MedKoo Biosciences

MRX-2843
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 207083

CAS#: 1429882-07-4

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.

Chemical Structure

MRX-2843

CAS# 1429882-07-4

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 207083
Name: MRX-2843
CAS#: 1429882-07-4
Chemical Formula: C29H40N6O
Exact Mass: 488.33
Molecular Weight: 488.680
Elemental Analysis: C, 71.28; H, 8.25; N, 17.20; O, 3.27

Price and Availability

Size	Price	Availability
5mg	USD 350	2 Weeks
10mg	USD 600	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

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

More Info:

Product Data:

Product Data

Instruction:

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Biological target:	MRX-2843 (UNC2371) is an orally active, ATP-competitive dual MERTK and FLT3 tyrosine kinases inhibitor (TKI) with enzymatic IC50s of 1.3 nM for MERTK and 0.64 nM for FLT3.
In vitro activity:	Indeed, treatment with MRX-2843, a first-in-class MERTK kinase inhibitor, resensitized GAS6-treated NSCLC cells to OSI. Functionally, OSIR cells were more sensitive to MRX-2843 than parental cells, suggesting acquired dependence on MERTK signaling. Reference: J Clin Invest. 2022 Aug 1;132(15):e150517. https://pubmed.ncbi.nlm.nih.gov/35708914/
In vivo activity:	A MERTK-selective tyrosine kinase inhibitor, MRX-2843, mediated therapeutic anti-leukemia effects in immunocompromised mice bearing a MERTK-expressing human leukemia xenograft. In addition, inhibition of host MERTK by genetic deletion (Mertk-/- mice) or treatment with MRX-2843 significantly decreased tumor burden and prolonged survival in immune-competent mice inoculated with a MERTK-negative ALL, suggesting immune-mediated therapeutic activity. Reference: JCI Insight. 2018 Nov 2;3(21):e97941. https://pubmed.ncbi.nlm.nih.gov/30385715/

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	34.5	70.60
	Ethanol	25.0	51.16

Preparing Stock Solutions

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

Formulation protocol:	1. Yan D, Huelse JM, Kireev D, Tan Z, Chen L, Goyal S, Wang X, Frye SV, Behera M, Schneider F, Ramalingam SS, Owonikoko T, Earp HS, DeRyckere D, Graham DK. MERTK activation drives osimertinib resistance in EGFR-mutant non-small cell lung cancer. J Clin Invest. 2022 Aug 1;132(15):e150517. doi: 10.1172/JCI150517. PMID: 35708914; PMCID: PMC9337831. 2. 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. PMID: 27158668; PMCID: PMC4855528. 3. Su YT, Butler M, Zhang M, Zhang W, Song H, Hwang L, Tran AD, Bash RE, Schorzman AN, Pang Y, Yu G, Zamboni WC, Wang X, Frye SV, Miller CR, Maric D, Terabe M, Gilbert MR, Earp Iii HS, Wu J. MerTK inhibition decreases immune suppressive glioblastoma-associated macrophages and neoangiogenesis in glioblastoma microenvironment. Neurooncol Adv. 2020 Jun 3;2(1):vdaa065. doi: 10.1093/noajnl/vdaa065. PMID: 32642716; PMCID: PMC7324055. 4. 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):e97941. doi: 10.1172/jci.insight.97941. Erratum in: JCI Insight. 2020 Dec 3;5(23): PMID: 30385715; PMCID: PMC6238750.
In vitro protocol:	1. Yan D, Huelse JM, Kireev D, Tan Z, Chen L, Goyal S, Wang X, Frye SV, Behera M, Schneider F, Ramalingam SS, Owonikoko T, Earp HS, DeRyckere D, Graham DK. MERTK activation drives osimertinib resistance in EGFR-mutant non-small cell lung cancer. J Clin Invest. 2022 Aug 1;132(15):e150517. doi: 10.1172/JCI150517. PMID: 35708914; PMCID: PMC9337831. 2. 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. PMID: 27158668; PMCID: PMC4855528.
In vivo protocol:	1. Su YT, Butler M, Zhang M, Zhang W, Song H, Hwang L, Tran AD, Bash RE, Schorzman AN, Pang Y, Yu G, Zamboni WC, Wang X, Frye SV, Miller CR, Maric D, Terabe M, Gilbert MR, Earp Iii HS, Wu J. MerTK inhibition decreases immune suppressive glioblastoma-associated macrophages and neoangiogenesis in glioblastoma microenvironment. Neurooncol Adv. 2020 Jun 3;2(1):vdaa065. doi: 10.1093/noajnl/vdaa065. PMID: 32642716; PMCID: PMC7324055. 2. 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):e97941. doi: 10.1172/jci.insight.97941. Erratum in: JCI Insight. 2020 Dec 3;5(23): PMID: 30385715; PMCID: PMC6238750.

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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.

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