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MRTX849
CAS No. 2326521-71-3
MRTX849( —— )
Catalog No. M21642 CAS No. 2326521-71-3
MRTX849 is a potent selective and covalent KRASG12C inhibitor with potential antineoplastic activity.selectively modifies mutant cysteine 12 in GDP-bound KRASG12C and inhibits KRAS-dependent signaling.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 1 mL x 10 mM in DMSO | 75 | In Stock |
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| 5MG | 56 | In Stock |
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| 10MG | 88 | In Stock |
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| 25MG | 188 | In Stock |
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| 50MG | 343 | In Stock |
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| 100MG | 514 | In Stock |
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| 200MG | Get Quote | In Stock |
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| 500MG | 926 | In Stock |
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| 1G | Get Quote | In Stock |
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Biological Information
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Product NameMRTX849
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NoteResearch use only, not for human use.
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Brief DescriptionMRTX849 is a potent selective and covalent KRASG12C inhibitor with potential antineoplastic activity.selectively modifies mutant cysteine 12 in GDP-bound KRASG12C and inhibits KRAS-dependent signaling.
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DescriptionMRTX849 is a potent selective and covalent KRASG12C inhibitor with potential antineoplastic activity.selectively modifies mutant cysteine 12 in GDP-bound KRASG12C and inhibits KRAS-dependent signaling.
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In VitroCell Viability Assay Cell Line:MIA PaCa-2, H1373, H358, H2122, SW1573, H2030, KYSE-410 cells (G12C); H1299 (WT); A549 (G12S), HCT116 (G13D) cellsConcentration:0.1, 1, 10, 100, 1000, 10000 nM Incubation Time:24 hours Result:Inhibits cell growth in the vast majority of KRAS G12C-mutant cell lines with IC50 values ranging between 10 and 973 nM in the 2D format and between 0.2 and 1042 nM in the 3D format.Western Blot AnalysisCell Line:MIA PaCa-2 cells Concentration:0.24, 0.5, 1.0, 2.0, 3.9, 7.8, 15.6, 31.3, 62.5, 125, 250, 500, 1000 nM Incubation Time:24 hours Result:Inhibits KRAS-dependent signaling targets including ERK1/2 phosphorylation (Thr202/Tyr204 ERK1; pERK), S6 phosphorylation (RSK-dependent Ser235/236; pS6) and expression of the ERK-regulated DUSP6, each with IC50s in the single-digit nanomolar range in cell lines.
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In VivoAnimal Model:MIA PaCa-2 model (6-8-week-old, female, athymic nude-Foxn1 nu mice)Dosage:1, 3, 10, 30 and 100 mg/kg Administration:Oral gavage; daily until Day 16Result:Rapid tumor regression was observed at the earliest posttreatment tumor measurement and animals in the 30 and 100 mg/kg cohorts exhibited evidence of a complete response at study Day 15. Dosing was stopped at study Day 16 and all 4 mice in the 100 mg/kg cohort and 2 out of 7 mice in the 30 mg/kg cohort remained tumor-free through study Day 70.
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Synonyms——
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PathwayMAPK/ERK Signaling
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TargetRas
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RecptorKRAS G12C
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Research Areacancer
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Indication——
Chemical Information
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CAS Number2326521-71-3
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Formula Weight604.12
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Molecular FormulaC32H35ClFN7O2
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Purity>98% (HPLC)
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SolubilityDMSO:100 mg/mL (165.53 mM; Need ultrasonic)
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SMILESCN1CCC[C@H]1COc1nc2CN(CCc2c(n1)N1CCN([C@@H](CC#N)C1)C(=O)C(F)=C)c1cccc2cccc(Cl)c12
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Chemical Name——
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1.Jill Hallin Lars D Engstrom Lauren Hargis.The KRAS G12C Inhibitor MRTX849 Provides Insight Toward Therapeutic Susceptibility of KRAS-Mutant Cancers in Mouse Models and Patients.Cancer Discov. 2020 Jan;10(1):54-71.
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