Sapitinib (AZD8931)

目錄號：S2192 Purity: 99.96%

Sapitinib (AZD8931)是一種可逆的，ATP競爭性EGFR，ErbB2和ErbB3抑制劑，無細(xì)胞試驗(yàn)中IC50分別為4 nM，3 nM和4 nM，作用于NSCLC細(xì)胞更有效，作用于ErbB家族比作用于MNK1和Flt選擇性強(qiáng)100倍。Phase 2。

Sapitinib (AZD8931) Chemical Structure

CAS: 848942-61-0

規(guī)格	價(jià)格	庫存
10mM (1mL in DMSO)	2608.15	現(xiàn)貨
5mg	1414.82	現(xiàn)貨
10mg	2624.23	現(xiàn)貨
50mg	7933.77	現(xiàn)貨
1g	24488.1	現(xiàn)貨
更大包裝有超大折扣
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產(chǎn)品質(zhì)控

批次：純度： 99.96%

99.96

Sapitinib (AZD8931)相關(guān)產(chǎn)品

相關(guān)產(chǎn)品	CP-724714 Mubritinib (TAK 165) AC480 (BMS-599626) Tyrphostin AG 879 HER2-Inhibitor-1 TAS0728	點(diǎn)擊展開
相關(guān)化合物庫	激酶抑制劑庫酪氨酸激酶抑制劑分子庫 PI3K/Akt 抑制劑庫細(xì)胞周期化合物庫血管生成相關(guān)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)
MCF-7	Function assay	4 hrs	Inhibition of full-length HER2 phosphorylation transfected in in human MCF-7 cl.24 cells after 4 hrs by laser scanning fluorescence microplate cytometry, IC50 = 0.06 μM.	24900741
KB	Function assay		Inhibition of EGF-stimulated EGFR phosphorylation in human KB cells, IC50 = 0.004 μM.	24900741
MCF7	Function assay		Inhibition of heregulin-stimulated HER3 phosphorylation in human MCF7 cells, IC50 = 0.004 μM.	24900741
MCF7	Function assay		Inhibition of heregulin-stimulated HER2 phosphorylation in human MCF7 cells, IC50 = 0.003 μM.	24900741
TC32	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells	29435139
DAOY	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY 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
BT-37	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 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
Saos-2	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	29435139
SK-N-SH	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH 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
BT-12	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 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
RD	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	29435139
Rh41	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells	29435139
NB1643	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells	29435139
SK-N-MC	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells	29435139
LAN-5	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells	29435139
NB-EBc1	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells	29435139
BT-37	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells	29435139
TC32	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells	29435139
Rh18	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells	29435139
Rh30	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells	29435139
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生物活性

產(chǎn)品描述

靶點(diǎn)

ErbB2 ^[1] (Cell-free assay)	EGFR ^[1] (Cell-free assay)	ErbB3 ^[1] (Cell-free assay)
3 nM	4 nM	4 nM

體外研究(In Vitro)
體外研究活性	AZD8931作用于NSCLC和SCCHN 細(xì)胞系的效果不同。AZD8931高度選擇性作用于 PC-9細(xì)胞(EGFR 激活突變型),GI50為0.1 nM，而低活性作用于 NCI-1437細(xì)胞，GI50 >10 μM。AZD8931作用于 PE/CA-PJ41, PE/CA-PJ49, DOK 和FaDu細(xì)胞，更有效作用于p-EGFR, p-erbB2 和 p-erbB3。^[1]
激酶實(shí)驗(yàn)	分離的激酶實(shí)驗(yàn)
激酶實(shí)驗(yàn)	人類EGFR和erbB2 細(xì)胞內(nèi)激酶域在桿狀病毒/Sf21 系統(tǒng)中克隆和表達(dá)。使用ATP在 K_m濃度(0.4 mM 測定 erbB2,2 mM 測定 EGFR)，使用 ELISA 法測定AZD8931的一種活性。
細(xì)胞實(shí)驗(yàn)	細(xì)胞系	頭頸部腫瘤細(xì)胞系(KYSE-30, OE21, PE/CA-PJ15, PE/CA-PJ34 (克隆 C12), PE/CA-PJ41 (克隆 D2), PE/CA-PJ49, DOK, Detroit562, RPMI2650, SCC-4, SCC-9, SCC-25, CAL 27, SW579, FaDu, Hs 840.T, KB, KYSE-450, 和 HEp-2, HN5) 和 NSCLC 細(xì)胞系 (PC-9, Calu-3, NCI-H2073, NCI-H1623, NCI-H522,
	濃度	0.001-10 μM
	孵育時(shí)間	96 小時(shí)
	方法	為了測定AZD8931體外抗細(xì)胞增殖活性，使用AZD8931處理一組 NSCLC 和SCCHN 細(xì)胞系。細(xì)胞和 AZD8931 (0.001-10 μM)溫育96小時(shí)。細(xì)胞和 MTS 比色分析實(shí)驗(yàn)試劑溫育4小時(shí)而測定存活細(xì)胞數(shù)，然后通過分光光度計(jì)在490 nm處測量吸光值。
實(shí)驗(yàn)圖片	檢測方法	檢測指標(biāo)	實(shí)驗(yàn)圖片	PMID
	Western blot	pEGFR / EGFR / pAKT / AKT / pERK / ERK HER3 / p-HER3 / HER2 / p-HER2 / p-PRAS40 / p-S6 / p-4EBP1 / p-FOXO / PARP / cleaved PARP		27102572
	Growth inhibition assay	Cell viability		28638122

體內(nèi)研究(In Vivo)
體內(nèi)研究活性	AZD8931 作用于BT474c, Calu-3, LoVo, FaDu 和 PC-9移植瘤，具有抗腫瘤活性。AZD8931急性處理BT474c移植瘤，可降低 p-AKT, Ki67 表達(dá)和p-ERK。AZD8931 可誘導(dǎo)產(chǎn)生M30凋亡標(biāo)記。而且, AZD8931治療LoVo移植瘤，具有更有效的促凋亡效果。^[1]
動(dòng)物實(shí)驗(yàn)	Animal Models	攜帶BT474c, Calu-3, LoVo, FaDu 和 PC-9移植瘤的Swiss 裸鼠或SCID小鼠
	Dosages	6.25-50 mg/kg
	Administration	口服飼喂

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)
NCT01596530	Terminated	Breast Neoplasm	AstraZeneca	June 2012	Phase 1
NCT01579578	Terminated	Metastatic Gastric or Gastro-oesophageal Junction Cancer	AstraZeneca	April 2012	Phase 2
NCT01330758	Completed	Healthy	AstraZeneca	April 2011	Phase 1
NCT01284595	Completed	Healthy	AstraZeneca	March 2011	Phase 1
NCT01151215	Terminated	Neoplasms\|Breast Neoplasms\|Breast Cancer	AstraZeneca	June 2010	Phase 2

參考文獻(xiàn)
https://pubmed.ncbi.nlm.nih.gov/20145185/

參考文獻(xiàn)

https://pubmed.ncbi.nlm.nih.gov/20145185/

化學(xué)信息&溶解度

分子量	473.93	分子式	C₂₃H₂₅ClFN₅O₃
CAS號	848942-61-0	SDF	Download Sapitinib (AZD8931) SDF
Smiles	CNC(=O)CN1CCC(CC1)OC2=C(C=C3C(=C2)C(=NC=N3)NC4=C(C(=CC=C4)Cl)F)OC
儲(chǔ)存條件(自收到貨起)	3年-20°C粉狀	儲(chǔ)備液保存和期限建議分裝儲(chǔ)備液，避免反復(fù)凍融！	1年-80°C溶于溶劑
儲(chǔ)存條件(自收到貨起)	3年-20°C粉狀	儲(chǔ)備液保存和期限建議分裝儲(chǔ)備液，避免反復(fù)凍融！	1個(gè)月-20°C溶于溶劑

體外溶解度
批次：

DMSO : 40 mg/mL ( (84.4 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 95 mg/mL ( (200.45 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請使用新開封DMSO)

Water : Insoluble

Ethanol : 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(dòng)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。
澄清溶液	30%PEG400 1 0.5%Tween80 2 5%propylene glycol 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 (10.55mM)	以 1 mL 工作液為例，取300μL16.67mg/ml的澄清PEG400儲(chǔ)備液加到5μLTween80中，混合均勻使其澄清；向上述體系中加入50μL Propylene glycol，混合均勻使其澄清；然后繼續(xù)加入645μL ddH2O定容至 1 mL。工作液請現(xiàn)配現(xiàn)用！

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(dòng)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(dòng)物的藥量）

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

第二步：請輸入動(dòng)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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