MRTX-1133 Synthesis Route

MRTX-1133 Synthesis

MRTX-1133 (Synonyms: 4-[4-(3,8-Diazabicyclo[3.2.1]oct-3-yl)-8-fluoro-2-[[(2R,7aS)-2-fluorotetrahydro-1H-pyrrolizin-7a(5H)-yl]methoxy]pyrido[4,3-d]pyrimidin-7-yl]-5-ethynyl-6-fluoro-2-naphthalenol)

MRTX-1133 is an inhibitor of K-RasG12D, a mutant form of K-Ras that accumulates in cancer cells.1 It selectively reduces ERK phosphorylation in AsPC-1 cells expressing mutant K-RasG12D (IC50 = 10.8 nM) over MiaPaCa-2 and SW620 cells expressing mutant K-RasG12C or K-RasG12V (IC50s = 456 and 4,400 nM, respectively) and MCF-7 cells expressing wild-type K-Ras in which ERK phosphorylation was not reduced.

MRTX-1133

An inhibitor of K-RasG12D

Item No. BG20948
CAS No. 2621928-55-8
Purity: 98%

1mg

＄73.00

5mg

＄272.00

50mg

＄329.00

100mg

＄427.00

250mg

＄853.00

＄2,529.00

Quantity

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MRTX-1133 Synthetic Route

BG18306

CAS: 2454397-74-9

A146951

CAS: 3019-71-4

Bl55571

CAS: 2454490-36-7

BG18309

CAS: 2454397-75-0

BA32496

CAS: 2454396-80-4

CAS: 149771-44-8

BG18345

CAS: 2454397-98-7

BA23190

CAS: 2097518-76-6

BG38014

CAS: 2621932-38-3

CAS: 2621932-37-2

CAS: 2621935-50-8

CAS: 2894138-41-9

BG20948

CAS: 2621928-55-8

1: tetrahydrofuran / 0.17 h / 25 °C
2: ammonia / methanol / 1 h / 25 °C
3: N-ethyl-N,N-diisopropylamine; trichlorophosphate / toluene / 3 h / 0 - 110 °C
4: N-ethyl-N,N-diisopropylamine / N,N-dimethyl acetamide / 1 h / 0 - 20 °C
5: N-ethyl-N,N-diisopropylamine / 1,4-dioxane / 24 h / 90 °C / Molecular sieve
6: caesium carbonate; (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride / 1,4-dioxane; water / 2.5 h / 100 °C / Inert atmosphere
7: hydrogenchloride / 1,4-dioxane; acetonitrile / 0.5 h / 0 °C / Inert atmosphere
8: cesium fluoride / N,N-dimethyl-formamide / 1 h / 20 °C / Inert atmosphere

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References

1.Current Patent Assignee: ARRAY BIOPHARMA - WO2021/41671, 2021, A1.
2.wiatnicki, M., Engel, L., Shrestha, R., et al. Profiling oncogenic KRAS mutant drugs with a cell-based Lumit p-ERK immunoassay. SLAS Discov. S2472-5552(22), (2022).