Name: LY2109761
Brand: Selleck Chemicals
SKU: S2704
Rating: 5 (139 reviews)

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품질 관리 (Quality Control)

배치: 순도: 99.99%

99.99

함께 자주 사용되는 제품 LY2109761

Galunisertib (LY2157299)

It and Galunisertib target TGF-β receptor I and exhibit anti-tumor activity.

관련 타겟	PKC ROCK Bcr-Abl
기타 TGF-beta/Smad 억제제	SB431542 RepSox (E-616452) Vactosertib (TEW-7197) LDN-193189 A-83-01 LDN-193189 Dihydrochloride SRI-011381 (C381) SIS3 Hydrochloride SB-525334 DMH1

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

세포주	분석 유형	농도	배양 시간	제형	활성 설명	PMID
HepG2	Function Assay	10 μM	2 h		inhibits autophagy induction by galangin	25268046
PC-3	Function Assay	0.2/2/4 μM	24 h	DMSO	inhibits TGF-β1–induced Smad2 activation	22173053
PMOs	Function Assay	0.2/2/4 μM	24 h	DMSO	inhibits TGF-β1–induced Smad2 activation	22173053
PC-3	Growth Inhibition Assay	0.2/2 μM	24 h	DMSO	blocks the inhibition of cell proliferation produced by TGF-β1	22173053
PMOs	Growth Inhibition Assay	0.2/2 μM	24 h	DMSO	blocks the inhibition of cell proliferation produced by TGF-β1	22173053
U87MG	Growth Inhibition Assay	5/10 μM	2 h		enhances radiosensitivity	22006998
T98	Growth Inhibition Assay	5/10 μM	2 h		enhances radiosensitivity	22006998
U87MG	Apoptosis Assay	10 μM	2 h		enhances radiation-induced DNA damage and apoptosis rates	22006998
NMA-23	Apoptosis Assay	10 μM	2 h		enhances radiation-induced DNA damage and apoptosis rates	22006998
HLE	Function Assay	0.01-100 nM	48 h		inhibits the migration in a dose-dependent manner	20844878
HLF	Function Assay	0.01-100 nM	48 h		inhibits the migration in a dose-dependent manner	20844878
10A/HER2YVMA	Growth Inhibition Assay	0.1-0.5 μM	9 d		reduces the size, invasiveness and cell number of colonies	20383197
MC38	Growth Inhibition Assay	5 μM	5 d		inhibits cell growth in a time-dependent manner	19909744
U937	Growth Inhibition Assay	5-20 μM	24-72 h		inhibits cell growth slightly	18492113
HLE	Cytotoxity Assay	0.001-20 μM	48 h		induces cell cytotoxity in a dose-dependent manner	18318443
HLF	Cytotoxity Assay	0.001-20 μM	48 h		induces cell cytotoxity in a dose-dependent manner	18318443
Sf9	Function assay		1 hr		Inhibition of human His-tagged TGFbetaR1 T204D mutant expressed in Sf9 insect cells after 1 hr by HTRF assay, IC50 = 0.0037 μM.	29422332
Sf9	Function assay				Inhibition of TGFbeta type receptor 1 ALK5 (T204D) expressed in Sf9 cells, IC50 = 0.069 μM.	18314943
Mv1Lu-p3TP-Lux	Antiproliferative assay				Antiproliferative activity against mink Mv1Lu-p3TP-Lux cells by luciferase reporter assay, IC50 = 0.18 μM.	18314943
NIH3T3	Antiproliferative assay				Antiproliferative activity against mouse NIH3T3 cells by [3H]thymidine assay, IC50 = 0.21 μM.	18314943
Calu6	Function assay				Inhibition of TGFbeta type receptor 1 in orally dosed human Calu6 cells xenografted mouse by IVTI pharmacokinetic assay, EC50 = 0.236 μM.	18314943
T-cells	Function assay		1 hr		Inhibition of TGFbetaR1 in human primary T-cells assessed as TGFbeta-stimulated PSMAD phosphorylation preincubated for 1 hr followed by TGFbeta addition measured after 90 mins by Alpha screen assay, IC50 = 0.37 μM.	29422332
Mv1Lu	Function assay		1 hr		Inhibition of TGFbetaR1 in mink Mv1Lu cells assessed as TGFbeta-stimulated PSMAD2 phosphorylation preincubated for 1 hr followed by TGFbeta addition measured after 15 mins, IC50 = 0.75 μM.	29422332
클릭하여 더 많은 세포주 실험 데이터 보기

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

분자량	441.52	화학식	C₂₆H₂₇N₅O₂	보관 (수령일로부터)	3년-20°C분말
CAS 번호	700874-71-1	SDF 다운로드		원액 보관	1년-80°C용매에 보관 1개월-20°C용매에 보관
동의어	N/A			Smiles	C1CC2=C(C(=NN2C1)C3=CC=CC=N3)C4=C5C=CC(=CC5=NC=C4)OCCN6CCOCC6

용해도 (Solubility)

In vitro
배치:

DMSO : 9 mg/mL (20.38 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 19 mg/mL (43.03 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 10.8 mg/mL (24.46 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 13 mg/mL (29.44 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 10 mg/mL (22.64 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)

Targets/IC₅₀/Ki	TβRI (Cell-free assay) 38 nM(Ki) TβRII (Cell-free assay) 300 nM(Ki)
시험관 내(In vitro)	LY2109761 treatment induces a dose-dependent low-anchorage growth inhibition of L3.6pl/GLT cells, leading to ~33% or 73% inhibition at 2 μM and 20 μM, respectively, which can be strongly enhanced when in combination index value of 0.36581. Blocking TβRI/II kinase activity with this compound completely suppresses both the basal and TGF-β1-stimulated migration and invasion of L3.6pl/GLT cells, significantly enhances the detachment-induced apoptosis by 26% at 8 hours treatment, and completely suppresses TGF-β–induced Smad2 phosphorylation. This chemical treatment at 1 nM is sufficient to significantly block the migration and invasion but not adhesion of hepatocellular carcinoma cells by increasing E-cadherin expression. It pretreatment enhances radiosensitivity of glioblastoma cells via TGF-β signaling blockage. This compound reduces the self-renewal and proliferation of GBM-derived cancer stem–like cells (CSLC), which can be significantly enhanced when combined with radiation.
생체 내(In vivo)	Administration of LY2109761 (50 mg/kg) alone or in combination significantly reduces the tumor volume by ~70% and ~90%, respectively, prolongs the survival with the median survival duration of 45.0 days and 77.5 days, respectively, and reduces spontaneous abdominal metastases in the L3.6pl/GLT Xenograft mice model. In consistent with the in vitro effect, administration of this compound alone or in combination with radiation, markedly inhibits tumor growth in the orthotopical CSLC glioblastoma model by 43.4% and 76.3%, respectively, decreases tumor invasion and tumor microvessel density, and significantly enhances radiation-induced tumor growth delay in the U87MG xenograft mice model.
참조	[1] https://pubmed.ncbi.nlm.nih.gov/18413796/ [2] https://pubmed.ncbi.nlm.nih.gov/18318443/ [3] https://pubmed.ncbi.nlm.nih.gov/22006998/

적용 분야 (Applications)

방법	바이오마커	이미지	PMID
Western blot	CDK2 / CDK4 / Cyclin D1 / p-Rb β-catenin / MMP-9 / MMP-2 / nm23 / uPA / COX-2 E-cadherin p-Smad2 / Smad		19909744

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):

LY2109761 TGF-beta/Smad inhibitor

화학 구조

분자량: 441.52

품질 관리 (Quality Control)

함께 자주 사용되는 제품 LY2109761

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)

LY2109761 TGF-beta/Smad inhibitor

화학 구조

분자량: 441.52

품질 관리 (Quality Control)

함께 자주 사용되는 제품 LY2109761

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)

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