Lonafarnib (SCH66336)

目錄號：S2797 Purity: 99.48%

Lonafarnib (SCH66336) 是一種口服生物有效的FPTase抑制劑，作用于H-ras，K-ras-4B和N-ras，無細胞試驗中IC50分別為1.9 nM， 5.2 nM和2.8 nM。Phase 3。

Lonafarnib (SCH66336) Chemical Structure

CAS: 193275-84-2

規(guī)格	價格	庫存
10mM (1mL in DMSO)	1695.33	現(xiàn)貨
5mg	1416.91	現(xiàn)貨
10mg	2229.57	現(xiàn)貨
25mg	4250.61	現(xiàn)貨
100mg	10622.43	現(xiàn)貨
1g	53153.1	現(xiàn)貨
更大包裝有超大折扣
400-668-6834 [email protected]

產(chǎn)品質(zhì)控

批次：純度： 99.48%

99.48

Lonafarnib (SCH66336)相關(guān)產(chǎn)品

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細胞實驗數(shù)據(jù)示例

細胞系	實驗類型	孵育時間	活性描述	文獻信息(PMID)
Caco-2	Cytotoxicity assay	48 hours	Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging, IC50 = 5.68 μM.	ChEMBL
Caco-2	Toxicity assay	48 hours	Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay, CC50 = 10.71 μM.	ChEMBL
NIH-H tumor cell lines	Growth inhibition assay		Compound ability to inhibit anchorage-independent growth of NIH-H tumor cell lines in soft agar, IC50=0.072 μM	9822558
HCT116	Growth inhibition assay		Compound was measured for inhibition of HCT116 tumor cell line in colon under soft agar assay, IC50=0.07 μM	9822558
MCF-7 tumor cell line	Growth inhibition assay		Compound was measured for inhibition of MCF-7 tumor cell line in breast under soft agar assay, IC50=0.05 μM	9822558
COS-7 monkey cells	Function assay		Inhibiting the farnesylation of H-ras proteins in COS-7 monkey cells transiently expressing H-ras[Val12]-CVLS in the whole cell assay, IC50=0.01 μM	9822558
Cos-1 monkey kidney cells	Function assay		Inhibition of Protein farnesyltransferase in Cos-1 monkey kidney cells expressing H-Ras-val, IC50=0.0019 μM	12190309
NIH3T3 cells	Function assay		Inhibition of Ras farnesylation in H-Ras transformed NIH3T3 cells, EC50=0.1 μM	15454228
NIH-K tumor cell lines	Growth inhibition assay		Compound ability to inhibit anchorage-independent growth of NIH-K tumor cell lines in soft agar, IC50=0.5 μM	9822558
Cos-1	Function assay		Inhibition of Protein farnesyltransferase in Cos-1 monkey kidney cells expressing H-Ras-val, IC50 = 0.0019 μM.	12190309
Cos-1	Function assay		Effect on Ras processing in Cos-1 monkey kidney cells expressing either H-Ras-Val 12-CVLS or H-Ras-Val12, IC50 = 0.01 μM.	10411485
COS7	Function assay		Inhibition of FTase in human COS7 cells, IC50 = 0.01 μM.	20925433
H-Ras transformed cells	Function assay		Inhibition of soft agar colony formation in H-Ras transformed cells, IC50 = 0.07 μM.	15501065
NIH3T3	Function assay		Effective concentration against Ha-RAS processing in NIH3T3 ras-transformed cells, EC50 = 0.16 μM.	12657284
NIH3T3	Function assay		TP_TRANSPORTER: inhibition of DNR efflux (DNR: ? uM) in MDR1-expressing NIH3T3 cells, IC50 = 2.7 μM.	11606389
A673	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
DAOY	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	29435139
Saos-2	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	29435139
BT-37	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	29435139
RD	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	29435139
BT-12	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells	29435139
MG 63 (6-TG R)	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells	29435139
NB1643	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	29435139
OHS-50	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	29435139
Rh41	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells	29435139
SJ-GBM2	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	29435139
SK-N-MC	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
NB-EBc1	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	29435139
LAN-5	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	29435139
點擊查看更多細胞系數(shù)據(jù)

生物活性

產(chǎn)品描述

Lonafarnib (SCH66336) 是一種口服生物有效的FPTase抑制劑，作用于H-ras，K-ras-4B和N-ras，無細胞試驗中IC50分別為1.9 nM， 5.2 nM和2.8 nM。Phase 3。

靶點

H-ras ^[1] (Cell-free assay)	N-ras ^[1] (Cell-free assay)	K-ras-4B ^[1] (Cell-free assay)
1.9 nM	2.8 nM	5.2 nM

體外研究(In Vitro)
體外研究活性	SCH66336在0.1 μM到8 μM濃度范圍均可抑制頭部和頸部鱗狀細胞癌(HNSCC) 生長和誘導(dǎo)凋亡，抑制效果具有劑量和時間依賴性。SCH66336 (8 μM)可在SqCC/Y1細胞中抑制蛋白激酶B/Akt活性和磷酸化 Akt蛋白底物糖原合酶激酶（GSK）- 3β，轉(zhuǎn)錄叉因子和BAD^[2]。SCH66336 對多細胞系有抗增殖作用，IC 50范圍從0.6 μM 到32.3 μM ^[3] ; Lonafarnib誘導(dǎo)CCAAT /增強子結(jié)合蛋白同源蛋白（CHOP）依賴性DR5啟動子的轉(zhuǎn)錄激活，從而誘導(dǎo)CHOP依賴性的DR5上調(diào)。Lonafarnib (< 10 μM) 可激活caspase - 8及其下游的半胱氨酸蛋白酶，從而誘導(dǎo)H1792細胞凋亡。Lonafarnib (5 μM)可增加DR5的細胞表面分布，增強腫瘤壞死因子相關(guān)凋亡誘導(dǎo)配體誘導(dǎo)的H1792細胞凋亡^[4]。
細胞實驗	細胞系	UMSCC10B, UMSCC14B, UMSCC17B, UMSCC22B, 和UMSCC35, UMSCC38 細胞
	濃度	0.1 μM - 8 μM
	孵育時間	24 小時
	方法	細胞鋪板于96孔板中，后續(xù)培養(yǎng)5天，據(jù)此確定起始密度。24小時后，用不同濃度SCH66336處理細胞。SCH66336溶解于DMSO。對照組細胞用同樣量的DMSO處理。5天后用SRB法檢測細胞數(shù)量。生長抑制的百分比的計算公式為：增長抑制百分比=（1?/At/Ac）×100，At和Ac分別代表實驗組和對照組的吸收值。IC 50值由劑量反應(yīng)曲線確定。
實驗圖片	檢測方法	檢測指標	實驗圖片	PMID
	Western blot	p-ERK / p-SAPK / p-JNK PARP / cleaved-PARP / pro-caspase3 / cleaved-caspase3 / Bcl-2 Cyclin D / CDK6 / CDK4 / SKP2 LC3A / LC3B		29285232
	Growth inhibition assay	Cell number Cell viability		29069775

體內(nèi)研究(In Vivo)
體內(nèi)研究活性	SCH66336 抑制HTBI77人肺癌裸鼠移植模型中的瘤生長，抑制作用呈劑量依賴性^[1]。在NOD/SCID免疫缺陷小鼠皮下注射XEN01, XEN05或XEN08 GBM建立腫瘤移植模型，SCH66336 以 50 mg/kg劑量口服灌胃21天后，可抑制腫瘤生長，抑制率高達69%^[3]。
動物實驗	Animal Models	6–12周齡NOD/SCID 小鼠
	Dosages	50 mg/kg
	Administration	口服

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試驗信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT05953545	Not yet recruiting	Chronic Hepatitis Delta	National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)\|National Institutes of Health Clinical Center (CC)	May 15 2024	Phase 2
NCT02579044	Enrolling by invitation	Progeria	Boston Children''s Hospital	December 2015	Phase 1\|Phase 2
NCT02430181	Completed	Chronic Hepatitis D Infection	Eiger BioPharmaceuticals	November 2014	Phase 2
NCT01495585	Completed	Hepatitis D	National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)\|National Institutes of Health Clinical Center (CC)	December 2011	Phase 2
NCT01232881	Terminated	Breast Cancer	Hoosier Cancer Research Network\|United States Department of Defense\|Indiana University School of Medicine\|Emory University	August 2009	--
NCT00916747	Active not recruiting	Progeria	Boston Children''s Hospital\|Schering-Plough\|Merck Sharp & Dohme LLC\|Eiger BioPharmaceuticals	August 2009	Phase 2

參考文獻
https://pubmed.ncbi.nlm.nih.gov/9810004/ https://pubmed.ncbi.nlm.nih.gov/12941797/ https://pubmed.ncbi.nlm.nih.gov/11389071/ https://pubmed.ncbi.nlm.nih.gov/17493934/ + 展開

參考文獻

https://pubmed.ncbi.nlm.nih.gov/9810004/
https://pubmed.ncbi.nlm.nih.gov/12941797/
https://pubmed.ncbi.nlm.nih.gov/11389071/

https://pubmed.ncbi.nlm.nih.gov/17493934/

+ 展開

化學(xué)信息&溶解度

分子量	638.82	分子式	C₂₇H₃₁Br₂ClN₄O₂
CAS號	193275-84-2	SDF	Download Lonafarnib (SCH66336) SDF
Smiles	C1CN(CCC1CC(=O)N2CCC(CC2)C3C4=C(CCC5=C3N=CC(=C5)Br)C=C(C=C4Br)Cl)C(=O)N
儲存條件(自收到貨起)	3年-20°C粉狀	儲備液保存和期限建議分裝儲備液，避免反復(fù)凍融！	1年-80°C溶于溶劑
儲存條件(自收到貨起)	3年-20°C粉狀	儲備液保存和期限建議分裝儲備液，避免反復(fù)凍融！	1個月-20°C溶于溶劑

體外溶解度
批次：

DMSO : 127 mg/mL ( (198.8 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Ethanol : 127 mg/mL (198.8 mM)

Water : Insoluble

DMSO : 11 mg/mL ( (17.21 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 100 mg/mL ( (156.53 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Ethanol : 2 mg/mL (3.13 mM)

Water : Insoluble

DMSO : 40 mg/mL ( (62.61 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Ethanol : 5 mg/mL (7.82 mM)

Water : Insoluble

摩爾濃度計算器

體內(nèi)溶解配方批次：現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑				動物體內(nèi)配方計算器
均勻懸濁液	CMC-NA	≥5mg/ml	以 1 mL 工作液為例，取 5 mg該產(chǎn)品加到 1 ml CMC-NA 溶液中，混合均勻，即可得工作液濃度為 5 mg/ml的均勻懸濁液。
均勻懸濁液	CMC-NA	≥5mg/ml	以 1 mL 工作液為例，取 5 mg該產(chǎn)品加到 1 ml CMC-NA 溶液中，混合均勻，即可得工作液濃度為 5 mg/ml的均勻懸濁液。
均勻懸濁液	CMC-NA	≥5mg/ml	以 1 mL 工作液為例，取 5 mg該產(chǎn)品加到 1 ml CMC-NA 溶液中，混合均勻，即可得工作液濃度為 5 mg/ml的均勻懸濁液。
澄清溶液	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O 該配方已經(jīng)過Selleck實驗室實測。如果上述溶解方案不能滿足您的需求，可聯(lián)系Selleck銷售提供定制化測試。	5.000mg/ml (7.83mM)	以 1 mL 工作液為例，取50μL100mg/ml的澄清DMSO儲備液加到400μL PEG300中，混合均勻使其澄清；向上述體系中加入50μLTween80，混合均勻使其澄清；然后繼續(xù)加入500μL ddH2O定容至 1 mL。工作液請現(xiàn)配現(xiàn)用！
均勻懸濁液	CMC-NA	≥5mg/ml	以 1 mL 工作液為例，取 5 mg該產(chǎn)品加到 1 ml CMC-NA 溶液中，混合均勻，即可得工作液濃度為 5 mg/ml的均勻懸濁液。

實驗計算

摩爾濃度計算器

質(zhì)量	濃度	體積	分子量
=	×	×

稀釋計算器分子量計算器

動物體內(nèi)配方計算器（澄清溶液）

第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）

給藥劑量 mg/kg 動物平均體重 g 每只動物給藥體積 μL 動物數(shù)量只

第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

計算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH₂O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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* 必填項

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):

Lonafarnib (SCH66336)

產(chǎn)品質(zhì)控

Lonafarnib (SCH66336)相關(guān)產(chǎn)品

相關(guān)信號通路圖

細胞實驗數(shù)據(jù)示例

生物活性

化學(xué)信息&溶解度

實驗計算

技術(shù)支持