Name: Trametinib (GSK1120212)
Brand: Selleck Chemicals
SKU: S2673
Rating: 5 (1326 reviews)

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품질 관리 (Quality Control)

배치: 순도: 99.98%

99.98

관련 타겟	ERK p38 MAPK Raf JNK Ras KRas S6 Kinase MAP4K TAK1 Mixed Lineage Kinase
기타 MEK 억제제	PD0325901 (Mirdametinib) U0126-EtOH PD 98059 CI-1040 (PD184352) (E/Z)-BIX02189 Pimasertib (AS-703026) Refametinib (RDEA119) TAK-733 AZD8330 GDC-0623

세포 배양, 처리 및 작업 농도
(Cell Culture, Treatment & Working Concentration)

세포주	분석 유형	농도	배양 시간	제형	활성 설명	PMID
MDA-MB-231, SW480 and SW1116 cells	Function assay	100 nM	24 h		trametinib could decrease YAP levels and inhibit LMB-induced YAP upregulation in MDA-MB-231, SW1116 and SW480 cells	30833665
RG7388-resistant U87MG cells	Function assay	10 nM	24 h	DMSO	Trametinib treatment reduced the invasive phenotype of RG7388 resistant cells.	30274984
BJAB cells	Function assay	0.01μM	24 h		0.01 μM trametinib effectively suppressed the ERK hyperactivation in BJAB cells caused by the combined treatment of BKM120 and Danusertib.	30947576
Human PDAC cell lines (MIA-PACA, PANC-1, CFPAC-1, PL45, CAPAN-2 and HPAF-II)	Function assay	10 nM or 100 nM	3-days or 6-days		The concentration of 10 nM trametinib consistently produced significant differences between gefitinib and trametinib alone compared to combination gefitinib and trametinib in all four sensitive cell lines (CFPAC-1, pl45, CAPAN-2 and HPAF-II). No additive effect was observed in the gefitinib insensitive or excitatory cell lines (MIA-Paca and PANC-1)	30921351
Transitional cell carcinoma (TCC) cell lines	Function assay	25 nM	6-24 h		Canine TCC cell lines are sensitive to MEK inhibition	31048548
COLO205	Growth inhibition assay		72 h		IC50 = 0.001 μM	ChEMBL
HT-29	Growth inhibition assay		72 h		IC50 = 0.001 μM	ChEMBL
COLO205	Growth inhibition assay		72 h		IC50 = 0.001 μM	ChEMBL
MV522	Growth inhibition assay		72 h		IC50 = 0.001 μM	ChEMBL
HT-29	Growth inhibition assay		72 h		IC50 = 0.002 μM	ChEMBL
MV522	Growth inhibition assay		72 h		IC50 = 0.002 μM	ChEMBL
NCI-H727	Growth inhibition assay		72 h		IC50 = 0.002 μM	ChEMBL
NCI-H727	Growth inhibition assay		72 h		IC50 = 0.002 μM	ChEMBL
SW1417	Growth inhibition assay		72 h		IC50 = 0.003 μM	ChEMBL
SW1417	Growth inhibition assay		72 h		IC50 = 0.003 μM	ChEMBL
Calu6	Growth inhibition assay		72 h		IC50 = 0.003 μM	ChEMBL
LS1034	Growth inhibition assay		72 h		IC50 = 0.004 μM	ChEMBL
SW1463	Growth inhibition assay		72 h		IC50 = 0.004 μM	ChEMBL
SW1463	Growth inhibition assay		72 h		IC50 = 0.004 μM	ChEMBL
Calu6	Growth inhibition assay		72 h		IC50 = 0.004 μM	ChEMBL
LS1034	Growth inhibition assay		72 h		IC50 = 0.005 μM	ChEMBL
RKO	Growth inhibition assay		72 h		IC50 = 0.005 μM	ChEMBL
NCI-H508	Growth inhibition assay		72 h		IC50 = 0.008 μM	ChEMBL
KM12	Growth inhibition assay		72 h		IC50 = 0.01 μM	ChEMBL
A427	Growth inhibition assay		72 h		IC50 = 0.01 μM	ChEMBL
NCI-H1155	Growth inhibition assay		72 h		IC50 = 0.01 μM	ChEMBL
HCT8	Growth inhibition assay		72 h		IC50 = 0.014 μM	ChEMBL
MDA-MB-175-VII	Growth inhibition assay		72 h		IC50 = 0.016 μM	ChEMBL
A549	Growth inhibition assay		72 h		IC50 = 0.016 μM	ChEMBL
RKO	Growth inhibition assay		72 h		IC50 = 0.018 μM	ChEMBL
NCI-H23	Growth inhibition assay		72 h		IC50 = 0.02 μM	ChEMBL
A427	Growth inhibition assay		72 h		IC50 = 0.022 μM	ChEMBL
KM12	Growth inhibition assay		72 h		IC50 = 0.023 μM	ChEMBL
NCI-H508	Growth inhibition assay		72 h		IC50 = 0.023 μM	ChEMBL
MDA-MB-231	Growth inhibition assay		3 days		GI50 = 0.025 μM	ChEMBL
SW837	Growth inhibition assay		72 h		IC50 = 0.025 μM	ChEMBL
SW480	Growth inhibition assay		72 h		IC50 = 0.026 μM	ChEMBL
NCI-H1355	Growth inhibition assay		72 h		IC50 = 0.027 μM	ChEMBL
NCI-H23	Growth inhibition assay		72 h		IC50 = 0.029 μM	ChEMBL
EFM19	Growth inhibition assay		72 h		IC50 = 0.03 μM	ChEMBL
T84	Growth inhibition assay		72 h		IC50 = 0.03 μM	ChEMBL
A549	Growth inhibition assay		72 h		IC50 = 0.034 μM	ChEMBL
NCI-H1792	Growth inhibition assay		72 h		IC50 = 0.035 μM	ChEMBL
SW480	Growth inhibition assay		72 h		IC50 = 0.037 μM	ChEMBL
COR-L23	Growth inhibition assay		72 h		IC50 = 0.037 μM	ChEMBL
SW1573	Growth inhibition assay		72 h		IC50 = 0.038 μM	ChEMBL
Calu3	Growth inhibition assay		72 h		IC50 = 0.039 μM	ChEMBL
HCC827	Growth inhibition assay		72 h		IC50 = 0.04 μM	ChEMBL
HOP62	Growth inhibition assay		72 h		IC50 = 0.05 μM	ChEMBL
NCI-H1355	Growth inhibition assay		72 h		IC50 = 0.052 μM	ChEMBL
NCI-H1792	Growth inhibition assay		72 h		IC50 = 0.053 μM	ChEMBL
HCT8	Growth inhibition assay		72 h		IC50 = 0.055 μM	ChEMBL
T84	Growth inhibition assay		72 h		IC50 = 0.061 μM	ChEMBL
SW900	Growth inhibition assay		72 h		IC50 = 0.072 μM	ChEMBL
SW837	Growth inhibition assay		72 h		IC50 = 0.074 μM	ChEMBL
DLD1	Growth inhibition assay		72 h		IC50 = 0.093 μM	ChEMBL
MDA-MB-175-VII	Growth inhibition assay		72 h		IC50 = 0.096 μM	ChEMBL
SW900	Growth inhibition assay		72 h		IC50 = 0.127 μM	ChEMBL
Calu3	Growth inhibition assay		72 h		IC50 = 0.158 μM	ChEMBL
COR-L23	Growth inhibition assay		72 h		IC50 = 0.329 μM	ChEMBL
DLD1	Growth inhibition assay		72 h		IC50 = 0.632 μM	ChEMBL
클릭하여 더 많은 세포주 실험 데이터 보기

화학 정보, 보관 및 안정성 (Chemical Information, Storage & Stability)

분자량	615.39	화학식	C₂₆H₂₃FIN₅O₄	보관 (수령일로부터)	3년-20°C분말
CAS 번호	871700-17-3	SDF 다운로드		원액 보관	1년-80°C용매에 보관 1개월-20°C용매에 보관
동의어	JTP-74057			Smiles	CC1=C2C(=C(N(C1=O)C)NC3=C(C=C(C=C3)I)F)C(=O)N(C(=O)N2C4=CC=CC(=C4)NC(=O)C)C5CC5

용해도 (Solubility)

In vitro
배치:

DMSO : 8 mg/mL (12.99 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 100 mg/mL (162.49 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 100 mg/mL (162.49 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 100 mg/mL (162.49 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 22 mg/mL (35.74 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

몰농도 계산기

질량	농도	부피	분자량
=	×	×

희석 계산기 분자량 계산기

In vivo 배치:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

생체 내 제형 계산기 (투명한 용액)

1단계: 아래 정보 입력 (권장: 실험 중 손실을 고려하여 추가 동물 포함)

투여량: mg/kg 동물 평균 체중: g 동물당 투여량:μL 동물 수:

2단계: 생체 내 제형 입력 (이것은 계산기일 뿐 제형이 아닙니다. 용해도 섹션에 생체 내 제형이 없는 경우 먼저 당사에 문의하십시오.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

계산 결과:

작업 농도: mg/ml;

DMSO 원액 준비 방법: mg 약물 사전 용해 μL DMSO ( 원액 농도 mg/mL, 농도가 해당 약물 배치의 DMSO 용해도를 초과하는 경우 먼저 당사에 문의하십시오. )

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가μL PEG300, 혼합하고 투명하게 한 다음 추가μL Tween 80, 혼합하고 투명하게 한 다음 추가 μL ddH₂O, 혼합하고 투명하게 합니다.

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가 μL 옥수수 기름, 혼합하고 투명하게 합니다.

참고: 1. 다음 용매를 추가하기 전에 액체가 투명한지 확인하십시오.
2. 용매를 순서대로 추가해야 합니다. 다음 용매를 추가하기 전에 이전 추가에서 얻은 용액이 투명한 용액인지 확인해야 합니다. 와동, 초음파 또는 뜨거운 물 중탕과 같은 물리적 방법을 사용하여 용해를 도울 수 있습니다.

작용 메커니즘 (Mechanism of Action)

특징	More potent than PD0325901 or AZD6244.
Targets/IC₅₀/Ki	MEK1 (Cell-free assay) 0.92 nM MEK2 (Cell-free assay) 1.8 nM
시험관 내(In vitro)	Trametinib (GSK1120212) inhibits the phosphorylation of MBP regardless of the isotype of Raf and MEK, with IC50 ranging from 0.92 nM to 3.4 nM. It demonstrates no inhibition of the kinase activities of c-Raf, B-Raf, ERK1 and ERK2. In addition, this compound does not show drastic inhibitory activity against the other 98 kinases. It displays potent inhibitory activity against human colorectal cancer cell lines. HT-29 and COLO205 cells, which are known to have a constitutively active B-Raf mutant, are most sensitive to it with IC50 0.48 nM and 0.52 nM, respectively. The cell lines bearing a K-Ras mutation show a wide range of sensitivity to it with IC50 of 2.2-174 nM. In contrast, COLO320 DM cells, bearing the wild-type gene in both B-Raf and K-Ras, are found to be resistant even at 10 μM. Treatment for 24 hours induces cell-cycle arrest at the G1 phase in all sensitive cell lines. Consistently, it leads to upregulation of p15^INK4b and/or p27^KIP1 in most of the colorectal cancer cell lines. It inhibits constitutive ERK phosphorylation in all sensitive cell lines. This compound induces apoptosis both in HT-29 and COLO205 cells, but that COLO205 cells are more sensitive than HT-29 cells in terms of apoptosis induction. It blocks tumor necrosis factor-α and interleukin-6 production from peripheral blood mononuclear cells (PBMCs).
키나아제 분석	Raf-MEK-ERK cascade kinase assay
키나아제 분석	Non-phosphorylated myelin basic protein (MBP) is coated onto an ELISA plate, and the active form of B-Raf/c-Raf is mixed with unphosphorylated MEK1/MEK2 and ERERK2 in 10 μM ATP and 12.5 mM MgCl₂ containing MOPS buffer in the presence of various concentrations of Trametinib (GSK1120212). The phosphorylation of MBP is detected by the anti-phospho-MBP antibody.
생체 내(In vivo)	Oral administration of Trametinib (GSK1120212) at 0.3 mg/kg or 1 mg/kg once daily for 14 days is effective in inhibiting the HT-29 xenograft growth, and 1 mg/kg of this compound almost completely blocks the tumor increase. The phosphorylation of ERK1/2 is completely inhibited in the established tumor tissues by single oral dose of 1 mg/kg, and both p15^INK4b and p27^KIP1 protein levels are upregulated after 14 days of treatment. In the COLO205 xenograft model, tumor regression is observed even at a dose of 0.3 mg/kg. At a dose of 1 mg/kg, a complete regression is obtained in 4 out of 6 mice in which the tumor degenerates to the point that tumor volume is not measurable. Administration at 0.1 mg/kg almost completely suppresses adjuvant-induced arthritis (AIA) and type II collagen-induced arthritis (CIA) in Lewis rats or DBA1/J mice, respectively.
참조	[1] https://pubmed.ncbi.nlm.nih.gov/21523318/ [2] https://pubmed.ncbi.nlm.nih.gov/22245957/ [3] https://pubmed.ncbi.nlm.nih.gov/22389471/ [4] https://pubmed.ncbi.nlm.nih.gov/22733540/

적용 분야 (Applications)

방법	바이오마커	PMID
Western blot	ERRα / IDH3 / c-Myc / Cyclin D1 pERK /ERK / pS6 / S6 β-catenin	30185207
Growth inhibition assay	Cell proliferation MTT assay	30185207
Immunofluorescence	phospho-PR(S345) β-catenin	29237804

임상시험 정보 (Clinical Trial Information)

(데이터 출처 https://clinicaltrials.gov, 업데이트 날짜 2024-05-22)

NCT 번호	모집	조건	스폰서/협력자	시작일	단계
NCT05275374	Not yet recruiting	Cancer\|BRAF V600 Mutation\|Melanoma\|Colorectal Cancer\|Thyroid Cancer\|Nonsmall Cell Lung Cancer	Xynomic Pharmaceuticals Inc.	December 2024	Phase 1\|Phase 2
NCT06098872	Not yet recruiting	Arteriovenous Malformations	University Health Network Toronto	November 2023	Phase 2
NCT05907304	Recruiting	Advanced or Metastatic Solid Tumors	Erasca Inc.	August 17 2023	Phase 1
NCT05874414	Recruiting	Cholangiocarcinoma	Genfit	August 21 2023	Phase 1\|Phase 2

자주 묻는 질문 (Frequently Asked Questions)

질문 1:
Could you help us with the best way to prepare it for in vivo i.p. injections?

답변:
It can be dissolved in 4% DMSO/corn oil at 3 mg/ml clearly.

질문 2:
How to solve the problem that it didn't dissolve up to 10mM in DMSO at room temperature?

답변:
The solution can be heated up to 50 degrees to help dissolve it. Besides, sonication (with a probe sonicator) also greatly helps with this compound.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

Trametinib (GSK1120212) MEK inhibitor

화학 구조

분자량: 615.39

품질 관리 (Quality Control)

세포 배양, 처리 및 작업 농도
(Cell Culture, Treatment & Working Concentration)

화학 정보, 보관 및 안정성 (Chemical Information, Storage & Stability)

용해도 (Solubility)

몰농도 계산기

생체 내 제형 계산기 (투명한 용액)

작용 메커니즘 (Mechanism of Action)

적용 분야 (Applications)

임상시험 정보 (Clinical Trial Information)

자주 묻는 질문 (Frequently Asked Questions)

Trametinib (GSK1120212) MEK inhibitor

화학 구조

분자량: 615.39

품질 관리 (Quality Control)

세포 배양, 처리 및 작업 농도 (Cell Culture, Treatment & Working Concentration)

화학 정보, 보관 및 안정성 (Chemical Information, Storage & Stability)

용해도 (Solubility)

몰농도 계산기

생체 내 제형 계산기 (투명한 용액)

작용 메커니즘 (Mechanism of Action)

적용 분야 (Applications)

임상시험 정보 (Clinical Trial Information)

자주 묻는 질문 (Frequently Asked Questions)

세포 배양, 처리 및 작업 농도
(Cell Culture, Treatment & Working Concentration)