Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
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 |
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 230 mg/mL (382.93 mM), Sonication is recommended.
You can also refer to dose conversion for different animals. More
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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