 days Evaluate the effect of MRTX1719 on growth and SDMA levels in MTAP-deleted tumor cells. Results showed MRTX1719 significantly inhibited growth and reduced SDMA levels in Mtap-KO cells but had minimal effects on WT cells. J Immunother Cancer. 2024 Sep 23;12(9):e009600
MC38/gp100 Mtap-KO tumor cells 0.1 μM and 0.5 μM 5 days Evaluate the effect of MRTX1719 on growth and SDMA levels in MTAP-deleted tumor cells. Results showed MRTX1719 significantly inhibited growth and reduced SDMA levels in Mtap-KO cells but had minimal effects on WT cells. J Immunother Cancer. 2024 Sep 23;12(9):e009600
MTAP-deleted CRC cell lines 9.14, 27.43, 82.3, 246.9 nM 7 days Evaluate the growth inhibitory effect of MRTX1719 on MTAP-deleted CRC cell lines, showing high sensitivity of MTAP-deleted cells to MRTX1719. Mol Oncol. 2024 Jun;18(6):1460-1485

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6 mice MC38/gp100 Mtap-KO and B16 Mtap-KO tumor models Oral 30 mg/kg/day Once daily for 7 or 14 days Evaluate the antitumor efficacy of MRTX1719 in combination with anti-PD-1 in MTAP-deleted tumors. Results showed combination therapy significantly inhibited tumor growth and improved survival. J Immunother Cancer. 2024 Sep 23;12(9):e009600
BALB/c nude mice Subcutaneous xenograft model Intraperitoneal injection 10 mg/kg Once daily, continuous treatment Evaluate the inhibitory effect of MRTX-1719 on MTAP-deficient gliomas in vivo, results showed that MRTX-1719 significantly reduced the volume of Hs683 xenografts, but the inhibitory effect was weakened in mixed xenografts Cancer Med. 2024 Dec;13(24):e70526

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.15mL

0.43mL

0.22mL

10.76mL

2.15mL

1.08mL

21.51mL

4.30mL

2.15mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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