ChemicalBook > CAS DataBase List > UNC-2371A

UNC-2371A

Product Name: UNC-2371A
CAS No.: 1429882-07-4
Chemical Name: UNC-2371A
Synonyms: UNC2371;MRX-2843;UNC-2371A;UNC2371;MRX-2843;MRX-2843 (UNC2371);MRX-2843, 10 mM in DMSO;MRX-2843?(Synonyms: UNC2371;(1r,4r)-4-(2-(2-cyclopropylethylamino)-5-(4-((4-methylpiperazin-1-yl)methyl)phenyl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl)cyclohexanol;trans-4-(2-((2-Cyclopropylethyl)amino)-5-(4-((4-methylpiperazin-1-yl)methyl)phenyl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl)cyclohexanol;trans-4-[2-[(2-Cyclopropylethyl)amino]-5-[4-[(4-methyl-1-piperazinyl)methyl]phenyl]-7H-pyrrolo[2,3-d]pyrimidin-7-yl]cyclohexanol
CBNumber: CB73168663
Molecular Formula: C29H40N6O
Formula Weight: 488.67
MOL File: 1429882-07-4.mol

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UNC-2371A Property

Melting point:: >137°C (dec.)
Boiling point:: 697.3±65.0 °C(Predicted)
Density: 1.31±0.1 g/cm3(Predicted)
storage temp.: Refrigerator
solubility: Chloroform (Slightly), DMSO (Slightly), Methanol (Slightly, Heated, Sonicated)
pka: 14.63±0.40(Predicted)
form: Solid
color: White to Pale Beige

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P271Use only outdoors or in a well-ventilated area.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P312Call a POISON CENTER or doctor/physician if you feel unwell.

P321Specific treatment (see … on this label).

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

P403+P233Store in a well-ventilated place. Keep container tightly closed.

P405Store locked up.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 27923
Product name: MRX-2843
Packaging: 1mg
Price: $49
Updated: 2024/03/01

Cayman Chemical

Product number: 27923
Product name: MRX-2843
Packaging: 10mg
Price: $333
Updated: 2024/03/01

Cayman Chemical

Product number: 27923
Product name: MRX-2843
Packaging: 5mg
Price: $179
Updated: 2024/03/01

TRC

Product number: M750145
Product name: MRX-2843
Packaging: 25mg
Price: $545
Updated: 2021/12/16

ChemScene

Product number: CS-8117
Product name: MRX-2843
Purity: 99.70%
Packaging: 10mg
Price: $672
Updated: 2021/12/16

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UNC-2371A Chemical Properties,Usage,Production

Description

MRX-2843 is an inhibitor of Mer and FMS-like tyrosine kinase 3 (FLT3; IC₅₀s = 1.3 and 1 nM, respectively). It also inhibits Axl and Tyro3 (IC₅₀s = 15 and 17 nM, respectively). MRX-2843 (10-300 nM) inhibits Mer phosphorylation in MOLM-14 and MV4-11 acute myeloid leukemia (AML) cells and reduces clonal expansion of Kasumi-1 AML cells (IC₅₀ = 143.5 nM). In vivo, MRX-2843 increases survival in NOMO-1 and MOLM-14 AML mouse xenograft models when administered at doses of 65 and 50 mg/kg, respectively.

Uses

MRX-2843, is an orally available small-molecule inhibitor of both MERTK and FLT3.

in vivo

MRX-2843 is 78% orally bioavailable at a dose of 3 mg/kg with a C_max of 1.3 μM and a t_1/2 of 4.4 hours. In MOLM-14 parental xenografts, both quizartinib and MRX-2843 increase median survival compare with that of vehicle-treated mice (172.5 days versus 40 days and 121 days versus 36 days, respectively, P<0.001). In this model, quizartinib is more effective than MRX-2843 (P<0.005), although higher doses of MRX-2843 are not evaluated. In MOLM-14:D835Y xenografts, quizartinib prolongs survival compare with that of vehicle-treated mice, but the effect is minimal (median survival 45 days vs. 36 days, P<0.001). In MOLM-14:F691L xenografts, treatment with MRX-2843 prolongs survival by almost 2-fold in NSG and NSGS mice (median survival 87 vs. 44.5 days and 87 vs. 48 days, respectively, P<0.005). Increased survival is observed in response to treatment with MRX-2843 versus quizartinib, but the difference is only significant in NSG mice^[1].

References

[1] WEIHE ZHANG. UNC2025, a Potent and Orally Bioavailable MER/FLT3 Dual Inhibitor[J]. Journal of Medicinal Chemistry, 2014, 57 16: 7031-7041. DOI: 10.1021/jm500749d
[2] KATHERINE A MINSON. The MERTK/FLT3 inhibitor MRX-2843 overcomes resistance-conferring FLT3 mutations in acute myeloid leukemia.[J]. JCI insight, 2016, 1 3: e85630. DOI: 10.1172/jci.insight.85630

UNC-2371A Preparation Products And Raw materials

Raw materials

Preparation Products

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UNC-2371A Suppliers

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1429882-07-4, UNC-2371ARelated Search:

(1r,4r)-4-(2-(2-cyclopropylethylamino)-5-(4-((4-methylpiperazin-1-yl)methyl)phenyl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl)cyclohexanol

UNC-2371A

MRX-2843 (UNC2371)

MRX-2843

UNC2371

UNC2371;MRX-2843

Cyclohexanol, 4-[2-[(2-cyclopropylethyl)amino]-5-[4-[(4-methyl-1-piperazinyl)methyl]phenyl]-7H-pyrrolo[2,3-d]pyrimidin-7-yl]-, trans-

MRX-2843?(Synonyms: UNC2371

UNC 2371,FLT3,Fms like tyrosine kinase 3,CD135,inhibit,MRX2843,Cluster of differentiation antigen 135,UNC-2371,Inhibitor,MRX-2843,MRX 2843

trans-4-(2-((2-Cyclopropylethyl)amino)-5-(4-((4-methylpiperazin-1-yl)methyl)phenyl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl)cyclohexanol

MRX-2843, 10 mM in DMSO

trans-4-[2-[(2-Cyclopropylethyl)amino]-5-[4-[(4-methyl-1-piperazinyl)methyl]phenyl]-7H-pyrrolo[2,3-d]pyrimidin-7-yl]cyclohexanol

(1r,4r)-4-(2-((2-cyclopropylethyl)amino)-5-(4-((4-methylpiperazin-1-yl)methyl)phenyl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl)cyclohexan-1-ol

1429882-07-4

C29H40N6O