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(xì)胞試驗(yàn)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(jià)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
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產(chǎn)品質(zhì)控

批次：純度： 99.48%

99.48

Lonafarnib (SCH66336)相關(guān)產(chǎn)品

相關(guān)產(chǎn)品	Tipifarnib (IND 58359) FTI 277 HCl LB42708	點(diǎn)擊展開
相關(guān)化合物庫	代謝化合物庫抗癌代謝化合物庫谷氨酰胺代謝化合物庫糖代謝化合物庫脂代謝化合物庫	點(diǎn)擊展開

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系	實(shí)驗(yàn)類型	孵育時(shí)間	活性描述	文獻(xiàn)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(diǎn)擊查看更多細(xì)胞系數(shù)據(jù)

生物活性

產(chǎn)品描述

靶點(diǎn)

H-ras (Cell-free assay)	N-ras (Cell-free assay)	K-ras-4B (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(xì)胞癌(HNSCC) 生長和誘導(dǎo)凋亡，抑制效果具有劑量和時(shí)間依賴性。SCH66336 (8 μM)可在SqCC/Y1細(xì)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。SCH66336 對多細(xì)胞系有抗增殖作用，IC 50范圍從0.6 μM 到32.3 μM ; Lonafarnib誘導(dǎo)CCAAT /增強(qiáng)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(xì)胞凋亡。Lonafarnib (5 μM)可增加DR5的細(xì)胞表面分布，增強(qiáng)腫瘤壞死因子相關(guān)凋亡誘導(dǎo)配體誘導(dǎo)的H1792細(xì)胞凋亡。
細(xì)胞實(shí)驗(yàn)	細(xì)胞系	UMSCC10B, UMSCC14B, UMSCC17B, UMSCC22B, 和UMSCC35, UMSCC38 細(xì)胞
	濃度	0.1 μM - 8 μM
	孵育時(shí)間	24 小時(shí)
	方法	細(xì)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(shí)后，用不同濃度SCH66336處理細(xì)胞。SCH66336溶解于DMSO。對照組細(xì)胞用同樣量的DMSO處理。5天后用SRB法檢測細(xì)胞數(shù)量。生長抑制的百分比的計(jì)算公式為：增長抑制百分比=（1?/At/Ac）×100，At和Ac分別代表實(shí)驗(yàn)組和對照組的吸收值。IC 50值由劑量反應(yīng)曲線確定。
實(shí)驗(yàn)圖片	檢測方法	檢測指標(biāo)	實(shí)驗(yàn)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。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(dá)69%。
動物實(shí)驗(yàn)	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(yàn)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(xiàn)
[1]https://pubmed.ncbi.nlm.nih.gov/9810004/ [2]https://pubmed.ncbi.nlm.nih.gov/12941797/ [3]https://pubmed.ncbi.nlm.nih.gov/11389071/ [4]https://pubmed.ncbi.nlm.nih.gov/17493934/ + 展開

參考文獻(xiàn)

[1]https://pubmed.ncbi.nlm.nih.gov/9810004/
[2]https://pubmed.ncbi.nlm.nih.gov/12941797/
[3]https://pubmed.ncbi.nlm.nih.gov/11389071/

[4]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(jì)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(jì)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(shí)驗(yàn)室實(shí)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(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量	濃度	體積	分子量
=	×	×

稀釋計(jì)算器分子量計(jì)算器

動物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)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(jì)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(jìn)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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C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

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Lonafarnib (SCH66336)

產(chǎn)品質(zhì)控

Lonafarnib (SCH66336)相關(guān)產(chǎn)品

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

生物活性

化學(xué)信息&溶解度

實(shí)驗(yàn)計(jì)算

技術(shù)支持