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MRTX1133

Catalog No. T9303 CAS 2621928-55-8

MRTX1133 is a KRAS G12D inhibitor (KD=0.2 pM) that is potent, selective, and non-covalent. MRTX1133 exhibits inhibitory activity against KRAS G12D-mutated tumors, but not against KRAS wild-type tumors.

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MRTX1133, CAS 2621928-55-8

Pack Size	Availability	Price/USD
1 mg	In stock	$ 197.00
5 mg	In stock	$ 424.00
10 mg	In stock	$ 649.00
25 mg	In stock	$ 997.00
50 mg	In stock	$ 1,420.00
100 mg	In stock	$ 1,920.00
1 mL * 10 mM (in DMSO)	In stock	$ 557.00

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Purity: 99.10%

Purity: 99.06%

Purity: 98.82%

Purity: 98.63%

Purity: 98.41%

Purity: 98.28%

Purity: 98.18%

ee: 100%

Purity: 98.08%

Purity: 97.39%

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Description	MRTX1133 is a KRAS G12D inhibitor (KD=0.2 pM) that is potent, selective, and non-covalent. MRTX1133 exhibits inhibitory activity against KRAS G12D-mutated tumors, but not against KRAS wild-type tumors.
Targets&IC50	KRas (G12D):0.2 pM (Kd)
In vitro	METHODS: Human gastric cancer cells AGS (KRASG12D) and MKN1 (KRASWT) were treated with MRTX1133 (0-3 μM) for 72 h, and cell viability was measured by CTG method in 2D culture. RESULTS: The IC50 of MRTX1133 on AGS and MKN1 cells was 6 nM and >3000 nM, respectively. [1] METHODS: Human gastric cancer cells AGS (KRASG12D) were treated with MRTX1133 (0-10 μM) for 3-72 h, and the expression levels of target proteins were detected by In-Cell Western method. RESULTS: MRTX1133 inhibited the p-ERK level of AGS with an IC50 of 2 nM. [1] METHODS: Human pancreatic cancer cells SUIT2 (KRASG12D) were treated with MRTX1133 (60 nmol/L) for 24 h, and the expression levels of target proteins were detected by Western Blot. RESULTS: SUIT2 cells treated with MRTX1133 showed a significant decrease in pMEK1/2, a partial decrease in pERK1/2, and an initial decrease in pAKT followed by a recovery at a later time point. The levels of pEGFR and pHER2 decreased and recovered at 72 h. [2]
In vivo	METHODS: To test the antitumor activity in vivo, MRTX1133 (3-30 mg/kg, 10% Captisol in 50 mM citrate buffer pH 5.0) was intraperitoneally injected into nude-Foxn1nu mice bearing human pancreatic adenocarcinoma tumor Panc 04.03 twice daily for seven weeks. RESULTS: MRTX1133 exhibited dose-dependent antitumor activity, with 94% tumor growth inhibition observed at the 3 mg/kg group. Tumor regression of -62% and -73% was observed in the 10 mg/kg and 30 mg/kg groups, respectively. [1] METHODS: To assay antitumor activity in vivo, MRTX1133 (0.5 mg/kg in 12.5% Cremophor+12.5% ethanol+75%, orally once daily) and Cetuximab (50 mg/kg, intraperitoneally once weekly) were administered to BALB/c nude mice harboring human colorectal tumors, LS531 or CACO-2 for twenty-one days. RESULTS: MRTX1133 significantly inhibited tumorigenesis in both in vivo models. The anti-tumor effect was further enhanced when MRTX1133 was combined with Cetuximab. [3]

Molecular Weight	600.63
Formula	C33H31F3N6O2
CAS No.	2621928-55-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 230 mg/mL (382.93 mM), Sonication is recommended.

References and Literature

1. Wang X, et al. Identification of MRTX1133, a Noncovalent, Potent, and Selective KRASG12D Inhibitor. J Med Chem. 2022 Feb 24;65(4):3123-3133. 2. Gulay KCM, et al. Dual Inhibition of KRASG12D and Pan-ERBB Is Synergistic in Pancreatic Ductal Adenocarcinoma. Cancer Res. 2023 Sep 15;83(18):3001-3012. 3. Kataoka M, et al. Cetuximab Enhances the Efficacy of MRTX1133, a Novel KRASG12D Inhibitor, in Colorectal Cancer Treatment. Anticancer Res. 2023 Oct;43(10):4341-4348.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Cancer Active Compound Library Membrane Protein-targeted Compound Library GPCR Compound Library Kinase Inhibitor Library HIF-1 Signaling Pathway Compound Library Preclinical Compound Library Anti-Obesity Compound Library Anti-Ovarian Cancer Compound Library NO PAINS Compound Library

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Keywords

MRTX1133 2621928-55-8 GPCR/G Protein MAPK Ras KRAS G12D MRTX 1133 cells active wild-type phosphorylation mutant inactive ERK inhibit tumor states MRTX-1133 Inhibitor inhibitor

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