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Combretastatin A4 Microtubule Associated 억제제

Name: Combretastatin A4
Brand: Selleck Chemicals
SKU: S7783
Rating: 5 (7 reviews)

제품 번호S7783

Combretastatin A4는 microtubule 표적화 약물로, 0.4 μM의 K_d로 β-튜불린에 결합합니다. 3상.

Combretastatin A4 Microtubule Associated 억제제 Chemical Structure

화학 구조

분자량: 316.35

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품질 관리

배치: S778301 DMSO]63 mg/mL]false]Ethanol]34 mg/mL]false]Water]Insoluble]false 순도: 99.87%

최고 수준의 품질로 Nature Medicine에 인용됨
COA
NMR
SDS
데이터시트

99.87

관련 타겟	Akt Wnt/beta-catenin PKC HSP ROCK Integrin Bcr-Abl Actin FAK Kinesin
기타 Microtubule Associated 억제제	Nocodazole MMAF Patupilone (Epothilone B) Lexibulin (CYT997) CW069 Epothilone A ABT-751 (E7010) TAI-1 Cucurbitacin B INH1

세포 배양, 처리 및 작업 농도

세포주	분석 유형	배양 시간	활성 설명
SKMEL-5	Growth inhibition assay		Cytotoxic concentration required to inhibit 50% cell growth in SKMEL-5 melanoma cell lines, ED50=3.00E-08 μM
A-549	Growth inhibition assay		Cytotoxic concentration required to inhibit 50% cell growth in A-549 lung carcinoma cell lines, ED50=1.20E-06 μM
MCF-7	Growth inhibition assay		Cytotoxic concentration required to inhibit 50% cell growth in MCF-7 breast carcinoma cell lines, ED50=3.80E-06 μM
HT-29	Growth inhibition assay		Cytotoxic concentration required to inhibit 50% cell growth in HT-29 colon adenocarcinoma cell lines, ED50=1.20E-06 μM
MLM melanoma cell	Growth inhibition assay		Cytotoxic concentration required to inhibit 50% cell growth in MLM melanoma cell lines, ED50=1.40E-06 μM
M14	Cytotoxicity assay		In vitro cytotoxic activity was tested against human melanoma cancer (M14) cell line, GI50=0.0001 μM
SK-OV3	Cytotoxicity assay		In vitro cytotoxic activity tested against human ovarian cancer (SK-OV3) cell line, GI50=0.0001 μM
HL60 cells	Cytotoxicity assay	72 h	Cytotoxicity against human HL60 cells after 72 hrs by MTT assay, IC50=0.0001 μM
SK-OV-3	Growth inhibition assay	48 h	Growth inhibition of human SK-OV-3 after 48 hrs by SRB assay, GI50=0.00013 μM
HepG2 cells	Cytotoxicity assay		Cytotoxicity against human HepG2 cells, IC50=0.00014 μM
ZR-75-1	Cytotoxicity assay		Cytotoxicity against ZR-75-1 cell line, IC50=0.00024 μM
HeLa cell	Cytotoxicity assay		Cytotoxicity against HeLa cell line, IC50=0.0003 μM
HCT116 cell	Cytotoxicity assay		Cytotoxicity against HCT116 cell line, IC50=0.00035 μM
KBV1 cells	Cytotoxicity assay	72 h	Cytotoxicity against human vinblastine-resistant KBV1 cells after 72 hrs by MTT assay, IC50=0.0004 μM
SKOV3	Cytotoxicity assay		Cytotoxicity against human SKOV3 cells by SRB assay, GI50=0.00042 μM
SKOV3 cells	Growth inhibition assay		Growth inhibition of human SKOV3 cells by sulforhodamine B assay, GI50=0.00042 μM
HeLa cells	Cytotoxicity assay		Cytotoxicity against human HeLa cells by MTT assay, IC50=0.00051 μM
DU145 cells	Cytotoxicity assay		Cytotoxicity against human DU145 cells by SRB assay, GI50=0.00054 μM
DU145 cells	Growth inhibition assay		Growth inhibition of human DU145 cells by sulforhodamine B assay, GI50=0.00054 μM
SK-N-BE	Proliferation assay	72 h	Antiproliferative activity in human SK-N-BE cells assessed as cell viability after 72 hrs by MTT assay, IC50=0.00058 μM
NCIH460 cells	Cytotoxicity assay	48 h	Cytotoxicity against human NCIH460 cells after 48 hrs by SRB assay, GI50=0.0006 μM
KB-VIN10 cells	Proliferation assay	72 h	Antiproliferative activity against human KB-VIN10 cells over-expressing P-gp 170/MDR1 after 72 hrs by methylene blue assay, IC50=0.0007 μM
HCT116 cells	Cytotoxicity assay	72 h	Cytotoxicity against human HCT116 cells assessed as reduction of [3H]thymidine incorporation after 72 hrs by scintillation counting, IC50=0.00074 μM
DU145 cells	Cytotoxicity assay	48 h	Cytotoxicity against human DU145 cells after 48 hrs by SRB assay, GI50=0.0008 μM
RS4:11 cells	Proliferation assay	72 h	Antiproliferative activity against human RS4:11 cells after 72 hrs by (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide test, IC50=0.0008 μM
HCT 116	Growth inhibition assay		Concentration which produces 50% inhibition of growth of human colon tumor HCT 116, IC50=0.0009 μM
HeLa cells	Cytotoxicity assay	72 h	Cytotoxicity against human HeLa cells after 72 hrs by resazurin based fluorescence assay, IC50=0.0009 μM
BNL 1ME A.7R.1 cells	Cytotoxicity assay		Cytotoxicity against mouse BNL 1ME A.7R.1 cells, IC50=0.0009 μM
Calu6	Proliferation assay	48 h	Antiproliferative activity against human Calu6 after 48 hrs by spectrophotometry, IC50=0.00094 μM
melanoma B16 cell	Growth inhibition assay		Concentration which produces 50% inhibition of growth of murine melanoma B16 cell line, IC50=0.001 μM
DU145 cells	Cytotoxicity assay		Cytotoxicity against human DU145 cells by SRB assay, GI50=0.001 μM
HCT116 cells	Proliferation assay	72 h	Antiproliferative activity against human HCT116 cells after 72 hrs by MTS assay, IC50=0.001 μM
HCT15 cells	Proliferation assay	72 h	Antiproliferative activity against human HCT15 cells after 72 hrs by MTS assay, IC50=0.001 μM
HL60 cells	Proliferation assay	72 h	Antiproliferative activity against human HL60 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50=0.001 μM
A10 cells	Growth inhibition assay	48 h	Growth inhibition of rat A10 cells after 48 hrs by MTT assay, IC50=0.001 μM
HUVEC cells	Growth inhibition assay	48 h	Growth inhibition of HUVEC cells after 48 hrs by MTT assay, IC50=0.001 μM
HL60 cells	Cytotoxicity assay	72 h	Cytotoxicity against human HL60 cells after 72 hrs by MTT assay, IC50=0.001 μM
HL60 cells	Proliferation assay	72 h	Antiproliferative activity against human HL60 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50=0.001 μM
NCI-H522 cells	Growth inhibition assay	48 h	Growth inhibition of human NCI-H522 cells after 48 hrs by SRB assay, GI50=0.001 μM
MDA-MB-435 cells	Growth inhibition assay	48 h	Growth inhibition of human MDA-MB-435 cells after 48 hrs by SRB assay, GI50=0.001 μM
OVCAR3	Growth inhibition assay	48 h	Growth inhibition of human OVCAR3 cells after 48 hrs by SRB assay, GI50=0.001 μM
NCI/ADR-RES cells	Growth inhibition assay	48 h	Growth inhibition of human NCI/ADR-RES cells after 48 hrs by SRB assay, GI50=0.001 μM
PC3 cells	Growth inhibition assay	48 h	Growth inhibition of human PC3 cells after 48 hrs by SRB assay, GI50=0.001 μM
DU145 cells	Growth inhibition assay	48 h	Growth inhibition of human DU145 cells after 48 hrs by SRB assay, GI50=0.001 μM
MDA-MB-231 cells	Growth inhibition assay	48 h	Growth inhibition of human MDA-MB-231 cells after 48 hrs by SRB assay, GI50=0.001 μM
CEM cells	Cytotoxicity assay	72 h	Cytotoxicity against human CEM cells after 72 hrs by MTT assay, IC50=0.001 μM
HCT116 cells	Cytotoxicity assay	72 h	Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay, IC50=0.001 μM
MDA-MB-435 cells	Cytotoxicity assay	72 h	Cytotoxicity against human MDA-MB-435 cells after 72 hrs by MTT assay, IC50=0.001 μM
HaCaT cells	Proliferation assay		Antiproliferative activity against human HaCaT cells assessed as cell viability by MTT assay, IC50=0.001 μM
HL60 cells	Proliferation assay	72 h	Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay, IC50=0.001 μM
HL60 cells	Proliferation assay	72 h	Antiproliferative activity against human HL60 cells after 72 hrs by (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide test, IC50=0.001 μM
HT-29	Growth inhibition assay		Growth inhibition of human HT-29 cells by MTT assay, IC50=0.001 μM
HL60 cells	Proliferation assay	72 h	Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay, IC50=0.001 μM
Hs578T cells	Growth inhibition assay	48 h	Growth inhibition of human Hs578T cells after 48 hrs by SRB assay, GI50=0.001 μM
HL60 cells	Cytotoxicity assay	72 h	Cytotoxicity against human HL60 cells after 72 hrs by MTT assay, IC50=0.001 μM
SKOV3 cells	Growth inhibition assay		Growth inhibition of human SKOV3 cells by MTT assay, IC50=0.001 μM
MDA-MB-468 cells	Cytotoxicity assay	4 days	Cytotoxicity against human MDA-MB-468 cells assessed as cell viability after 4 days by MTS assay, IC50=0.0011 μM
MCF7 cells	Proliferation assay	72 h	Antiproliferative activity in human MCF7 cells assessed as cell viability after 72 hrs by MTT assay, IC50=0.00111 μM
H460	Cytotoxicity assay		Cytotoxicity against human H460 cells by sulforhodamine B test, IC50=0.0012 μM
H460	Proliferation assay		Antiproliferative activity against human H460 cells, IC50=0.00124 μM
NCI-H460 cells	Cytotoxicity assay	72 h	Cytotoxic activity against human NCI-H460 cells after 72 hrs by sulforhodamine B test, IC50=0.0013 μM
OVCAR8 cells	Growth inhibition assay	96 h	Growth inhibition of human OVCAR8 cells overexpressing P-glycoprotein after 96 hrs, IC50=0.0013 μM
NCI/ADR-RES cells	Cytotoxicity assay		Cytotoxicity against human NCI/ADR-RES cells assessed as growth inhibition by trypan blue exclusion assay, IC50=0.0013 μM
OVCAR8 cells	Cytotoxicity assay	96 h	Cytotoxicity against human OVCAR8 cells assessed as growth inhibition after 96 hrs by Giemsa staining-based light microscopy, IC50=0.0013 μM
NCI/ADR-RES cells	Cytotoxicity assay	96 h	Cytotoxicity against human NCI/ADR-RES cells assessed as growth inhibition after 96 hrs by Giemsa staining-based light microscopy, IC50=0.0013 μM
OVCAR8 cells	Cytotoxicity assay		Cytotoxicity against human OVCAR8 cells assessed as growth inhibition by trypan blue exclusion assay, IC50=0.0013 μM
HuTu 80 cells	Proliferation assay	72 h	Antiproliferative activity in human HuTu 80 cells assessed as cell viability after 72 hrs by MTT assay, IC50=0.00137 μM
K562 cells	Cytotoxicity assay		Cytotoxicity against human K562 cells, IC50=0.0014 μM
NCI/ADR (MDR) cells	Function assay		Cell cycle arrest in NCI/ADR (MDR) cells by accumulation at G2/M phase, IC50=0.0015 μM
HUVEC	Proliferation assay		Antiproliferative activity against human HUVEC, IC50=0.0015 μM
KB cell	Proliferation assay		Antiproliferative activity against human KB cell line by methylene blue dye assay, IC50=0.0015 μM
KB-VIN10 cell	Proliferation assay		Antiproliferative activity against human KB-VIN10 cell line by methylene blue dye assay, IC50=0.0015 μM
Human SH-SY5Y neuroblastoma cells	Function assay		Inhibitory concentration against Human SH-SY5Y neuroblastoma cells, IC50=0.0015 μM
SW620 cells	Proliferation assay	72 h	Antiproliferative activity in human SW620 cells assessed as cell viability after 72 hrs by MTT assay, IC50=0.00152 μM
Molt4/C8 cells	Proliferation assay		Antiproliferative activity against human Molt4/C8 cells, IC50=0.0016 μM
ACHN cell	Proliferation assay		Antiproliferative activity against drug resistant ACHN cell line expressing MDR1 by Alamar Blue assay, IC50=0.0016 μM
Molt4/C8 cells	Proliferation assay	3 days	Antiproliferative effect against human Molt4/C8 cells after 3 days, IC50=0.0016 μM
클릭하여 더 많은 세포주 실험 데이터 보기

화학 정보, 보관 및 안정성

분자량	316.35	화학식	C₁₈H₂₀O₅	보관 (수령일로부터)	3년-20°C분말
CAS 번호	117048-59-6	SDF 다운로드		원액 보관	1년-80°C용매에 보관 1개월-20°C용매에 보관
동의어	N/A			Smiles	COC1=C(C=C(C=C1)C=CC2=CC(=C(C(=C2)OC)OC)OC)O

용해도

In vitro
배치:

DMSO : 63 mg/mL (199.14 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : 34 mg/mL

Water : 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.

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

Targets/IC₅₀/Ki	β-tubulin 0.4 μM(Kd)
시험관 내(In vitro)	Combretastatin A4는 MDA-MB-231, A549, Hela, HL-60, SF295, HCT-8, MDA-MB435, PC3M, OVCAR-8, NCI-H358M 및 림프구 세포의 성장을 각각 2.8, 3.8, 0.9, 2.1, 6.2, 5.3, 7.9, 4.7, 0.37, 8 및 3.2 nM의 IC50으로 억제합니다. 이 화합물 1 μM은 튜불린 중합을 35% 억제하며, 10 μM은 튜불린 중합을 거의 완전히 차단합니다. 이 화학 물질은 콜히친 결합의 78%에 달하는 높은 상대 결합 능력을 보여줍니다.
키나아제 분석	LC-MS/MS를 이용한 경쟁 결합 분석
키나아제 분석	콜히친 (1.2 μM)은 튜불린 (1.3 mg/mL)과 함께 배양 완충액 (80 mM PIPES, 2.0 mM MgCl2, 0.5 mM EGTA, pH 6.9)에서 37℃로 1시간 동안 배양됩니다. 다양한 농도 (0.1 – 125 μM)의 이 화합물을 사용하여 원래 튜불린에 결합된 콜히친과 경쟁합니다. 배양 후, 여과액을 얻습니다. 아날로그가 콜히친 결합을 억제하는 능력은 경쟁자가 없는 상태에서의 대조군 결합의 백분율로 표현됩니다.
생체 내(In vivo)	NT2 및 MDA-MB-231 유방암 모델에서 Combretastatin A4 (100 mg/kg, i.p.) 투여는 지질 R1의 유의미한 감소와 전자 상자성 공명 (EPR) 산소 측정법으로 측정한 종양 pO2의 감소를 유도합니다. 이 화합물 (100 mg/kg, i.p.)은 수컷 NMRI 마우스에서 K^trans를 유의미하게 감소시킵니다.
참조	[1] https://pubmed.ncbi.nlm.nih.gov/24669888/ [2] https://pubmed.ncbi.nlm.nih.gov/25765253/ [3] https://pubmed.ncbi.nlm.nih.gov/25323069/

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자주 묻는 질문

질문 1:
How to make solution for in vivo IP injection of it?

답변:
We've tested some vehicles for this compound, and found it can be dissolved in 5% DMSO+50% PEG 300+ddH2O at 30mg/ml clearly. When prepare the solution, please dissolve it in DMSO clearly first. Then add PEG, after they mixed well, then dilute with water.

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):