製品番号: HY-114277

Sotorasib

(別名: AMG-510)

121 Cited Publications

カスタマーレビュー

Based on 121 publication(s) in Google Scholar

Sotorasib (AMG-510) is a first-in-class, orally bioavailable, and selective KRAS G12C covalent inhibitor. Sotorasib irreversibly inhibits KRAS G12C by locking it in an inactive GDP-bound state. Sotorasib leads to the regression of KRAS G12C‑mutated locally advanced or metastatic non‑small cell lung cancer (NSCLC).

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

純度: 99.70%
CAS 番号: 2296729-00-3
分子式: C₃₀H₃₀F₂N₆O₃
分子量:560.59

保管条件:

-20°C, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Sotorasib 構造式

CAS 番号: 2296729-00-3

容量

価格（税別）

在庫状況

数量

Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
- 体内実験
- 臨床実験
化学情報
Publications (121)
溶剤 & 溶解度
- 体外
- 体内
純度とドキュメンテーション
参考文献
Help & FAQs
関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target^[1]

KRAS(G12C)

Ras アイソフォーム固有の製品をすべて表示 :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	36.5 μM Compound: (R)-38; AMG-510	Antiproliferative activity against human A549 cells harboring KRAS G12S point mutant assessed as cell growth inhibition after 72 hrs by Celltiter-Glo luminescent cell viability assay Antiproliferative activity against human A549 cells harboring KRAS G12S point mutant assessed as cell growth inhibition after 72 hrs by Celltiter-Glo luminescent cell viability assay	[PMID: 31820981]
A549	IC₅₀	>10 μM Compound: 2; AMG510	Antiproliferative activity against human A549 cells harboring KRAS G12S mutant assessed as growth inhibition measured after 72 hrs by SRB assay Antiproliferative activity against human A549 cells harboring KRAS G12S mutant assessed as growth inhibition measured after 72 hrs by SRB assay	[PMID: 33309163]
A549	IC₅₀	50 μM Compound: 2; AMG510	Antiproliferative activity against human A549 cells harboring KRAS G12S mutant measured after 72 hrs by CCK-8 assay Antiproliferative activity against human A549 cells harboring KRAS G12S mutant measured after 72 hrs by CCK-8 assay	[PMID: 35007863]
ASPC1	IC₅₀	>10 μM Compound: AMG510	Antiproliferative activity against human ASPC1 cells expressing KRAS G12D mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human ASPC1 cells expressing KRAS G12D mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 37852032]
HEK-293T	IC₅₀	>10 μM Compound: AMG510	Cytotoxicity against HEK293T cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Cytotoxicity against HEK293T cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 37852032]
HepG2	IC₅₀	>10 μM Compound: AMG510	Antiproliferative activity against human HepG2 cells expressing KRAS assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human HepG2 cells expressing KRAS assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 37852032]
MIA PaCa-2	IC₅₀	0.005 μM Compound: (R)-38; AMG-510	Antiproliferative activity against human MIAPaCa2 cells harboring KRAS G12C point mutant assessed as cell growth inhibition after 72 hrs by Celltiter-Glo luminescent cell viability assay Antiproliferative activity against human MIAPaCa2 cells harboring KRAS G12C point mutant assessed as cell growth inhibition after 72 hrs by Celltiter-Glo luminescent cell viability assay	[PMID: 31820981]
MIA PaCa-2	IC₅₀	0.029 μM Compound: 2; AMG510	Antiproliferative activity against human MIA PaCa-2 cells harboring KRAS G12C mutant assessed as growth inhibition measured after 72 hrs by CCK8 assay Antiproliferative activity against human MIA PaCa-2 cells harboring KRAS G12C mutant assessed as growth inhibition measured after 72 hrs by CCK8 assay	[PMID: 33309163]
MIA PaCa-2	IC₅₀	0.022 μM Compound: AMG-510	Antiproliferative activity against human MIA PaCa-2 cells harboring KRAS G12C mutant assessed as inhibition of cell growth Antiproliferative activity against human MIA PaCa-2 cells harboring KRAS G12C mutant assessed as inhibition of cell growth	[PMID: 36621179]
MIA PaCa-2	IC₅₀	0.018 μM Compound: AMG510	Antiproliferative activity against human MIA PaCa-2 cells expressing KRAS G12C mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human MIA PaCa-2 cells expressing KRAS G12C mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 37852032]
MIA PaCa-2	IC₅₀	>40 μM Compound: AMG510	Cytotoxicity against human MIA PaCa-2 cells harboring KRAS G12C mutant assessed as cell growth inhibition incubated for 24 hrs by MTT assay Cytotoxicity against human MIA PaCa-2 cells harboring KRAS G12C mutant assessed as cell growth inhibition incubated for 24 hrs by MTT assay	[PMID: 38272464]
MIA PaCa-2	IC₅₀	13 nM Compound: AMG-510	Antiproliferative activity against human MIA PaCa-2 cells incubated for 6 days in presence of 1 uM (2S,4R)-1-((S)-2-(5-((4-(((R)-1-(3-amino-5-(trifluoromethyl)phenyl)ethyl)amino)-7-methoxy-2-methylquinazolin-6-yl)oxy)pentanamido)-3,3-dimethylbutanoyl)-4-h Antiproliferative activity against human MIA PaCa-2 cells incubated for 6 days in presence of 1 uM (2S,4R)-1-((S)-2-(5-((4-(((R)-1-(3-amino-5-(trifluoromethyl)phenyl)ethyl)amino)-7-methoxy-2-methylquinazolin-6-yl)oxy)pentanamido)-3,3-dimethylbutanoyl)-4-h	[PMID: 38316747]
MIA PaCa-2	IC₅₀	37 nM Compound: AMG-510	Antiproliferative activity against human MIA PaCa-2 cells incubated for 6 days by CCK8 assay Antiproliferative activity against human MIA PaCa-2 cells incubated for 6 days by CCK8 assay	[PMID: 38316747]
MIA PaCa-2	IC₅₀	6 nM Compound: AMG-510	Antiproliferative activity against human MIA PaCa-2 cells incubated for 6 days in presence of 10 uM (2S,4R)-1-((S)-2-(5-((4-(((R)-1-(3-amino-5-(trifluoromethyl)phenyl)ethyl)amino)-7-methoxy-2-methylquinazolin-6-yl)oxy)pentanamido)-3,3-dimethylbutanoyl)-4- Antiproliferative activity against human MIA PaCa-2 cells incubated for 6 days in presence of 10 uM (2S,4R)-1-((S)-2-(5-((4-(((R)-1-(3-amino-5-(trifluoromethyl)phenyl)ethyl)amino)-7-methoxy-2-methylquinazolin-6-yl)oxy)pentanamido)-3,3-dimethylbutanoyl)-4-	[PMID: 38316747]
MIA PaCa-2	IC₅₀	>10 nM Compound: AMG510	Cytotoxicity against human MIA PaCa-2 cells incubated for 48 hrs by CCK-8 assay Cytotoxicity against human MIA PaCa-2 cells incubated for 48 hrs by CCK-8 assay	[PMID: 38593589]
NCI-H1373	IC₅₀	355.7 nM Compound: AMG-510	Cytotoxicity against human NCI-H1373 cells harboring KRASG12C mutant assessed as reduction in cell viability measured after 72 hrs in presence of compound 1 by CellTiter-Glo luciferase-based ATP detection assay Cytotoxicity against human NCI-H1373 cells harboring KRASG12C mutant assessed as reduction in cell viability measured after 72 hrs in presence of compound 1 by CellTiter-Glo luciferase-based ATP detection assay	[PMID: 34676026]
NCI-H1373	IC₅₀	>10000 nM Compound: AMG-510	Cytotoxicity against human NCI-H1373 cells harboring KRAS G12C mutant assessed as reduction in cell viability measured after 72 hrs by CellTiter-Glo luciferase-based ATP detection assay Cytotoxicity against human NCI-H1373 cells harboring KRAS G12C mutant assessed as reduction in cell viability measured after 72 hrs by CellTiter-Glo luciferase-based ATP detection assay	[PMID: 34676026]
NCI-H1792	IC₅₀	>10000 nM Compound: AMG-510	Cytotoxicity against human NCI-H1792 cells harboring KRAS G12C mutant assessed as reduction in cell viability measured after 72 hrs by CellTiter-Glo luciferase-based ATP detection assay Cytotoxicity against human NCI-H1792 cells harboring KRAS G12C mutant assessed as reduction in cell viability measured after 72 hrs by CellTiter-Glo luciferase-based ATP detection assay	[PMID: 34676026]
NCI-H1792	IC₅₀	3 μM Compound: AMG-510	Cytotoxicity against human NCI-H1792 cells harboring KRASG12C mutant assessed as reduction in cell viability measured after 72 hrs in presence of compound 1 by CellTiter-Glo luciferase-based ATP detection assay Cytotoxicity against human NCI-H1792 cells harboring KRASG12C mutant assessed as reduction in cell viability measured after 72 hrs in presence of compound 1 by CellTiter-Glo luciferase-based ATP detection assay	[PMID: 34676026]
NCI-H1975	IC₅₀	>10 μM Compound: 2; AMG510	Antiproliferative activity against human NCI-H1975 cells harboring wild-type KRAS assessed as growth inhibition measured after 72 hrs by SRB assay Antiproliferative activity against human NCI-H1975 cells harboring wild-type KRAS assessed as growth inhibition measured after 72 hrs by SRB assay	[PMID: 33309163]
NCI-H2122	IC₅₀	530.3 nM Compound: AMG-510	Cytotoxicity against human NCI-H2122 cells harboring KRAS G12C mutant assessed as reduction in cell viability measured after 72 hrs by CellTiter-Glo luciferase-based ATP detection assay Cytotoxicity against human NCI-H2122 cells harboring KRAS G12C mutant assessed as reduction in cell viability measured after 72 hrs by CellTiter-Glo luciferase-based ATP detection assay	[PMID: 34676026]
NCI-H2122	IC₅₀	90.5 nM Compound: AMG-510	Cytotoxicity against human NCI-H2122 cells harboring KRASG12C mutant assessed as reduction in cell viability measured after 72 hrs in presence of compound 1 by CellTiter-Glo luciferase-based ATP detection assay Cytotoxicity against human NCI-H2122 cells harboring KRASG12C mutant assessed as reduction in cell viability measured after 72 hrs in presence of compound 1 by CellTiter-Glo luciferase-based ATP detection assay	[PMID: 34676026]
NCI-H23	IC₅₀	1500 nM Compound: AMG-510	Cytotoxicity against human NCI-H23 cells harboring KRASG12C mutant assessed as reduction in cell viability measured after 72 hrs in presence of compound 1 by CellTiter-Glo luciferase-based ATP detection assay Cytotoxicity against human NCI-H23 cells harboring KRASG12C mutant assessed as reduction in cell viability measured after 72 hrs in presence of compound 1 by CellTiter-Glo luciferase-based ATP detection assay	[PMID: 34676026]
NCI-H23	IC₅₀	>10000 nM Compound: AMG-510	Cytotoxicity against human NCI-H23 cells harboring KRAS G12C mutant assessed as reduction in cell viability measured after 72 hrs by CellTiter-Glo luciferase-based ATP detection assay Cytotoxicity against human NCI-H23 cells harboring KRAS G12C mutant assessed as reduction in cell viability measured after 72 hrs by CellTiter-Glo luciferase-based ATP detection assay	[PMID: 34676026]
NCI-H23	IC₅₀	111.5 nM Compound: 2; AMG510	Antiproliferative activity against human NCI-H23 cells harboring KRAS G12C mutant measured after 72 hrs by CCK-8 assay Antiproliferative activity against human NCI-H23 cells harboring KRAS G12C mutant measured after 72 hrs by CCK-8 assay	[PMID: 35007863]
NCI-H358	IC₅₀	<0.03 μM Compound: 16, AMG510	Antiproliferative activity against human NCI-H358 cells Antiproliferative activity against human NCI-H358 cells	[PMID: 32910655]
NCI-H358	IC₅₀	<0.016 μM Compound: 2; AMG510	Antiproliferative activity against human NCI-H358 cells harboring KRAS G12C mutant assessed as growth inhibition measured after 72 hrs by SRB assay Antiproliferative activity against human NCI-H358 cells harboring KRAS G12C mutant assessed as growth inhibition measured after 72 hrs by SRB assay	[PMID: 33309163]
NCI-H358	IC₅₀	213 nM Compound: AMG-510	Cytotoxicity against human NCI-H358 cells harboring KRAS G12C mutant assessed as reduction in cell viability measured after 72 hrs by CellTiter-Glo luciferase-based ATP detection assay Cytotoxicity against human NCI-H358 cells harboring KRAS G12C mutant assessed as reduction in cell viability measured after 72 hrs by CellTiter-Glo luciferase-based ATP detection assay	[PMID: 34676026]
NCI-H358	IC₅₀	3 nM Compound: AMG-510	Cytotoxicity against human NCI-H358 cells harboring KRASG12C mutant assessed as reduction in cell viability measured after 72 hrs in presence of compound 1 by CellTiter-Glo luciferase-based ATP detection assay Cytotoxicity against human NCI-H358 cells harboring KRASG12C mutant assessed as reduction in cell viability measured after 72 hrs in presence of compound 1 by CellTiter-Glo luciferase-based ATP detection assay	[PMID: 34676026]
NCI-H358	IC₅₀	8.4 nM Compound: 2; AMG510	Antiproliferative activity against human NCI-H358 cells harboring KRAS G12C mutant measured after 72 hrs by CCK-8 assay Antiproliferative activity against human NCI-H358 cells harboring KRAS G12C mutant measured after 72 hrs by CCK-8 assay	[PMID: 35007863]
NCI-H358	EC₅₀	6 nM Compound: AMG-510	Antiproliferative activity against human NCI-H358 Antiproliferative activity against human NCI-H358	[PMID: 36300829]
NCI-H358	EC₅₀	6.4 nM Compound: AMG-510	Antiproliferative activity against human NCI-H358 cells harboring KRAS G12C mutant incubated for 3 days by celltiter glo luminescent assay Antiproliferative activity against human NCI-H358 cells harboring KRAS G12C mutant incubated for 3 days by celltiter glo luminescent assay	[PMID: 36300829]
NCI-H358	IC₅₀	0.001 μM Compound: 1	Antiproliferative activity against human NCI-H358 cells harboring KRAS G12C mutant cultured as 3D spheroids assessed as reduction in cell proliferation incubated for 3 days by CellTiter-Glo 3D reagent based assay Antiproliferative activity against human NCI-H358 cells harboring KRAS G12C mutant cultured as 3D spheroids assessed as reduction in cell proliferation incubated for 3 days by CellTiter-Glo 3D reagent based assay	[PMID: 37395055]
NCI-H358	IC₅₀	0.012 μM Compound: AMG510	Antiproliferative activity against human NCI-H358 cells expressing KRAS G12C mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human NCI-H358 cells expressing KRAS G12C mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 37852032]
NCI-H358	IC₅₀	1 nM Compound: AMG-510	Antiproliferative activity against human NCI-H358 cells incubated for 6 days in presence of 10 uM (2S,4R)-1-((S)-2-(5-((4-(((R)-1-(3-amino-5-(trifluoromethyl)phenyl)ethyl)amino)-7-methoxy-2-methylquinazolin-6-yl)oxy)pentanamido)-3,3-dimethylbutanoyl)-4-hy Antiproliferative activity against human NCI-H358 cells incubated for 6 days in presence of 10 uM (2S,4R)-1-((S)-2-(5-((4-(((R)-1-(3-amino-5-(trifluoromethyl)phenyl)ethyl)amino)-7-methoxy-2-methylquinazolin-6-yl)oxy)pentanamido)-3,3-dimethylbutanoyl)-4-hy	[PMID: 38316747]
NCI-H358	IC₅₀	10 nM Compound: AMG-510	Antiproliferative activity against human NCI-H358 cells incubated for 6 days by CCK8 assay Antiproliferative activity against human NCI-H358 cells incubated for 6 days by CCK8 assay	[PMID: 38316747]
NCI-H358	IC₅₀	4 nM Compound: AMG-510	Antiproliferative activity against human NCI-H358 cells incubated for 6 days in presence of 1 uM (2S,4R)-1-((S)-2-(5-((4-(((R)-1-(3-amino-5-(trifluoromethyl)phenyl)ethyl)amino)-7-methoxy-2-methylquinazolin-6-yl)oxy)pentanamido)-3,3-dimethylbutanoyl)-4-hyd Antiproliferative activity against human NCI-H358 cells incubated for 6 days in presence of 1 uM (2S,4R)-1-((S)-2-(5-((4-(((R)-1-(3-amino-5-(trifluoromethyl)phenyl)ethyl)amino)-7-methoxy-2-methylquinazolin-6-yl)oxy)pentanamido)-3,3-dimethylbutanoyl)-4-hyd	[PMID: 38316747]
NCM460	IC₅₀	>40 μM Compound: AMG510	Cytotoxicity against human NCM460 cells harboring wild-type KRAS assessed as cell growth inhibition incubated for 24 hrs by MTT assay Cytotoxicity against human NCM460 cells harboring wild-type KRAS assessed as cell growth inhibition incubated for 24 hrs by MTT assay	[PMID: 38272464]
PANC-1	IC₅₀	>40 μM Compound: AMG510	Cytotoxicity against human PANC-1 cells harboring KRAS G12D mutant assessed as cell growth inhibition incubated for 24 hrs by MTT assay Cytotoxicity against human PANC-1 cells harboring KRAS G12D mutant assessed as cell growth inhibition incubated for 24 hrs by MTT assay	[PMID: 38272464]
PANC-1	IC₅₀	>40 μM Compound: AMG510	Cytotoxicity against human PANC-1 cells harboring wild-type KRAS assessed as cell growth inhibition incubated for 24 hrs by MTT assay Cytotoxicity against human PANC-1 cells harboring wild-type KRAS assessed as cell growth inhibition incubated for 24 hrs by MTT assay	[PMID: 38272464]
SW837	IC₅₀	2 nM Compound: AMG-510	Antiproliferative activity against human SW837 cells incubated for 6 days in presence of 10 uM (2S,4R)-1-((S)-2-(5-((4-(((R)-1-(3-amino-5-(trifluoromethyl)phenyl)ethyl)amino)-7-methoxy-2-methylquinazolin-6-yl)oxy)pentanamido)-3,3-dimethylbutanoyl)-4-hydro Antiproliferative activity against human SW837 cells incubated for 6 days in presence of 10 uM (2S,4R)-1-((S)-2-(5-((4-(((R)-1-(3-amino-5-(trifluoromethyl)phenyl)ethyl)amino)-7-methoxy-2-methylquinazolin-6-yl)oxy)pentanamido)-3,3-dimethylbutanoyl)-4-hydro	[PMID: 38316747]
SW837	IC₅₀	3 nM Compound: AMG-510	Antiproliferative activity against human SW837 cells incubated for 6 days in presence of 1 uM (2S,4R)-1-((S)-2-(5-((4-(((R)-1-(3-amino-5-(trifluoromethyl)phenyl)ethyl)amino)-7-methoxy-2-methylquinazolin-6-yl)oxy)pentanamido)-3,3-dimethylbutanoyl)-4-hydrox Antiproliferative activity against human SW837 cells incubated for 6 days in presence of 1 uM (2S,4R)-1-((S)-2-(5-((4-(((R)-1-(3-amino-5-(trifluoromethyl)phenyl)ethyl)amino)-7-methoxy-2-methylquinazolin-6-yl)oxy)pentanamido)-3,3-dimethylbutanoyl)-4-hydrox	[PMID: 38316747]
SW837	IC₅₀	9 nM Compound: AMG-510	Antiproliferative activity against human SW837 cells incubated for 6 days by CCK8 assay Antiproliferative activity against human SW837 cells incubated for 6 days by CCK8 assay	[PMID: 38316747]

体外実験

In cellular assays, Sotorasib (AMG-510) covalently modifies KRAS G12C and inhibits KRAS G12C signaling as measured by phosphorylation of ERK1/2 (p-ERK) in all KRAS p.G12C-mutant cell lines^[2].
Sotorasib (AMG-510; 1-10 μM; 72 hours) also potently impairs cellular viability in both NCI-H358 and MIA PaCa-2 with IC₅₀≈0.006 μM and 0.009 μM, respectively. Non-KRASG12C lines are insensitive to Sotorasib (IC₅₀>7.5 μM)^[3].
Sotorasib (AMG-510) (0-50 μM, 72 h) inhibits cell growth and has a synergistic effect with Cisplatin (HY-17394) in H23 and H358 cells^[5].
Sotorasib (AMG-510) (100 nM, 4-72 h) has sustained suppression against active KRAS, but still observes adaptive feedback reactivation of RAS-MAPK^[6].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[3]

Cell Line:

NCI-H358 and MIA PaCa-2 cells
Concentration:

1-10 μM
Incubation Time:

72 hours
Result:

Potently impaired cellular viability in both NCI-H358 and MIA PaCa-2 (IC₅₀=~0.006 μM and ~0.009 μM respectively).

Cell Viability Assay^[5]

Cell Line:

NCI-H23 (H23) and NCI-H358 (H358) cells (Lung adenocarcinoma cell lines harbor KRAS G12C mutations)
Concentration:

0-50 μM
Incubation Time:

72 h
Result:

The IC₅₀ values in H358 and H23 cell lines were 0.0818 μM, 0.6904 μM, respectively.
Had a synergistic effect with Cisplatin (HY-17394).

Western Blot Analysis^[6]

Cell Line:

H358, MGH1088-1, MGH1062, MIA PaCa-2, B8182, LIM2099, SW837, SW1463 (KRAS-^G12C mutant cell lines)
Concentration:

100 nM
Incubation Time:

4, 24, 48, 72 h
Result:

Showed effective inhibition of the MAPK pathway at 4 h, comparable rapid and robust reactivation of RAS-MAPK signaling was observed, such that phospho-ERK levels returned to an average of ~75% of baseline levels by just 72 h.
Adaptive feedback is likely to be a key driver of resistance.

体内実験

In preclinical tumor models, Sotorasib (AMG-510) rapidly and irreversibly binds to KRAS G12C, providing durable suppression of the mitogen-activated protein kinase (MAPK) signaling pathway. Sotorasib (orally; once daily) is capable of inducing tumor regression in mouse models of KRAS G12C cancer^[3].
Sotorasib (AMG-510) (30 mg/kg; p.o.; daily for 28 days) reduces tumor size in NCI-H358 cell-derived xenografts mice model, and has a synergistic effect with Cisplatin^[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Balb/C nude mice (injected with H358 cells under the skin)^[5]
Dosage:

30 mg/kg
Administration:

Oral gavage (p.o.); daily for 28 days
Result:

The mean tumor volume were 426.66mm³.
Reduced tumor size, and had a synergistic effect with Cisplatin.
Had little effects on body weight.

臨床実験

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

化学情報

CAS 番号 2296729-00-3
性状 Solid
分子量 560.59
分子式 C₃₀H₃₀F₂N₆O₃
SMILES

O=C(C=C)N1C[C@H](C)N(C2=NC(N(C3=C(C)C=CN=C3C(C)C)C4=C2C=C(F)C(C5=C(O)C=CC=C5F)=N4)=O)CC1
別名

AMG-510
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

-20°C, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Publications (121)

All Cell Proliferation/Viability AssayWB

Sort by:

Journal Impact Factor

Ann Oncol

Genomic landscape of clinically acquired resistance alterations in patients treated with KRASG12C inhibitors. [Abstract]

2025 Jun;36(6):682-692. PMID: 39914665
Nature

RNA-triggered cell killing with CRISPR-Cas12a2. [Abstract]

2026 Jul;655(8121):230-239. PMID: 42092133
Cancer Cell

A pan-KRAS inhibitor and its derived degrader elicit multifaceted anti-tumor efficacy in KRAS-driven cancers. [Abstract]

2025 Jul 25:S1535-6108(25)00310-1. PMID: 40780213
Science

Structural basis for the recruitment and selective phosphorylation of Akt by mTORC2. [Abstract]

2026 Mar 5;391(6789):eadv7111. PMID: 41308123
Science

Defining the KRAS- and ERK-dependent transcriptome in KRAS-mutant cancers. [Abstract]

2024 Jun 7;384(6700):eadk0775. PMID: 38843331
Mol Cancer

The phospholipid transporter PITPNC1 links KRAS to MYC to prevent autophagy in lung and pancreatic cancer. [Abstract]

2023 May 20;22(1):86. PMID: 37210549

Sotorasib purchased from MedChemExpress. Usage Cited in: Mol Cancer. 2023 May 20;22(1):86. [Abstract]

Sotorasib (5-100 nM; 48 h) can inhibit the proliferation of H1792, H2030, H358, H23, and MiaPaca2 cells. The inhibitory effect is more significant when combined with Fedratinib (HY-10409) (0.25-1 μM).

Sotorasib purchased from MedChemExpress. Usage Cited in: Mol Cancer. 2023 May 20;22(1):86. [Abstract]

Sotorasib (20 nM; 48 h) in combination with Fedratinib (1 μM; 48 h) inhibits KRASG12C in H358 and MiaPaca2 cells, activates STAT3, and induces specific apoptosis, indicating cytotoxic effects.
Cancer Discov

Oncogenic KRAS-dependent stromal interleukin-33 directs the pancreatic microenvironment to promote tumor growth. [Abstract]

2024 Oct 4;14(10):1964-1989. PMID: 38958646
Cancer Discov

D3S-001, a KRAS G12C inhibitor with rapid target engagement kinetics, overcomes nucleotide cycling and demonstrates robust preclinical and clinical activities. [Abstract]

2024 May 8. PMID: 38717075
Cancer Discov

Sotorasib is a pan-RASG12C inhibitor capable of driving clinical response in NRASG12C cancers. [Abstract]

2024 May 1;14(5):727-736. PMID: 38236605
Cancer Discov

Coordinated Transcriptional and Catabolic Programs Support Iron-Dependent Adaptation to RAS-MAPK Pathway Inhibition in Pancreatic Cancer. [Abstract]

2022 Sep 2;12(9):2198-2219. PMID: 35771494
Nat Cancer

The MEK-RAF molecular glue IK-595 has potent antitumor activity across RAS/MAPK pathway-altered cancers. [Abstract]

2026 Jan;7(1):116-130. PMID: 41482524
Nat Genet

Multiparametric and accurate functional analysis of genetic sequence variants using CRISPR-Select. [Abstract]

2022 Dec;54(12):1983-1993. PMID: 36471068
J Thorac Oncol

KRAS Secondary Mutations That Confer Acquired Resistance to KRAS G12C Inhibitors, Sotorasib and Adagrasib, and Overcoming Strategies: Insights From In Vitro Experiments. [Abstract]

2021 Aug;16(8):1321-1332. PMID: 33971321
Nat Cell Biol

RASH3D19 mediates RAS activation through a positive feedback loop in KRAS-mutant cancer. [Abstract]

2025 Dec 1. PMID: 41326795
Nat Cell Biol

Quantifying single-cell ERK dynamics in colorectal cancer organoids reveals EGFR as an amplifier of oncogenic MAPK pathway signalling. [Abstract]

2021 Apr;23(4):377-390. PMID: 33795873
Cancer Res

Prolonged KRAS-MAPK Inhibition Induces Interferon Signaling That Promotes Cell State Transition and Confers Therapeutic Vulnerabilities. [Abstract]

2026 Jul 2;86(13):3270-3286. PMID: 42008116
Cancer Res

PRT3789 is a First-in-Human SMARCA2-Selective Degrader that Induces Synthetic Lethality in SMARCA4-Mutated Cancers. [Abstract]

2025 Sep 24. PMID: 40991405
Cancer Res

Targeted Degradation of SOS1 Exhibits Potent Anticancer Activity and Overcomes Resistance in KRAS-Mutant Tumors and BCR-ABL-Positive Leukemia. [Abstract]

2025 Jan 2;85(1):101-117. PMID: 39437162
Cancer Res

Lentiviral-Driven Discovery of Cancer Drug Resistance Mutations. [Abstract]

2021 Sep 15;81(18):4685-4695. PMID: 34301758
Nat Commun

All-trans retinoic acid destabilizes ADAR1 protein through retinoylation-mediated USP7 dissociation and improves immunotherapy in pancreatic cancer. [Abstract]

2026 May 11. PMID: 42115161
Nat Commun

Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]

2026 Feb 12;17(1):1214. PMID: 41680175
Nat Commun

B7-H3-mediated cis-inhibition of EGFR by a tumor-selective bispecific antibody enhances anti-tumor efficacy and minimizes toxicities. [Abstract]

2026 Feb 24;17(1):3113. PMID: 41735305
Nat Commun

High-fidelity Cas9-mediated targeting of KRAS driver mutations restrains lung cancer in preclinical models. [Abstract]

2025 Sep 1;16(1):7080. PMID: 40890128
Nat Commun

Non-canonical pathway for Rb inactivation and external signaling coordinate cell-cycle entry without CDK4/6 activity. [Abstract]

2023 Nov 29;14(1):7847. PMID: 38030655
Nat Commun

Signature-driven repurposing of Midostaurin for combination with MEK1/2 and KRASG12C inhibitors in lung cancer. [Abstract]

2023 Oct 10;14(1):6332. PMID: 37816716
Nat Commun

Oncogenic KRAS is dependent upon an EFR3A-PI4KA signaling axis for potent tumorigenic activity. [Abstract]

2021 Sep 9;12(1):5248. PMID: 34504076
Nat Commun

Gilteritinib overcomes lorlatinib resistance in ALK-rearranged cancer. [Abstract]

2021 Feb 24;12(1):1261. PMID: 33627640
J Adv Res

Targeting class I HDACs suppresses oncogenic vulnerabilities and potentiates KRAS/MAPK pathway inhibitors in KRAS-mutant cancers. [Abstract]

2026 Feb 13:S2090-1232(26)00144-X. PMID: 41692243
J Am Chem Soc

Fluorescent Biosensor for Measuring Ras Activity in Living Cells. [Abstract]

2022 Sep 28;144(38):17432-17440. PMID: 36122391
Redox Biol

Reactivation of MAPK-SOX2 pathway confers ferroptosis sensitivity in KRASG12C inhibitor resistant tumors. [Abstract]

2024 Nov 5:78:103419. PMID: 39527862
J Clin Invest

Cotargeting DNA topoisomerase II enhances efficacy of RAS-targeted therapy in KRAS-mutant cancer models. [Abstract]

2026 Feb 16;136(4):e197192. PMID: 41697749
J Exp Clin Cancer Res

Dual inhibition of HERs and PD-1 counteract resistance in KRASG12C-mutant head and neck cancer. [Abstract]

2024 Nov 20;43(1):308. PMID: 39567998
J Clin Invest

Oncogenic KRAS signaling drives evasion of innate immune surveillance in lung adenocarcinoma by activating CD47. [Abstract]

2023 Jan 17;133(2):e153470. PMID: 36413402
Adv Sci (Weinh)

Real-Time Visualization of Isoform-Specific RAF-KRAS Interactions in Living Cells Using FRET-BRET Hybrid Biosensors. [Abstract]

2026 Feb 12:e15654. PMID: 41674298
Cell Rep Med

Syndecan-1-targeted therapeutic antibody impairs macropinocytosis and elicits antitumor immunity in pancreatic cancer. [Abstract]

2026 Feb 17;7(2):102613. PMID: 41707651
Cell Rep Med

Developing a therapeutic elastase that stimulates anti-tumor immunity by selectively killing cancer cells. [Abstract]

2025 Nov 18;6(11):102446. PMID: 41205593
Cell Rep Med

Overcoming Adaptive Resistance to KRAS and MEK Inhibitors by Co-targeting mTORC1/2 Complexes in Pancreatic Cancer. [Abstract]

2020 Nov 17;1(8):100131. PMID: 33294856
Sci Adv

Noncanonical role of Golgi-associated macrophage TAZ in chronic inflammation and tumorigenesis. [Abstract]

2025 Jan 24;11(4):eadq2395. PMID: 39841821
Cell Death Differ

Elevated FSP1 protects KRAS-mutated cells from ferroptosis during tumor initiation. [Abstract]

2023 Feb;30(2):442-456. PMID: 36443441
Cell Death Dis

Simultaneous targeting of KRAS and CDK4 synergistically induces durable growth arrest in pancreatic cancer cells. [Abstract]

2025 Dec 23. PMID: 41436723
Cell Death Dis

Anlotinib enhances the efficacy of KRAS-G12C inhibitors through c-Myc/ORC2 axis inhibition in non-small cell lung cancer. [Abstract]

2025 May 2;16(1):356. PMID: 40316534
Pharmacol Res

ABCB1 limits brain exposure of the KRASG12C inhibitor sotorasib, whereas ABCB1, CYP3A, and possibly OATP1a/1b restrict its oral availability. [Abstract]

2022 Apr:178:106137. PMID: 35192958
Cancer Lett

PDP1 promotes KRAS mutant colorectal cancer progression by serving as a scaffold for BRAF and MEK1. [Abstract]

2024 Jun 5:217007. PMID: 38849010
Cancer Lett

AKT1/FOXP3 axis-mediated expression of CerS6 promotes p53 mutant pancreatic tumorigenesis. [Abstract]

2021 Dec 1:522:105-118. PMID: 34343636
Cell Commun Signal

Off-target engagement of sotorasib with PPARγ via FABP4: a novel mechanism driving interstitial lung disease. [Abstract]

2025 Oct 2;23(1):416. PMID: 41039446
Cell Commun Signal

KRAS-mutant non-small cell lung cancer (NSCLC) therapy based on tepotinib and omeprazole combination. [Abstract]

2024 Jun 12;22(1):324. PMID: 38867255
Clin Cancer Res

Theranostic targeting of CUB domain containing protein 1 (CDCP1) in multiple subtypes of bladder cancer. [Abstract]

2023 Apr 3;29(7):1232-1242. PMID: 36648492
Clin Cancer Res

Epithelial-to-Mesenchymal Transition is a Cause of Both Intrinsic and Acquired Resistance to KRAS G12C Inhibitor in KRAS G12C-Mutant Non-Small Cell Lung Cancer. [Abstract]

2020 Nov 15;26(22):5962-5973. PMID: 32900796
Clin Cancer Res

Vertical Pathway Inhibition Overcomes Adaptive Feedback Resistance to KRASG12C Inhibition. [Abstract]

2020 Apr 1;26(7):1633-1643. PMID: 31776128
Cell Death Discov

AURKA/PHB2 signaling drives acquired resistance to KRAS G12C inhibitors in KRAS G12C-mutant NSCLC. [Abstract]

2026 Apr 25. PMID: 42031711
Acta Pharmacol Sin

143D, a novel selective KRASG12C inhibitor exhibits potent antitumor activity in preclinical models. [Abstract]

2023 Jul;44(7):1475-1486. PMID: 36725884
NPJ Precis Oncol

KRAS mutated lung adenocarcinoma responds to pan-ERBB and Aurora kinase inhibitors. [Abstract]

2026 Jan 12;10(1):14. PMID: 41526435
NPJ Precis Oncol

Mechanisms of KRAS inhibitor resistance in KRAS-mutant colorectal cancer harboring Her2 amplification and aberrant KRAS localization. [Abstract]

2025 Jan 6;9(1):4. PMID: 39762482
Oncogene

Targeting ATF3-mediated asparagine biosynthesis reverses acquired resistance to KRASG12C inhibitors. [Abstract]

2026 Jul;45(28):2808-2822. PMID: 42270775
Cell Chem Biol

Systematic cysteine scanning identifies a druggable pocket in oncogenic KRAS. [Abstract]

2026 Feb 11:S2451-9456(26)00027-9. PMID: 41679298
Cell Chem Biol

Specific inhibition of oncogenic RAS using cell-permeable RAS-binding domains. [Abstract]

2021 Nov 18;28(11):1581-1589.e6. PMID: 33964212
Int J Biol Macromol

Ganoderma microsporum immunomodulatory protein combined with KRASG12C inhibitor impedes intracellular AKT/ERK network to suppress lung cancer cells with KRAS mutation. [Abstract]

2024 Feb;259(Pt 2):129291. PMID: 38211909
Br J Cancer

Farnesyl-transferase inhibitors show synergistic anticancer effects in combination with novel KRAS-G12C inhibitors. [Abstract]

2024 Apr;130(6):1059-1072. PMID: 38278976
Cell Rep

Mutant KRAS-driven selective mRNA translation reveals mechanisms and therapeutic vulnerabilities in cancer. [Abstract]

2026 Jun 23;45(6):117520. PMID: 42284146
Cell Rep

The TRIM4 E3 ubiquitin ligase degrades TPL2 and is modulated by oncogenic KRAS. [Abstract]

2024 Aug 22;43(9):114667. PMID: 39178114
Cell Rep

KRASG12C-independent feedback activation of wild-type RAS constrains KRASG12C inhibitor efficacy. [Abstract]

2022 Jun 21;39(12):110993. PMID: 35732135
J Med Chem

Discovery of Novel, Potent, and Orally Bioavailable SMARCA2 Proteolysis-Targeting Chimeras with Synergistic Antitumor Activity in Combination with Kirsten Rat Sarcoma Viral Oncogene Homologue G12C Inhibitors. [Abstract]

2025 Apr 25. PMID: 40280558
Mol Cancer Ther

MRTX1133 suppresses ERK signaling but elicits context-dependent antiproliferative responses in KRAS (G12C) cancer cells. [Abstract]

2026 Mar 14. PMID: 41830517
Mol Cancer Ther

AMT-562, a Novel HER3-targeting Antibody-Drug Conjugate, Demonstrates a Potential to Broaden Therapeutic Opportunities for HER3-expressing Tumors. [Abstract]

2023 Sep 5;22(9):1013-1027. PMID: 37302522
Biochem Pharmacol

Sotorasib induces intestinal epithelial injury through suppression of the cAMP/PKA/CREB signaling axis. [Abstract]

2026 May 16:118078. PMID: 42144204
Cell Rep Methods

Tumor immune microenvironment reconstitution in patient-derived organoids enables therapy modeling for NSCLC. [Abstract]

2026 Jun 15;6(6):101339. PMID: 42134319
Int J Mol Sci

Novel Camptothecin Derivative 9c with Enhanced Antitumor Activity via NSA2-EGFR-P53 Signaling Pathway. [Abstract]

2025 Feb 25;26(5):1987. PMID: 40076615
Int J Mol Sci

Triple Blockade of Oncogenic RAS Signaling Using KRAS and MEK Inhibitors in Combination with Irradiation in Pancreatic Cancer. [Abstract]

2024 Jun 6;25(11):6249. PMID: 38892436
Front Cell Dev Biol

A Covalent Calmodulin Inhibitor as a Tool to Study Cellular Mechanisms of K-Ras-Driven Stemness. [Abstract]

2021 Jul 8:9:665673. PMID: 34307350
ACS Omega

Application and Cross-Validation of a High-Throughput SPR Method for Characterizing Covalent Binding Ligands. [Abstract]

2025 Jul 4;10(27):29637-29646. PMID: 40687013
Transl Oncol

Sotorasib combined with 3-methyladenine for the treatment of KRAS G12C-mutant pancreatic cancer and its underlying mechanisms. [Abstract]

2026 May 26:70:102821. PMID: 42190605
Sci Rep

Cysteine-reactive mitigators of small vessel disease-related NOTCH3 mutants. [Abstract]

2026 Mar 20;16(1):14300. PMID: 41862552
Cancer Sci

Application of plasma circulating KRAS mutations as a predictive biomarker for targeted treatment of pancreatic cancer. [Abstract]

2024 Apr;115(4):1283-1295. PMID: 38348576
Cancers (Basel)

Proteomic Mapping of the Interactome of KRAS Mutants Identifies New Features of RAS Signalling Networks and the Mechanism of Action of Sotorasib. [Abstract]

2023 Aug 17;15(16):4141. PMID: 37627169
J Cell Mol Med

Inactivation of CDK12 Enhances Mitochondrial Efficiency to Suppress DNA Damage. [Abstract]

2026 Apr;30(7):e71101. PMID: 41896195
iScience

Overcoming MET-mediated resistance in oncogene-driven NSCLC. [Abstract]

2023 May 29;26(7):107006. PMID: 37534190
Metabolites

Regulation and Therapeutic Targeting of MTHFD2 and EZH2 in KRAS-Mutated Human Pulmonary Adenocarcinoma. [Abstract]

2022 Jul 15;12(7):652. PMID: 35888776
Bioengineering (Basel)

Evaluation of AMG510 Therapy on KRAS-Mutant Non-Small Cell Lung Cancer and Colorectal Cancer Cell Using a 3D Invasive Tumor Spheroid System under Normoxia and Hypoxia. [Abstract]

2022 Dec 12;9(12):792. PMID: 36550998
Eur J Cell Biol

Detection of Ras nanoclustering-dependent homo-FRET using fluorescence anisotropy measurements. [Abstract]

2023 Apr 11;102(2):151314. PMID: 37058825
J Biol Chem

Oncogenic RAS promotes MYC protein stability by upregulating the expression of the inhibitor of apoptosis protein family member Survivin. [Abstract]

2023 Feb;299(2):102842. PMID: 36581205

Sotorasib purchased from MedChemExpress. Usage Cited in: J Biol Chem. 2023 Feb;299(2):102842. [Abstract]

Sotorasib (1 μM) strongly downregulates survival protein Survivin in MIA PaCa-2 cells.
Cancer Res Commun

Constitutive EGFR Activation Induced by PTPRR Downregulation Confers Resistance to KRAS Inhibitors. [Abstract]

2026 Mar 10. PMID: 41808249
Cancer Res Commun

The Selective WEE1 Inhibitor Azenosertib Shows Synergistic Antitumor Activity with KRASG12C Inhibitors in Preclinical Models. [Abstract]

2025 Feb 1;5(2):240-252. PMID: 39807828
ACS Pharmacol Transl Sci

Suite of Biochemical and Cell-Based Assays for the Characterization of Kirsten Rat Sarcoma (KRAS) Inhibitors and Degraders. [Abstract]

2024 Dec 2;7(12):3921-3934. PMID: 39698278
J Proteome Res

Cholesterol Regulates the Tumor Adaptive Resistance to MAPK Pathway Inhibition. [Abstract]

2021 Dec 3;20(12):5379-5391. PMID: 34751028
Front Oncol

Transcriptomic analysis on pancreatic adenocarcinoma patients uncovers KRAS-mediated PPAR pathway alteration. [Abstract]

2025 Aug 11:15:1613773. PMID: 40860798
Future Med Chem

Identification of KRAS mutants (G12C, G12D, and G12V) inhibitors. [Abstract]

2025 Sep;17(18):2221-2234. PMID: 40959979
PLoS One

Potential of phenothiazines to synergistically block calmodulin and reactivate PP2A in cancer cells. [Abstract]

2022 May 26;17(5):e0268635. PMID: 35617282
Biochem Biophys Res Commun

Carboxyl ester lipase truncation mutant unveils lipotoxicity induced pancreatic β-cell demise. [Abstract]

2025 Oct 17:789:152800. PMID: 41167005
J Chromatogr B Analyt Technol Biomed Life Sci

Validated extended multiplexed LC-MS/MS assay for the quantification of adagrasib and sotorasib in human plasma, together with four additional SMIs. [Abstract]

2023 Dec 1:1231:123918. PMID: 37979367
Biochem Biophys Res Commun

Functional dissection of the KRAS G12C mutation by comparison among multiple oncogenic driver mutations in a lung cancer cell line model. [Abstract]

2021 Jan 1:534:1-7. PMID: 33302159
Biomed Chromatogr

Development and validation of an ultra-performance liquid chromatography-tandem mass spectrometry method to quantify the small molecule inhibitors adagrasib, alectinib, brigatinib, capmatinib, crizotinib, lorlatinib, selpercatinib, and sotorasib in human plasma. [Abstract]

2024 Oct;38(10):e5986. PMID: 39136165
STAR Protoc

Generating drug resistance models in human and murine cancer cell lines and assessing cross-resistance to chemotherapeutics and KRAS inhibitors. [Abstract]

2026 Jun 26;7(3):104649. PMID: 42360881
STAR Protoc

A flow-cytometry-based pipeline for the rapid quantification of C2C12 cell differentiation. [Abstract]

2023 Oct 10;4(4):102637. PMID: 37819762
Drug Discov Ther

Solid phase extraction and high-performance liquid chromatographic determination of lazertinib in human plasma. [Abstract]

2025 Oct 17. PMID: 41110965
bioRxiv

Dual inhibition of GTP-bound (ON) and GDP-bound (OFF) KRASG12C suppresses PI3Kα and leads to potent tumor inhibition. [Abstract]

2026 Apr 30:2026.04.27.718135. PMID: 42094443
Res Sq

2026 Apr 30.
bioRxiv

2026 Mar 12.
bioRxiv

2026 Feb 20.
bioRxiv

2025 Sep 14.
bioRxiv

Post-Translational Modifications Remodel Proteome-Wide Ligandability. [Abstract]

2025 Aug 2:2025.07.31.667978. PMID: 40766426
bioRxiv

Thioredoxin Reductase 1 inhibition triggers ferroptosis in KRAS-independent lung cancers. [Abstract]

2025 Jul 30:2025.07.25.666783. PMID: 40766571
bioRxiv

2025 Jun 13.
Patent

US20250154156A1.
bioRxiv

2025 April 17.
bioRxiv

2025 March 19.
bioRxiv

Revealing Functional Hotspots: Temperature-Dependent Crystallography of K-RAS Highlights Allosteric and Druggable Sites. [Abstract]

2025 Feb 28:2025.02.27.639303. PMID: 40060414
bioRxiv

2025 January 14.
Patent

US20240238294A1
Research Square Preprint

2024 Nov 26.
bioRxiv

All-trans retinoic acid-mediated ADAR1 degradation synergizes with PD-1 blockade to suppress pancreatic cancer. [Abstract]

2024 Oct 23:2024.10.20.619300. PMID: 39484589
Patent

US12083121.
Patent

US20240238294A1.
bioRxiv

2024 July 23.
bioRxiv

Discovery of Novel, Potent and Orally Bioavailable SMARCA2 PROTACs with Synergistic Anti-tumor Activity in Combination with KRAS G12C Inhibitors. [Abstract]

2024 Aug 26:2024.08.23.608456. PMID: 39253520
bioRxiv

Alveolar differentiation drives resistance to KRAS inhibition in lung adenocarcinoma. [Abstract]

2023 Oct 1:2023.09.29.560194. PMID: 37808711
bioRxiv

2023 Oct 6.
Universität zu Köln

2023 Feb 13.
bioRxiv

2023 Jun 22.
Research Square Print

December 21st, 2022.
Patent

US11285156.
bioRxiv

June 17, 2021.

溶剤 & 溶解度

体外:

DMSO : 50 mg/mL (89.19 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 33.33 mg/mL (59.46 mM; ultrasonic and adjust pH to 11 with NaOH)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.7838 mL

8.9192 mL

17.8383 mL

5 mM

0.3568 mL

1.7838 mL

3.5677 mL

10 mM

0.1784 mL

0.8919 mL

1.7838 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

モル濃度計算機

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (3.71 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.08 mg/mL (3.71 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (3.71 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 20% HP-β-CD in Saline

Solubility: 10 mg/mL (17.84 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Working solution concentration: 0.22 mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact

MedChemExpress (MCE) .

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (285 KB)
SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
取扱説明書 (2659 KB)

参考文献

[1]. Marwan Fakih, et al, Phase 1 study evaluating the safety, tolerability, pharmacokinetics (PK), and efficacy of AMG 510, a novel small molecule KRASG12Cinhibitor, in advanced solid tumors. Journal of Clinical Oncology.

[2]. Karen Rex, et al. Abstract 3090: In vivo characterization of AMG 510 - a potent and selective KRASG12Ccovalent small molecule inhibitor in preclinical KRASG12Ccancer models. Experimental and Molecular Therapeutics.

[3]. Canon J, et al. The clinical KRAS(G12C) inhibitor AMG 510 drives anti-tumour immunity. Nature. 2019 Nov;575(7781):217-223. [Content Brief]

[4]. Brian A. Lanman, et al.Abstract 4455: Discovery of AMG 510, a first-in-human covalent inhibitor of KRASG12C for the treatment of solid tumors. Cancer Chemistry.

[5]. Wu LL, et al. AMG-510 and cisplatin combination increases antitumor effect in lung adenocarcinoma with mutation of KRAS G12C: a preclinical and translational research. Discov Oncol. 2023 Jun 7;14(1):91. [Content Brief]

[6]. Ryan MB, et al. KRASG12C-independent feedback activation of wild-type RAS constrains KRASG12C inhibitor efficacy. Cell Rep. 2022 Jun 21;39(12):110993. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
H₂O / DMSO	1 mM	1.7838 mL	8.9192 mL	17.8383 mL	44.5959 mL
	5 mM	0.3568 mL	1.7838 mL	3.5677 mL	8.9192 mL
	10 mM	0.1784 mL	0.8919 mL	1.7838 mL	4.4596 mL
	15 mM	0.1189 mL	0.5946 mL	1.1892 mL	2.9731 mL
	20 mM	0.0892 mL	0.4460 mL	0.8919 mL	2.2298 mL
	25 mM	0.0714 mL	0.3568 mL	0.7135 mL	1.7838 mL
	30 mM	0.0595 mL	0.2973 mL	0.5946 mL	1.4865 mL
	40 mM	0.0446 mL	0.2230 mL	0.4460 mL	1.1149 mL
	50 mM	0.0357 mL	0.1784 mL	0.3568 mL	0.8919 mL
DMSO	60 mM	0.0297 mL	0.1487 mL	0.2973 mL	0.7433 mL
DMSO	80 mM	0.0223 mL	0.1115 mL	0.2230 mL	0.5574 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Keywords

Sotorasib

121 Cited Publications

100 mg お問い合わせ

Subscribe to the

MedChemExpress

Newsletter

製品名:
製品番号:
数量:
日本の代理先をお選びください:

製品名:
CAS 番号:
生物種:
純度:
数量:

Sotorasib

GPCR/G Protein Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

MAPK Compound Library

FDA-Approved Drug Library

Anti-Cancer Compound Library

Drug Repurposing Compound Library

Covalent Screening Library

Oxygen Sensing Compound Library

Ferroptosis Compound Library

Orally Active Compound Library

Chemical Probe Library

Glutamine Metabolism Compound Library

FDA Approved & Pharmacopeial Drug Library

Anti-Lung Cancer Compound Library

Drug-Induced Liver Injury (DILI) Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Angiogenesis-Related Compound Library

Targeted Diversity Library

Anti-Liver Cancer Compound Library

Rare Diseases Drug Library

Anti-Colorectal Cancer Compound Library

FDA-Approved Anticancer Drug Library

Human Metabolite Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

Kinase Inhibitor Library Mini

MCE Bioactive Compound Library

Covalent Screening Library Plus

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Anti-Cancer Approved Drug Library

Mass Spectrometry Human Metabolite Library

Posttranslational Modification Library

FDA Kinase Inhibitor Library

Lactylation Compound Library

KRAS Targeted Compound Library

MedChemExpress（MCE）の使用を引用している文献 Sotorasib

Ras アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (121)

溶剤 & 溶解度

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

Sotorasib 関連分類

HY-114277 関連分類