Name: FK866 (Daporinad)
Brand: Selleck Chemicals
SKU: S2799
Rating: 5 (70 reviews)

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품질 관리

배치: 순도: 99.99%

99.99

함께 자주 사용되는 제품 FK866 (Daporinad)

Padnarsertib (KPT-9274, ATG-019)

It and KPT 9274 are NMPT inhibitors and can strongly decrease total NAD+ levels and mitochondrial respiration in M2 macrophages.

GMX1778

It and GMX1778 are iNAMPT enzymatic inhibitors that have been developed as anti-cancer treatment options.

관련 타겟	Dehydrogenase HSP P450 (e.g. CYP17) PDE phosphatase PPAR Vitamin Carbohydrate Metabolism Mitochondrial Metabolism Drug Metabolite
기타 Transferase 억제제	Tunicamycin Ezatiostat AOA (Aminooxyacetic acid) hemihydrochloride GGTI 298 TFA salt OSMI-4 2-Bromohexadecanoic acid (2-BP) A-922500 (DGAT-1 Inhibitor 4a) PF-04620110 OSMI-1 ERG240

세포 배양, 처리 및 작업 농도

세포주	분석 유형	농도	배양 시간	활성 설명	PMID
SH-SY5Y	Cytotoxicity assay			Cytotoxicity against human SH-SY5Y cells assessed as reduction of total cellular NAD(P) level, IC50 = 0.0005 μM.	19961183
SH-SY5Y	Cytotoxicity assay		48 hrs	Cytotoxicity against human SH-SY5Y cells assessed as cell viability after 48 hrs by MTT assay, IC50 = 0.0017 μM.	19961183
HT1080	Cytotoxicity assay		6 days	Cytotoxicity against human HT1080 cells after 6 days by SRB assay, IC50 = 0.16 μM.	21330015
A549	Cytotoxicity assay		6 days	Cytotoxicity against human A549 cells after 6 days by SRB assay, IC50 = 0.16 μM.	21330015
HCT116	Cytotoxicity assay		6 days	Cytotoxicity against human HCT116 cells after 6 days by SRB assay, IC50 = 0.16 μM.	21330015
SNU638	Cytotoxicity assay		6 days	Cytotoxicity against human SNU638 cells after 6 days by SRB assay, IC50 = 0.16 μM.	21330015
MCF7	Antitumor assay	10 uM	6 days	Antitumor activity against human MCF7 cells at 10 uM after 6 days by SRB assay, IC50 = 0.68 μM.	21330015
K562	Cytotoxicity assay		6 days	Cytotoxicity against human K562 cells after 6 days by SRB assay, IC50 = 20 μM.	21330015
A2780	Cytotoxicity assay		72 hrs	Cytotoxicity against human A2780 cells after 72 hrs by SRB assay, IC50 = 0.001 μM.	23617784
NYH	Cytotoxicity assay		3 weeks	Cytotoxicity against human NYH cells after 3 weeks by clonogenic survival assay, LD50 = 0.0015 μM.	23679915
K562	Cytotoxicity assay		96 hrs	Cytotoxicity against human K562 cells after 96 hrs by MTT assay, IC50 = 0.0072 μM.	23679915
A2780	Antiproliferative assay		72 hrs	Antiproliferative activity against human A2780 cells assessed as growth inhibition after 72 hrs by SRB-based microplate reader analysis, IC50 = 0.001 μM.	23859118
NYH	Cytotoxicity assay			Cytotoxicity against human NYH cells by clonogenic assay, IC50 = 0.0015 μM.	24164086
A2780	Cytotoxicity assay		72 hrs	Cytotoxicity against human A2780 cells assessed as growth inhibition after 72 hrs by WST-1 assay, IC50 = 0.0016 μM.	24164086
HepG2	Function assay		1 hr	Inhibition of NAMPT in human HepG2 cells using [14C]-nicotinamide/PRPP as substrate assessed as formation of [14C]-nicotinamide mononucleotide after 1 hr by liquid scintillation counting analysis, IC50 = 0.0022 μM.	24164086
PC3	Cytotoxicity assay			Cytotoxicity against human PC3 cells by clonogenic assay, IC50 = 0.0038 μM.	24164086
A2780	Cytotoxicity assay			Cytotoxicity against human A2780 cells by clonogenic assay, IC50 = 0.0057 μM.	24164086
A431	Cytotoxicity assay			Cytotoxicity against human A431 cells by clonogenic assay, IC50 = 0.0061 μM.	24164086
MCF-7	Cytotoxicity assay		72 hrs	Cytotoxicity against human MCF-7 cells assessed as growth inhibition after 72 hrs by WST-1 assay, IC50 = 0.0074 μM.	24164086
MCF7	Cytotoxicity assay			Cytotoxicity against human MCF7 cells by clonogenic assay, IC50 = 0.0084 μM.	24164086
HCT116	Cytotoxicity assay		72 hrs	Cytotoxicity against human HCT116 cells assessed as growth inhibition after 72 hrs by WST-1 assay, IC50 = 0.0109 μM.	24164086
SKOV3	Cytotoxicity assay			Cytotoxicity against human SKOV3 cells by clonogenic assay, IC50 = 0.211 μM.	24164086
HCT116	Cytotoxicity assay		72 hrs	Cytotoxicity against APO866-resistant human HCT116 cells assessed as growth inhibition after 72 hrs by WST-1 assay, IC50 = 0.946 μM.	24164086
A2780	Antiproliferative assay		72 hrs	Antiproliferative activity against human A2780 cells after 72 hrs by sulforhodamine B assay, IC50 = 0.001 μM.	24405419
A2780	Function assay		72 hrs	Inhibition of NAMPT in human A2780 cells assessed as decrease in cell viability after 72 hrs by SRB assay, IC50 = 0.001 μM.	27541271
DE3	Function assay		15 mins	Inhibition of human full length C-terminal His6-tagged NAMPT expressed in Escherichia coli Rosetta (DE3) cells using nicotinamide as substrate incubated for 15 mins prior to substrate addition measured after 30 mins in presence of PRPP, IC50 = 0.003 μM.	27541271
SH-SY5Y	Cytotoxicity assay		56 hrs	Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability after 56 hrs by MTT assay, EC50 = 0.0034 μM.	28165742
A2780	Cytotoxicity assay			Cytotoxicity against human A2780 cells assessed as reduction in cell viability, IC50 = 0.0042 μM.	28165742
PC3	Antiproliferative assay		5 days	Antiproliferative activity against human PC3 cells assessed as reduction in cell viability incubated for 5 days by Cell-titer Glo reagent based assay, IC50 = 0.0057 μM.	28610984
HepG2	Cytotoxicity assay		72 hrs	Cytotoxicity in human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50 = 0.89 μM.	28885834
MDA-MB-231	Cytotoxicity assay		72 hrs	Cytotoxicity in human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50 = 1.3 μM.	28885834
HCT116	Cytotoxicity assay		72 hrs	Cytotoxicity in human HCT116 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50 = 1.6 μM.	28885834
HepG2	Cytotoxicity assay		72 hrs	Cytotoxicity against human HepG2 cells assessed as inhibition of cell growth after 72 hrs by MTT assay, IC50 = 0.89 μM.	29348808
HCT116	Cytotoxicity assay		72 hrs	Cytotoxicity against human HCT116 cells assessed as inhibition of cell growth after 72 hrs by MTT assay, IC50 = 1.6 μM.	29348808
A549	Cytotoxicity assay		72 hrs	Cytotoxicity against human A549 cells assessed as inhibition of cell growth after 72 hrs by MTT assay, IC50 = 3.7 μM.	29348808
SH-SY5Y	Autophagy assay		40 hrs	Induction of autophagy in human SH-SY5Y cells assessed as LC3/phosphotidylethanolamine coupling after 40 hrs by Western blot analysis	19961183
MCF7	Antitumor assay		6 days	Antitumor activity against human MCF7 cells after 6 days by SRB assay	21330015
MDCK	Function assay	10 uM		Apparent permeability across apical to basolateral side in dog MDCK cells at 10 uM by LC-MS/MS analysis	23859118
DU145	Cytotoxicity assay			Cytotoxicity against human DU145 cells by clonogenic assay	24164086
MCF7	Cytotoxicity assay		96 hrs	Cytotoxicity against human MCF7 cells after 96 hrs by clonogenic assay	24164086
HCT116	Function assay			Resistance factor, ratio of IC50 for APO866-resistant human HCT116 cells to IC50 for human HCT116 cells	24164086
A2780	Antiproliferative assay		72 hrs	Antiproliferative activity against human A2780 cells after 72 hrs by sulforhodamine B assay in presence of nicotinamide mononucleotide	24405419
Sf9	Function assay		30 mins	Inhibition of recombinant full length human C-terminal His/flag-tagged HDAC1 expressed in baculovirus infected Sf9 insect cells after 30 mins by fluorescence assay	29348808
클릭하여 더 많은 세포주 실험 데이터 보기

화학 정보, 보관 및 안정성

분자량	391.51	화학식	C₂₄H₂₉N₃O₂	보관 (수령일로부터)	3년-20°C분말
CAS 번호	658084-64-1	SDF 다운로드		원액 보관	1년-80°C용매에 보관 1개월-20°C용매에 보관
동의어	APO866			Smiles	C1CN(CCC1CCCCNC(=O)C=CC2=CN=CC=C2)C(=O)C3=CC=CC=C3

용해도

In vitro
배치:

DMSO : 78 mg/mL (199.22 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : 78 mg/mL

Water : Insoluble

DMSO : 78 mg/mL (199.22 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : 78 mg/mL

Water : Insoluble

DMSO : 80 mg/mL (204.33 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : 78 mg/mL

Water : Insoluble

Ethanol : 78 mg/mL

DMSO : Insoluble
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

DMSO : 78 mg/mL (199.22 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : 78 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.
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.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Selleck 연구소에서 검증되었습니다. 이 제형에 대한 조정이 필요한 경우 맞춤 테스트를 위해 당사 영업팀에 문의하십시오.	4.000mg/ml (10.22mM)	Taking the 1 mL working solution as an example, add 50 μL of 80 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O 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

Targets/IC₅₀/Ki	NMPRTase (Cell-free assay) 0.4 nM(Ki)
시험관 내(In vitro)	FK866 (Daporinad)는 0.09-27 nM 범위의 낮은 농도에서 급성 골수성 백혈병 [AML], 급성 림프모구성 백혈병 [ALL], 맨틀 세포 림프종 [MCL], 만성 림프구성 백혈병 [CLL] 및 T-세포 림프종을 포함한 41가지 혈액 악성 세포에서 용량 의존적 세포 독성을 유도합니다. 0-10 nM 범위의 농도에서 이 화합물은 세포 사멸을 유도하는데, 이는 카스파제 활성화와는 무관하지만 미토콘드리아 막의 탈분극과 관련이 있습니다. 또한 0-10 nM 범위의 농도에서 다양한 혈액암 세포에서 세포내 NAD 및 ATP 함량 고갈과 세포 사멸을 용량 의존적으로 유도합니다. 10 nM 농도에서 HFFF2 세포에서 PBEF 유도 MMP-3, CCL2 및 CXCL8 분비를 억제합니다.
생체 내(In vivo)	FK866 (Daporinad)를 인간 AML, 림프모구성 림프종 및 백혈병의 C.B.-17 SCID 마우스 이종이식 모델에서 20 mg/kg 용량으로 4일간 하루 두 번 복강 내 투여하고 3주 동안 매주 반복하면 종양 성장을 예방하고 소멸시킵니다. 0.12 mg/kg/시간 용량에서 이 화합물은 CIA가 있는 마우스에서 PBEF 억제를 통해 관절 파괴 및 백혈구 침윤을 예방합니다. }
참조	[1] https://pubmed.ncbi.nlm.nih.gov/19196867/ [2] https://pubmed.ncbi.nlm.nih.gov/21400478/ [3] https://pubmed.ncbi.nlm.nih.gov/20515945/ [4] https://pubmed.ncbi.nlm.nih.gov/20696207/ [5] https://pubmed.ncbi.nlm.nih.gov/14612543/

적용 분야

방법	바이오마커	PMID
Western blot	SIRT1 p-AMPK / AMPK / p-EIF2A / EIF2A / p-4EBP1 / 4EBP1 AKT / pAKT(Ser-473) / mTOR / p-mTOR(Ser-2448)	29905535
Immunofluorescence	pMLKL phGSK3β ph-β-catenin	29996103
Growth inhibition assay	Cell viability	27462772

임상시험 정보

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

NCT 번호	모집	조건	스폰서/협력자	시작일	단계
NCT00435084	Completed	B-cell Chronic Lymphocytic Leukemia	Valerio Therapeutics	February 2007	Phase 1\|Phase 2

기술 지원

취급 설명서

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자주 묻는 질문

질문 1:
We are considering the use of it for in vivo injections. Any suggestions for the formula?

답변:
The recommended vehicle for in vivo study of this compound is 45% Propylene glycol (dissolve first) +5% Tween 80+ddH2O. It can be dissolved in Propylene glycol first and then diluted with water containing Tween 80. The solution is clear and suitable for injection.

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):

FK866 (Daporinad) NAMPT 저해제

화학 구조

분자량: 391.51

품질 관리

함께 자주 사용되는 제품 FK866 (Daporinad)

세포 배양, 처리 및 작업 농도

화학 정보, 보관 및 안정성

용해도

몰농도 계산기

생체 내 제형 계산기 (투명한 용액)

작용 메커니즘

적용 분야

임상시험 정보

기술 지원

자주 묻는 질문