MRTX1133

SKU: orb1298201

描述

MRTX1133 is a potent, selective, and non-covalent small-molecule inhibitor targeting the KRAS G12D mutant with sub-picomolar affinity (K_D = 0.2 pM). It demonstrates antitumor efficacy in G12D-mutated cell lines and in vivo models, showing selectivity over wild-type KRAS, making it a valuable research tool for oncology and targeted therapy studies.

研究领域

Pharmacology & Drug Discovery, Signal Transduction

图片与验证

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关键属性

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CAS 号	2621928-55-8
MW	600.63
纯度	99.92% (May vary between batches)
分子式	C₃₃H₃₁F₃N₆O₂
SMILES	C(OC=1N=C(C2=C(N1)C(F)=C(N=C2)C=3C4=C(C=C(O)C3)C=CC(F)=C4C#C)N5CC6NC(C5)CC6)[C@@]78N(C[C@H](F)C7)CCC8
靶点	Kras,Ras
溶解性	DMSO: 50 mg/mL (83.25 mM), Sonication is recommended

生物活性

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靶点 IC50	KRas (G12D):0.2 pM (Kd)\|KRas (G12D):< 2 nM
体内	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. 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.
体外	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. 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. 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.

储存与操作

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储存	-20°C
有效期	12 months from date of receipt.
免责声明	For research use only

别名

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active, cells, Inhibitor, ERK, G12D, mutant, MRTX1133, MRTX-1133, MRTX 1133, inactive, KRAS G12D, KRAS, inhibit, tumor, states, Ras, phosphorylation, wild-type

相似产品

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G13Ci-22 [orb3174547]
可选规格： 10 mg, 50 mg
NOX2-IN-3 [orb2565654]
CAS 号：
921145-98-4
MW:
372.4165
分子式：
C₂₃H₂₀N₂O₃
可选规格： 50 mg, 10 mg
MRTX1133 formic [orb1693136]
MW:
646.67
分子式：
C₃₄H₃₃F₃N₆O₄
可选规格： 5 mg, 10 mg

质量保证

Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our 条款与条件和选购指南.

化合物标识

PubChem CID

162369732 ↗

关键属性

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暂无计算属性。

实验方案信息

查看更多实验方案

按应用筛选

In vivo (1)

按种属筛选

Mouse (1)

Elodie Roger et al. ATM Deficiency Induces TGF-β-Mediated Stromal Programming in Pancreatic Cancer Cancer Res, (2026)

PubMed: 42113576

应用

In vivo

反应性

Mouse

CAS 号：	921145-98-4
MW:	372.4165
分子式：	C₂₃H₂₀N₂O₃

MW:	646.67
分子式：	C₃₄H₃₃F₃N₆O₄

MRTX1133

描述

研究领域

图片与验证

关键属性

生物活性

储存与操作

别名

相似产品

G13Ci-22 [orb3174547]

NOX2-IN-3 [orb2565654]

MRTX1133 formic [orb1693136]

质量保证

化合物标识

关键属性

实验方案信息

可选规格