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Chemical Structure| 1429882-07-4 Chemical Structure| 1429882-07-4

Structure of MRX-2843
CAS No.: 1429882-07-4

Chemical Structure| 1429882-07-4

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MRX-2843 (UNC2371) is an orally active, ATP-competitive MERTK and FLT3 tyrosine kinase inhibitor (TKI) with IC50 values of 1.3 nM and 0.64 nM, respectively.

Synonyms: UNC2371

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Product Details of MRX-2843

CAS No. :1429882-07-4
Formula : C29H40N6O
M.W : 488.67
SMILES Code : O[C@H]1CC[C@H](N2C=C(C3=CC=C(CN4CCN(C)CC4)C=C3)C5=CN=C(NCCC6CC6)N=C52)CC1
Synonyms :
UNC2371
MDL No. :MFCD28502224

Safety of MRX-2843

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 MRX-2843

RTK

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
GL261 88.6 nM MRX-2843 inhibits cell growth Neurooncol Adv. 2020 Jun 3;2(1):vdaa065
GSC407 217.7 nM 48 hours MRX-2843 inhibits cell growth and induces apoptosis Neurooncol Adv. 2020 Jun 3;2(1):vdaa065
GSC923 288.1 nM 48 hours MRX-2843 inhibits cell growth and induces apoptosis Neurooncol Adv. 2020 Jun 3;2(1):vdaa065
H1650 300 nM 3-4 days Evaluate the effect of MRX-2843 on EGFR-mutant NSCLC cells J Clin Invest. 2022 Aug 1;132(15):e150517
H4006 300 nM 3-4 days Evaluate the effect of MRX-2843 on EGFR-mutant NSCLC cells J Clin Invest. 2022 Aug 1;132(15):e150517
NOMO-1 150-300 nM 72 hours MRX-2843 induced apoptosis and inhibited colony formation. JCI Insight. 2016 Mar;1(3):e85630
Kasumi-1 10-300 nM 1 hour MRX-2843 inhibited MERTK phosphorylation and downstream signaling pathways ERK1/2, AKT, and STAT6, leading to apoptosis and reduced colony formation. JCI Insight. 2016 Mar;1(3):e85630
U251 95.5 nM 48 hours MRX-2843 inhibits cell growth and induces apoptosis Neurooncol Adv. 2020 Jun 3;2(1):vdaa065
MV4-11 50-100 nM 72 hours MRX-2843 induced apoptosis and inhibited colony formation. JCI Insight. 2016 Mar;1(3):e85630
Jurkat cells 300 nM 48 hours MRX-2843 induced cell death Cancers (Basel). 2022 Dec 13;14(24):6142
PEER cells 10-100 nM 1 hour MRX-2843 inhibited MERTK activation with IC50 of 3.9 nM Cancers (Basel). 2022 Dec 13;14(24):6142
Loucy cells 10-100 nM 1 hour MRX-2843 inhibited MERTK activation with IC50 of 9.5 nM Cancers (Basel). 2022 Dec 13;14(24):6142
MOLM-14 50 nM 48 hours MRX-2843 inhibited FLT3-ITD activation and downstream signaling pathways, leading to apoptosis and reduced colony formation. JCI Insight. 2016 Mar;1(3):e85630
HMC-3 100 nM MRX-2843 decreases cell viability Neurooncol Adv. 2020 Jun 3;2(1):vdaa065
Jurkat (T-ALL) 100 nM MRX-2843 and 1.4 nM vincristine 72 hours To evaluate the synergistic effect of MRX-2843 and vincristine, results showed that the combination significantly inhibited cell growth. J Control Release. 2023 Sep;361:470-482
TC32 cells 178-297 nM (IC50) 72 hours MRX-2843 resulted in a dose-dependent reduction in cell density with IC50 values ranging from 178 to 297 nM. Cancers (Basel). 2024 Aug 12;16(16):2831
RD-ES cells 178-297 nM (IC50) 72 hours MRX-2843 resulted in a dose-dependent reduction in cell density with IC50 values ranging from 178 to 297 nM. Cancers (Basel). 2024 Aug 12;16(16):2831
SK-ES-1 cells 178-297 nM (IC50) 72 hours MRX-2843 resulted in a dose-dependent reduction in cell density with IC50 values ranging from 178 to 297 nM. Cancers (Basel). 2024 Aug 12;16(16):2831
TC106 cells 34.5 nM (IC50) 1 hour MRX-2843 decreased phosphorylation of MERTK in a dose-dependent manner with an IC50 of 34.5 nM. Cancers (Basel). 2024 Aug 12;16(16):2831
A673 cells 13.3 nM (IC50) 1 hour MRX-2843 decreased phosphorylation of MERTK in a dose-dependent manner with an IC50 of 13.3 nM. Cancers (Basel). 2024 Aug 12;16(16):2831
697 B-ALL cells 5-25 nM to >250 nM Evaluate the inhibitory effect of MRX-2843 on MERTK phosphorylation JCI Insight. 2018 Nov 2;3(21):e97941
human alveolar bone mesenchymal stem cells 100 nM 21 days To evaluate the effect of MRX-2843 on osteogenic differentiation of alveolar bone MSCs. Results showed enhanced mineralization with MRX-2843 treatment. J Dent Res. 2023 Sep;102(10):1131-1140

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Nude-Foxn1nu mice H4006 xenograft model Oral gavage 3 mg/kg OSI and 20 mg/kg MRX-2843 OSI once daily and MRX-2843 twice daily for 57 days Evaluate the effect of MRX-2843 in combination with OSI on tumor growth in EGFR-mutant NSCLC J Clin Invest. 2022 Aug 1;132(15):e150517
Nude mice A673 xenograft model Intraperitoneal injection 10 mg/kg Twice a week for 28 days MRX-2843 enhances irinotecan-mediated tumor growth suppression effects in Ewing sarcoma murine models Nat Commun. 2024 Jun 21;15(1):5292
Mice Xenograft model Oral 50-75 mg/kg Once daily until study end MRX-2843 significantly prolonged survival in xenograft models of FLT3-ITD or MERTK-positive AML. JCI Insight. 2016 Mar;1(3):e85630
NSG mice Jurkat T-ALL cell line xenograft model Oral 75 mg/kg Once daily for 28 days MRX-2843 significantly reduced disease burden and prolonged survival Cancers (Basel). 2022 Dec 13;14(24):6142
Mice GL261 syngeneic orthotopic glioblastoma model Oral gavage 50 mg/kg Daily for 14 days MRX-2843 extends survival and reduces immunosuppression and angiogenesis in the tumor microenvironment Neurooncol Adv. 2020 Jun 3;2(1):vdaa065
Mice 697 B-ALL xenograft model Oral 3, 25, or 75 mg/kg single oral dose Assessed at 1 or 24 hours after single dose Evaluate the inhibitory effect of MRX-2843 on MERTK phosphorylation in vivo JCI Insight. 2018 Nov 2;3(21):e97941

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT03510104 Advanced Cancer|Metastatic Can... More >>cer|Neoplasms|Neoplasm Metastasis|Neoplastic Processes|Pathologic Processes Less << PHASE1 ACTIVE_NOT_RECRUITING 2025-04-25 Emory University, Atlanta, Geo... More >>rgia, 30322, United States|Lineberger Comprehensive Cancer Center, Chapel Hill, North Carolina, 27514, United States Less <<
NCT04872478 Acute Myeloid Leukemia|Acute L... More >>ymphoblastic Leukemia|Mixed Phenotype Acute Leukemia Less << PHASE1 RECRUITING 2026-03-31 Emory University - WINSHIP Can... More >>cer Center, Atlanta, Georgia, 30322, United States|Emory University, Children's Healthcare of Atlanta, Atlanta, Georgia, 30322, United States|Memorial Sloan Kettering Cancer Center, New York, New York, 10065, United States Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.05mL

0.41mL

0.20mL

10.23mL

2.05mL

1.02mL

20.46mL

4.09mL

2.05mL

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
 

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