Name: ABT-751 (E7010)
Brand: Selleck Chemicals
SKU: S1165
Rating: 5 (5 reviews)

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품질 관리

배치: S116501 DMSO]74 mg/mL]false]Ethanol]12 mg/mL]false]Water]Insoluble]false 순도: 99.95%

최고 수준의 품질로 Nature Medicine에 인용됨
COA
NMR
SDS
데이터시트

99.95

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 Combretastatin A4 Epothilone A TAI-1 Cucurbitacin B INH1

세포 배양, 처리 및 작업 농도

세포주	분석 유형	농도	배양 시간	활성 설명
HCT-15 cell	Proliferation assay			Antiproliferative activity against human colon carcinoma HCT-15 cell line(MDR(-)), IC50=0.34 μM
HCT116-C9 cell	Function assay			Effective concentration to inhibit cell proliferation by 50% relative to untreated control cell after 72 hr of continuous exposure in HCT116-C9 cell line, IC50=0.9 μM
NCI-H460 cell	Proliferation assay			Antiproliferative activity against human lung carcinoma NCI-H460 cell line (MDR(+)), IC50=0.35 μM
P388 cell line	Function assay		72 h	Effective concentration to inhibit cell proliferation by 50% relative to untreated control cell after 72 hr of continuous exposure in P388 cell line， IC50=0.19 μM
P388/4.0 r-M cell line	Function assay		72 h	Effective concentration to inhibit cell proliferation by 50% relative to untreated control cell after 72 hr of continuous exposure in P388/4.0 r-M cell line, IC50=15 μM
human HL60 cells	Proliferation assay			Antiproliferative activity against human HL60 cells, IC50=0.34 μM
HeLa cells	Cytotoxicity assay		48-72 h	Cytotoxicity against human HeLa cells after 48 to 72 hrs by WAT-1 assay, IC50=0.27 μM
MDR1 cells	Cytotoxicity assay		48-72 h	Cytotoxicity against human NCI-ADR-RES expressing MDR1 cells after 48 to 72 hrs by WAT-1 assay, IC50=0.29 μM
Jurkat cells	Function assay		24 h	Cell cycle arrest in human Jurkat cells assessed as accumulation at G2/M phase after 24 hrs using propidium iodide staining by FACS analysis, IC50=0.16 μM
SW620 cells	Cytotoxicity assay		48-72 h	Cytotoxicity against human SW620 cells after 48 to 72 hrs by WAT-1 assay, IC50=0.19 μM
A2780 cells	Cytotoxicity assay		48-72 h	Cytotoxicity against human A2780 cells after 48 to 72 hrs by WAT-1 assay, IC50=0.17 μM
HT-29 cells	Proliferation assay		72 h	Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay, IC50=0.21 μM
HUVEC	Function assay	100-1000 nM	4 h	Induction of vascular disrupting activity in HUVEC assessed as VEGF-induced tube formation at 100 to 1000 nM after 4 hrs by microscopic analysis
H460 cells	Cytotoxicity assay		72 h	Cytotoxicity against human H460 cells assessed as growth inhibition after 72 hrs by methylene blue staining-based assay, IC50=0.2177 μM
MKN45 cells	Cytotoxicity assay		72 h	Cytotoxicity against human MKN45 cells assessed as growth inhibition after 72 hrs by methylene blue staining-based assay, IC50=0.166 μM
HT-29 cells	Cytotoxicity assay		72 h	Cytotoxicity against human HT-29 cells assessed as growth inhibition after 72 hrs by methylene blue staining-based assay, IC50=0.3387 μM
human A549 cells	Cytotoxicity assay		48 h	Cytotoxicity against human A549 cells after 48 hrs by MTT assay, IC50=1.31 μM
ACHN cells	Cytotoxicity assay		48 h	Cytotoxicity against human ACHN cells after 48 hrs by MTT assay, IC50=2.13 μM
MCF7 cells	Cytotoxicity assay		48 h	Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay, IC50=1.25 μM
HT-29 cells	Cytotoxicity assay		48 h	Cytotoxicity against human HT-29 cells after 48 hrs by MTT assay, IC50=1.62 μM
A549 cells	Proliferation assay		24 h	Antiproliferative activity against human A549 cells assessed as growth inhibition after 24 hrs by SRB assay, GI50=1.31 μM
human MCF7 cells	Proliferation assay		24 h	Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 24 hrs by SRB assay, GI50=1.25 μM
KB-S15 cells	Cytotoxicity assay		72 h	Cytotoxicity against human KB-S15 cells overexpressing P-gp170/MDR assessed as growth inhibition after 72 hrs by methylene blue staining-based assay, IC50=0.206 μM
KB-7d cells	Cytotoxicity assay		72 h	Cytotoxicity against human KB-7d cells overexpressing MRP assessed as growth inhibition after 72 hrs by methylene blue staining-based assay, IC50=0.205 μM
KB-VIN10 cells	Cytotoxicity assay		72 h	Cytotoxicity against human KB-VIN10 cells overexpressing P-gp170/MDR assessed as growth inhibition after 72 hrs by methylene blue staining-based assay, IC50=0.227 μM
human PC3 cells	Cytotoxicity assay		48 h	Cytotoxicity against human PC3 cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay, GI50=0.62 μM
human AsPC1 cells	Cytotoxicity assay		48 h	Cytotoxicity against human AsPC1 cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay, GI50=4.11 μM
human A549 cells	Cytotoxicity assay		48 h	Cytotoxicity against human A549 cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay, GI50=5.33 μM
Hep3B cells	Cytotoxicity assay		48 h	Cytotoxicity against human Hep3B cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay, GI50=0.84 μM
KB cells	Cytotoxicity assay		72 h	Cytotoxicity against human KB cells assessed as growth inhibition after 72 hrs by methylene blue staining-based assay, IC50=0.2513 μM
DU145 cells	Proliferation assay		24 h	Antiproliferative activity against human DU145 cells assessed as growth inhibition after 24 hrs by SRB assay, GI50=1.81 μM
DU145 cells	Cytotoxicity assay		48 h	Cytotoxicity against human DU145 cells after 48 hrs by MTT assay， GI50=1.81 μM
human SKBR3 cells	Growth inhibition assay		48 h	Growth inhibition of human SKBR3 cells after 48 hrs by MTT assay, IC50=0.74 μM
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화학 정보, 보관 및 안정성

분자량	371.41	화학식	C₁₈H₁₇N₃O₄S	보관 (수령일로부터)	3년-20°C분말
CAS 번호	141430-65-1	SDF 다운로드		원액 보관	1년-80°C용매에 보관 1개월-20°C용매에 보관
동의어	N/A			Smiles	COC1=CC=C(C=C1)S(=O)(=O)NC2=C(N=CC=C2)NC3=CC=C(C=C3)O

용해도

In vitro
배치:

DMSO : 74 mg/mL (199.24 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : 12 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.
Clear solution	30%propylene glycol 1 5%Tween80 2 65%D5W Selleck 연구소에서 검증되었습니다. 이 제형에 대한 조정이 필요한 경우 맞춤 테스트를 위해 당사 영업팀에 문의하십시오.	15.000mg/ml (40.39mM)	Taking the 1 mL working solution as an example, add 300 μL of 50 mg/ml clarified propylene glycol stock solution to 50 μL of Tween 80, mix evenly to clarify it; then continue to add 650 μL of D5W to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

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

특징	An orally bioavailable tubulin-binding and antimitotic sulfonamide.
Targets/IC₅₀/Ki	Microtubules
시험관 내(In vitro)	생체 외에서 ABT-751 (E7010)은 신경모세포종에서 0.6–2.6 μM, 다른 고형암 세포주에서 0.7–4.6 μM의 IC50 값을 가진 선택적 세포독성을 보입니다. 또한, 동적 미세소관에 선택적인 영향을 미치고 안정적인 미세소관은 보존하며, 이는 IC90 농도에서 아세틸화되고 탈티로신화된 α-튜불린 양성 중합 미세소관의 지속성을 설명합니다.
생체 내(In vivo)	이 Calu-6 이종이식 모델에서 ABT-751 (E7010)은 100 및 75 mg/kg/day의 단일 약제로 유의미한 항종양 활성을 보였으며, 시스플라틴과 병용 시 용량 의존적인 성장 지연 증가를 보였습니다. HT-29 결장 이종이식 모델에서 이 화합물은 단일 약제로도 유의미한 항종양 활성을 보였고, 5-FU와 병용 시 용량 의존적인 성장 지연 증가를 나타냈습니다. 림프종을 앓는 개에서 구토, 설사, 식욕 부진 또는 이들의 조합을 포함하는 용량 제한 독성을 보였으며, 최대 내약 용량 (MTD)은 350 mg/m² PO q24h였습니다. 또한, MTD 350 mg/m²에서 ABT-751의 평균 AUC 및 C_max는 각각 5.55 μg-시간/mL 및 0.9 μg/mL였습니다.
참조	[1] https://pubmed.ncbi.nlm.nih.gov/19731320/ [2] https://pubmed.ncbi.nlm.nih.gov/16967299/ [3] https://pubmed.ncbi.nlm.nih.gov/22369215/

임상시험 정보

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

NCT 번호	모집	조건	스폰서/협력자	시작일	단계
NCT00436852	Completed	Disseminated Neuroblastoma\|Recurrent Neuroblastoma	Children''s Oncology Group\|National Cancer Institute (NCI)	January 2007	Phase 2
NCT00735878	Terminated	Non Small Cell Lung Cancer\|Lung Cancer	Konstantin Dragnev\|Abbott\|Dartmouth-Hitchcock Medical Center	September 2004	Phase 1\|Phase 2

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ABT-751 (E7010) Microtubule Associated 억제제

화학 구조

분자량: 371.41