WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 207083
Description: MRX-2843, also known as UNC2371, is a potent and orally active MERTK and FLT3 inhibitor. MRX-2843 overcomes resistance-conferring FLT3 mutations in acute myeloid leukemia. MRX-2843 in combination with an irreversible EGFR TKI as a novel strategy for treatment of patients with wtEGFR NSCLC. MRX-2843 treatment induces apoptosis and inhibits colony formation in AML cell lines and primary patient samples expressing MERTK and/or FLT3-ITD, with a wide therapeutic window compared with that of normal human cord blood cells.
MedKoo Cat#: 207083
Chemical Formula: C29H40N6O
Exact Mass: 488.3264
Molecular Weight: 488.68
Elemental Analysis: C, 71.28; H, 8.25; N, 17.20; O, 3.27
Related CAS #: 1429882-07-4
Synonym: MRX-2843; MRX 2843; MRX2843; UNC2371; UNC-2371; UNC 2371; UNC2371A; UNC-2371A; UNC 2371A;
IUPAC/Chemical Name: (1r,4r)-4-(2-((2-cyclopropylethyl)amino)-5-(4-((4-methylpiperazin-1-yl)methyl)phenyl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl)cyclohexanol
InChi Key: LBEJYFVJIPQSNX-SOAUALDESA-N
InChi Code: InChI=1S/C29H40N6O/c1-33-14-16-34(17-15-33)19-22-4-6-23(7-5-22)27-20-35(24-8-10-25(36)11-9-24)28-26(27)18-31-29(32-28)30-13-12-21-2-3-21/h4-7,18,20-21,24-25,36H,2-3,8-17,19H2,1H3,(H,30,31,32)/t24-,25-
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
Appearance: Solid powder
Purity: >95% (or refer to the Certificate of Analysis)
Shipping Condition: 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 Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >3 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
The following data is based on the product molecular weight 488.68 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.15 mL||5.76 mL||11.51 mL|
|5 mM||0.23 mL||1.15 mL||2.3 mL|
|10 mM||0.12 mL||0.58 mL||1.15 mL|
|50 mM||0.02 mL||0.12 mL||0.23 mL|
1: Lee-Sherick AB, Jacobsen KM, Henry CJ, Huey MG, Parker RE, Page LS, Hill AA,
Wang X, Frye SV, Earp HS, Jordan CT, DeRyckere D, Graham DK. MERTK inhibition
alters the PD-1 axis and promotes anti-leukemia immunity. JCI Insight. 2018 Nov
2;3(21). pii: 97941. doi: 10.1172/jci.insight.97941. [Epub ahead of print] PubMed
PMID: 30385715; PubMed Central PMCID: PMC6238750.
2: Yan D, Parker RE, Wang X, Frye SV, Earp HS 3rd, DeRyckere D, Graham DK. MERTK
Promotes Resistance to Irreversible EGFR Tyrosine Kinase Inhibitors in Non-small
Cell Lung Cancers Expressing Wild-type EGFR Family Members. Clin Cancer Res. 2018
Dec 15;24(24):6523-6535. doi: 10.1158/1078-0432.CCR-18-0040. Epub 2018 Sep 7.
PubMed PMID: 30194074.
3: Minson KA, Smith CC, DeRyckere D, Libbrecht C, Lee-Sherick AB, Huey MG,
Lasater EA, Kirkpatrick GD, Stashko MA, Zhang W, Jordan CT, Kireev D, Wang X,
Frye SV, Earp HS, Shah NP, Graham DK. The MERTK/FLT3 inhibitor MRX-2843 overcomes
resistance-conferring FLT3 mutations in acute myeloid leukemia. JCI Insight. 2016
Mar;1(3):e85630. doi: 10.1172/jci.insight.85630. PubMed PMID: 27158668; PubMed
Central PMCID: PMC4855528.