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Saracatinib (AZD0530)

中文名稱：塞卡替尼

Saracatinib (AZD0530)是一種有效的Src抑制劑，無(wú)細(xì)胞試驗(yàn)中IC50為2.7 nM，對(duì)c-Yes， Fyn， Lyn， Blk， Fgr和Lck也具有活性；但對(duì)Abl和EGFR (L858R和L861Q)活性較低。Saracatinib可誘導(dǎo)自噬。Phase 2/3。

Saracatinib (AZD0530) Chemical Structure

Saracatinib (AZD0530) Chemical Structure

CAS: 379231-04-6

規(guī)格 價(jià)格 庫(kù)存 購(gòu)買數(shù)量
10mM (1mL in DMSO) 746.35 現(xiàn)貨
10mg 569.55 現(xiàn)貨
25mg 1395.95 現(xiàn)貨
200mg 5472.84 現(xiàn)貨
1g 16134.3 現(xiàn)貨
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Saracatinib (AZD0530)相關(guān)產(chǎn)品

相關(guān)信號(hào)通路圖

Src Signaling Pathways

Src信號(hào)通路圖

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系 實(shí)驗(yàn)類型 給藥濃度 孵育時(shí)間 活性描述 文獻(xiàn)信息
Huh7 Antiviral assay 2.5 uM 5 days Inhibition of viral spread in Dengue virus-infected human Huh7 cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM after 5 days by immunofluorescence assay relative to control 17360676
Huh7 Antiviral assay 2.5 uM 6 days Inhibition of viral spread in Dengue virus-infected human Huh7 cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM after 6 days by immunofluorescence assay relative to control 17360676
Vero Antiviral assay 2.5 uM 4 days Inhibition of viral spread in Dengue virus-infected african green monkey Vero cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM after 4 days by immunofluorescence assay relative to control 17360676
Vero Antiviral assay 2.5 uM 6 days Inhibition of viral spread in Dengue virus-infected african green monkey Vero cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM after 6 days by immunofluorescence assay relative to control 17360676
C6/36 Antiviral assay 2.5 uM 4 days Inhibition of viral spread in Dengue virus-infected asian tiger mosquito C6/36 cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM after 4 days by immunofluorescence assay relative to control 17360676
C6/36 Antiviral assay 2.5 uM 5 days Inhibition of viral spread in Dengue virus-infected asian tiger mosquito C6/36 cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM after 5 days by immunofluorescence assay relative to control 17360676
Vero Antiviral assay 2.5 uM 5 days Inhibition of viral spread in Dengue virus-infected african green monkey Vero cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM after 5 days by immunofluorescence assay relative to control 17360676
Huh7 Antiviral assay 2.5 uM 4 days Inhibition of viral spread in Dengue virus-infected human Huh7 cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM after 4 days by immunofluorescence assay relative to control 17360676
C6/36 Antiviral assay 2.5 uM 6 days Inhibition of viral spread in Dengue virus-infected asian tiger mosquito C6/36 cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM after 6 days by immunofluorescence assay relative to control 17360676
HEK293 Function assay 0.1 to 1 uM 16 hrs Inhibition of collagen I-induced DDR2 (unknown origin) phosphorylation expressed in HEK293 cells at 0.1 to 1 uM after 16 hrs by Western blotting 26191369
HEK293 Function assay 0.1 to 1 uM 16 hrs Inhibition of collagen I-induced DDR2 I638F mutant (unknown origin) phosphorylation expressed in HEK293 cells at 0.1 to 1 uM after 16 hrs by Western blotting 26191369
HEK293 Function assay 1 hr Inhibition of human full length PKMYT1 expressed in HEK293 cells using EFS (247 to 259 residues) as substrate after 1 hr by fluorescence polarization immunoasay, Ki = 0.0398 μM. 29941193
HEK293 Function assay 1 hr Inhibition of human full length PKMYT1 expressed in HEK293 cells using EFS (247 to 259 residues) as substrate after 1 hr by fluorescence polarization immunoasay, IC50 = 0.418 μM. 29941193
Rh30 Antiproliferative assay 48 hrs Antiproliferative activity against human Rh30 cells after 48 hrs by CellTiter-Glo luminescent assay, IC50 = 10.1 μM. 23787099
Vero Antiviral assay 3 days Antiviral activity against Dengue virus infected in african green monkey Vero cells administered after viral challenge after 3 days by viral plaque assay 17360676
SH-4 Growth Inhibition Assay IC50=4.25259 μM SANGER
PF-382 Growth Inhibition Assay IC50=3.83698 μM SANGER
OVCAR-4 Growth Inhibition Assay IC50=3.73433 μM SANGER
KNS-42 Growth Inhibition Assay IC50=3.65 μM SANGER
LC-2-ad Growth Inhibition Assay IC50=3.557 μM SANGER
SF126 Growth Inhibition Assay IC50=3.31174 μM SANGER
ETK-1 Growth Inhibition Assay IC50=3.20767 μM SANGER
LXF-289 Growth Inhibition Assay IC50=3.12109 μM SANGER
KU812 Growth Inhibition Assay IC50=3.05299 μM SANGER
GCIY Growth Inhibition Assay IC50=2.87005 μM SANGER
IST-SL2 Growth Inhibition Assay IC50=2.72379 μM SANGER
SNB75 Growth Inhibition Assay IC50=2.68594 μM SANGER
SW954 Growth Inhibition Assay IC50=2.57408 μM SANGER
BL-70 Growth Inhibition Assay IC50=2.47422 μM SANGER
MSTO-211H Growth Inhibition Assay IC50=2.35723 μM SANGER
MZ1-PC Growth Inhibition Assay IC50=2.29356 μM SANGER
NCI-H747 Growth Inhibition Assay IC50=2.25714 μM SANGER
SW872 Growth Inhibition Assay IC50=2.18507 μM SANGER
SW962 Growth Inhibition Assay IC50=2.17178 μM SANGER
GI-1 Growth Inhibition Assay IC50=2.16084 μM SANGER
TGBC24TKB Growth Inhibition Assay IC50=2.05958 μM SANGER
KALS-1 Growth Inhibition Assay IC50=1.98722 μM SANGER
SW982 Growth Inhibition Assay IC50=1.92093 μM SANGER
OS-RC-2 Growth Inhibition Assay IC50=1.88574 μM SANGER
SK-N-DZ Growth Inhibition Assay IC50=1.84688 μM SANGER
GB-1 Growth Inhibition Assay IC50=1.79833 μM SANGER
MFH-ino Growth Inhibition Assay IC50=1.7787 μM SANGER
DOHH-2 Growth Inhibition Assay IC50=1.71782 μM SANGER
RL95-2 Growth Inhibition Assay IC50=1.66902 μM SANGER
TE-10 Growth Inhibition Assay IC50=1.66252 μM SANGER
LB1047-RCC Growth Inhibition Assay IC50=1.55453 μM SANGER
EW-16 Growth Inhibition Assay IC50=1.55083 μM SANGER
HOP-62 Growth Inhibition Assay IC50=1.50246 μM SANGER
ST486 Growth Inhibition Assay IC50=1.45852 μM SANGER
TE-1 Growth Inhibition Assay IC50=1.44105 μM SANGER
TE-11 Growth Inhibition Assay IC50=1.43418 μM SANGER
NB69 Growth Inhibition Assay IC50=1.37497 μM SANGER
KGN Growth Inhibition Assay IC50=1.27687 μM SANGER
RXF393 Growth Inhibition Assay IC50=1.2436 μM SANGER
C2BBe1 Growth Inhibition Assay IC50=1.20507 μM SANGER
KS-1 Growth Inhibition Assay IC50=1.19779 μM SANGER
TK10 Growth Inhibition Assay IC50=0.90669 μM SANGER
A704 Growth Inhibition Assay IC50=0.8921 μM SANGER
TE-8 Growth Inhibition Assay IC50=0.87275 μM SANGER
BB30-HNC Growth Inhibition Assay IC50=0.86203 μM SANGER
NCI-H1436 Growth Inhibition Assay IC50=0.79049 μM SANGER
NCCIT Growth Inhibition Assay IC50=0.73218 μM SANGER
BV-173 Growth Inhibition Assay IC50=0.65249 μM SANGER
EW-24 Growth Inhibition Assay IC50=0.62693 μM SANGER
NOS-1 Growth Inhibition Assay IC50=0.60529 μM SANGER
D-336MG Growth Inhibition Assay IC50=0.50304 μM SANGER
K-562 Growth Inhibition Assay IC50=0.44967 μM SANGER
LB996-RCC Growth Inhibition Assay IC50=0.44196 μM SANGER
TE-12 Growth Inhibition Assay IC50=0.3268 μM SANGER
NCI-H1648 Growth Inhibition Assay IC50=0.28116 μM SANGER
TE-15 Growth Inhibition Assay IC50=0.27412 μM SANGER
EM-2 Growth Inhibition Assay IC50=0.265 μM SANGER
MEG-01 Growth Inhibition Assay IC50=0.23688 μM SANGER
LAMA-84 Growth Inhibition Assay IC50=0.1599 μM SANGER
CTV-1 Growth Inhibition Assay IC50=0.06143 μM SANGER
KM12 Growth Inhibition Assay IC50=4.32416 μM SANGER
NB5 Growth Inhibition Assay IC50=4.41864 μM SANGER
KURAMOCHI Growth Inhibition Assay IC50=4.65256 μM SANGER
Becker Growth Inhibition Assay IC50=4.66416 μM SANGER
MV-4-11 Growth Inhibition Assay IC50=4.81344 μM SANGER
KINGS-1 Growth Inhibition Assay IC50=4.82373 μM SANGER
LS-123 Growth Inhibition Assay IC50=5.49684 μM SANGER
SF268 Growth Inhibition Assay IC50=5.61262 μM SANGER
A388 Growth Inhibition Assay IC50=5.63667 μM SANGER
NMC-G1 Growth Inhibition Assay IC50=6.01811 μM SANGER
CGTH-W-1 Growth Inhibition Assay IC50=6.02075 μM SANGER
ES4 Growth Inhibition Assay IC50=6.53074 μM SANGER
SR Growth Inhibition Assay IC50=6.58807 μM SANGER
BB49-HNC Growth Inhibition Assay IC50=6.73206 μM SANGER
KLE Growth Inhibition Assay IC50=6.78377 μM SANGER
HUTU-80 Growth Inhibition Assay IC50=6.98466 μM SANGER
SNU-C2B Growth Inhibition Assay IC50=7.82737 μM SANGER
BB65-RCC Growth Inhibition Assay IC50=7.94904 μM SANGER
QIMR-WIL Growth Inhibition Assay IC50=8.42808 μM SANGER
GDM-1 Growth Inhibition Assay IC50=8.97292 μM SANGER
LC4-1 Growth Inhibition Assay IC50=9.00911 μM SANGER
MLMA Growth Inhibition Assay IC50=9.15006 μM SANGER
EoL-1-cell Growth Inhibition Assay IC50=9.30192 μM SANGER
BOKU Growth Inhibition Assay IC50=9.96466 μM SANGER
EVSA-T Growth Inhibition Assay IC50=10.6568 μM SANGER
D-283MED Growth Inhibition Assay IC50=10.9176 μM SANGER
NB1 Growth Inhibition Assay IC50=11.0242 μM SANGER
RPMI-8402 Growth Inhibition Assay IC50=11.178 μM SANGER
NCI-H1355 Growth Inhibition Assay IC50=11.1806 μM SANGER
NB7 Growth Inhibition Assay IC50=11.3297 μM SANGER
RPMI-6666 Growth Inhibition Assay IC50=12.9567 μM SANGER
697 Growth Inhibition Assay IC50=13.2701 μM SANGER
CTB-1 Growth Inhibition Assay IC50=13.5948 μM SANGER
VA-ES-BJ Growth Inhibition Assay IC50=13.9234 μM SANGER
BE-13 Growth Inhibition Assay IC50=14.3915 μM SANGER
SKM-1 Growth Inhibition Assay IC50=14.4499 μM SANGER
TE-6 Growth Inhibition Assay IC50=14.7591 μM SANGER
LB771-HNC Growth Inhibition Assay IC50=14.7898 μM SANGER
ECC4 Growth Inhibition Assay IC50=17.0277 μM SANGER
ES3 Growth Inhibition Assay IC50=17.4655 μM SANGER
LB647-SCLC Growth Inhibition Assay IC50=17.4949 μM SANGER
NB10 Growth Inhibition Assay IC50=18.5256 μM SANGER
L-540 Growth Inhibition Assay IC50=18.8109 μM SANGER
NCI-H2126 Growth Inhibition Assay IC50=19.51 μM SANGER
HH Growth Inhibition Assay IC50=20.0099 μM SANGER
MPP-89 Growth Inhibition Assay IC50=23.2289 μM SANGER
IST-MEL1 Growth Inhibition Assay IC50=23.8658 μM SANGER
KP-N-YS Growth Inhibition Assay IC50=23.9255 μM SANGER
EC-GI-10 Growth Inhibition Assay IC50=24.5989 μM SANGER
EKVX Growth Inhibition Assay IC50=26.0203 μM SANGER
TGBC1TKB Growth Inhibition Assay IC50=26.434 μM SANGER
Daudi Growth Inhibition Assay IC50=27.0773 μM SANGER
ALL-PO Growth Inhibition Assay IC50=27.081 μM SANGER
NB6 Growth Inhibition Assay IC50=27.488 μM SANGER
ES6 Growth Inhibition Assay IC50=27.9123 μM SANGER
COLO-320-HSR Growth Inhibition Assay IC50=28.0373 μM SANGER
K5 Growth Inhibition Assay IC50=28.1287 μM SANGER
ES1 Growth Inhibition Assay IC50=28.7773 μM SANGER
LC-1F Growth Inhibition Assay IC50=29.7346 μM SANGER
SCLC-21H Growth Inhibition Assay IC50=30.7317 μM SANGER
SK-PN-DW Growth Inhibition Assay IC50=32.5598 μM SANGER
D-247MG Growth Inhibition Assay IC50=32.9773 μM SANGER
TE-5 Growth Inhibition Assay IC50=33.0362 μM SANGER
MONO-MAC-6 Growth Inhibition Assay IC50=33.5048 μM SANGER
LB2518-MEL Growth Inhibition Assay IC50=33.7666 μM SANGER
LOXIMVI Growth Inhibition Assay IC50=33.7928 μM SANGER
NCI-H209 Growth Inhibition Assay IC50=35.144 μM SANGER
A253 Growth Inhibition Assay IC50=35.7429 μM SANGER
HCC1599 Growth Inhibition Assay IC50=36.7053 μM SANGER
EB-3 Growth Inhibition Assay IC50=36.9518 μM SANGER
GOTO Growth Inhibition Assay IC50=37.3224 μM SANGER
SW684 Growth Inhibition Assay IC50=41.8495 μM SANGER
DEL Growth Inhibition Assay IC50=42.0522 μM SANGER
HT-144 Growth Inhibition Assay IC50=42.1676 μM SANGER
TE-9 Growth Inhibition Assay IC50=43.4596 μM SANGER
KARPAS-45 Growth Inhibition Assay IC50=44.3925 μM SANGER
HAL-01 Growth Inhibition Assay IC50=44.5034 μM SANGER
RCC10RGB Growth Inhibition Assay IC50=44.7392 μM SANGER
CP67-MEL Growth Inhibition Assay IC50=45.6241 μM SANGER
NB17 Growth Inhibition Assay IC50=45.6643 μM SANGER
SK-UT-1 Growth Inhibition Assay IC50=45.9464 μM SANGER
JiyoyeP-2003 Growth Inhibition Assay IC50=46.0119 μM SANGER
HCE-4 Growth Inhibition Assay IC50=46.5968 μM SANGER
NCI-H720 Growth Inhibition Assay IC50=46.7682 μM SANGER
KARPAS-422 Growth Inhibition Assay IC50=47.0895 μM SANGER
Ramos-2G6-4C10 Growth Inhibition Assay IC50=47.1622 μM SANGER
HCE-T Growth Inhibition Assay IC50=47.6828 μM SANGER
PSN1 Growth Inhibition Assay IC50=47.7813 μM SANGER
NIH3T3 Function assay Inhibition of human c-Src in NIH3T3 cells, IC50 = 0.0027 μM. 17064066
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
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
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
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 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
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 Saracatinib (AZD0530)是一種有效的Src抑制劑，無(wú)細(xì)胞試驗(yàn)中IC50為2.7 nM，對(duì)c-Yes， Fyn， Lyn， Blk， Fgr和Lck也具有活性；但對(duì)Abl和EGFR (L858R和L861Q)活性較低。Saracatinib可誘導(dǎo)自噬。Phase 2/3。
特性 Saracatinib是第一個(gè)作用于人類腫瘤組織Src通路的抑制劑。
靶點(diǎn)
c-Src [2]
(Cell-free assay)		 LCK [2]
(Cell-free assay)		 c-YES [2]
(Cell-free assay)		 EGFR (L861Q) [2]
(Cell-free assay)		 Lyn [2]
(Cell-free assay)		 點(diǎn)擊更多
2.7 nM <4 nM 4 nM 4 nM 5 nM
體外研究(In Vitro)
體外研究活性

Saracatinib也有效抑制其他Src酪氨酸激酶家族成員，包括c-Yes, Fyn, Lyn, Blk, Fgr, 和Lck，IC50為4到10 nM。Saracatinib有效抑制SrcY530F突變的NIH 3T3細(xì)胞，IC50為80 nM。在NBT-II膀胱癌細(xì)胞中，Saracatinib顯著阻斷HT1080細(xì)胞通過立體骨膠原基質(zhì)的入侵，且完全抑制EGF誘導(dǎo)的細(xì)胞分散。[1]Saracatinib作用于DU145和PC3細(xì)胞，通過抑制Y419磷酸化而有效抑制Src激活。Saracatinib抑制前列腺癌包括PC3, DU145, CWR22Rv1和 LNCaP的生長(zhǎng)，而Saracatinib作用于 LAPC-4, PZ-HPV7和RWPE-1細(xì)胞時(shí)卻顯示低活性。Saracatinib使細(xì)胞周期停止在G1/S期，但是不使caspase 3斷裂。Saracatinib 也明顯抑制Boyden 小室的DU145和PC3 移動(dòng)。[2]Saracatinib有效且持久抑制Akt，且增強(qiáng)A549和Calu-6細(xì)胞對(duì)放射處理的敏感性。[3]Saracatinib在活性，再吸收，及組成上抑制蝕骨細(xì)胞。Saracatinib也可逆阻斷蝕骨細(xì)胞前體的移動(dòng)。[4]
激酶實(shí)驗(yàn) 激酶實(shí)驗(yàn)
使用受體和非受體酪氨酸激酶的重組催化區(qū)，通過酶聯(lián)免疫吸附法測(cè)定酪氨酸激酶活性的IC50值。加入的Saracatinib劑量從0.001到10 mM不等。針對(duì)絲氨酸/蘇氨酸激酶的特定實(shí)驗(yàn)是加32P 的滲透捕捉實(shí)驗(yàn)。在加入10 μL 20mM Mg.ATP開始反應(yīng)前，包含0.5 μL Saracatinib或DMSO（作對(duì)照) 或pH 3.0 buffer（作對(duì)照）的多支路384孔板加入15 μL酶和肽/蛋白底物溫育5分鐘。 所有酶的最終濃度都接近米氏常數(shù)（Km）。實(shí)驗(yàn)在室溫下進(jìn)行30分鐘，然后加入5 μL正磷酸終止反應(yīng)?；旌虾?，孔中的內(nèi)含物加到P81聯(lián)合板上，使用正磷酸作為洗滌緩沖液，然后計(jì)算IC50值。
細(xì)胞實(shí)驗(yàn) 細(xì)胞系 PC3, DU145, CWR22Rv1, LNCaP, LAPC-4, PZ-HPV7，和RWPE-1細(xì)胞
濃度 62.5 nM-16 mM
孵育時(shí)間 1, 3，和5天
方法

PC3, DU145, CWR22Rv1, LNCaP, LAPC-4, PZ-HPV7 及RWPE-1細(xì)胞按2×103密度接種在96孔板上，溫育過夜。加入濃度不等（62.5 nM-16 mM）的Saracatinib。1,3,5天后分離培養(yǎng)基，每孔加入0.2 mL DMSO，按每分鐘200輪持續(xù)震蕩96孔板15分鐘。MTT實(shí)驗(yàn)測(cè)IC50值。
實(shí)驗(yàn)圖片 檢測(cè)方法 檢測(cè)指標(biāo) 實(shí)驗(yàn)圖片 PMID
Western blot pY576-FAK / pY861-FAK / FAK pY418 Src / Src / pY410 CAS / CAS / Py421 Cortactin / Cortactin p-Akt / p-mTOR / Akt / mTOR / p-S6 / S6 / p-AMPKα / AMPKα 20551056
Growth inhibition assay Cell number 24349321
體內(nèi)研究(In Vivo)
體內(nèi)研究活性

Saracatinib作用于Src3T3異體移植物顯示出強(qiáng)的腫瘤生長(zhǎng)抑制率，且Saracatinib造成Calu-6, MDA-MB-231, AsPc-1和BT474C移植瘤生長(zhǎng)適當(dāng)延遲。[1]Saracatinib處理常位DU145鼠，按鼠體重，每千克每天口服處理25mg Saracatinib，結(jié)果顯示出強(qiáng)的抗癌活性。[2]
動(dòng)物實(shí)驗(yàn) Animal Models 移植DU145細(xì)胞的CB17鼠
Dosages 25 mg/kg
Administration 每天口服處理
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04598919 Active not recruiting
Idiopathic Pulmonary Fibrosis (IPF)
National Jewish Health|Yale University|Icahn School of Medicine at Mount Sinai|AstraZeneca|National Center for Advancing Translational Sciences (NCATS)|Baylor University|International Center for Health Outcomes and Innovation Research
 November 12 2020 Phase 1|Phase 2
NCT04307953 Recruiting
Fibrodysplasia Ossificans Progressiva
Amsterdam UMC location VUmc|Royal National Orthopaedic Hospital NHS Trust|Klinikum Garmisch-Patenkirchen|University of Oxford|Brigham and Women''s Hospital|AstraZeneca|Innovative Medicines Initiative
 August 5 2020 Phase 2
NCT02085603 Completed
Cancer
Sheffield Teaching Hospitals NHS Foundation Trust|AstraZeneca
 March 2014 Phase 2
NCT01864655 Completed
Alzheimer''s Disease
Stephen M. Strittmatter|National Institute of Neurological Disorders and Stroke (NINDS)|Yale University
 July 2013 Phase 1
NCT01000896 Withdrawn
Cancer|Non Small Cell Lung Cancer|Epithelial Ovarian Cancer
AstraZeneca
 January 2010 Phase 1

化學(xué)信息&溶解度

分子量 542.03 分子式

C27H32ClN5O5
CAS號(hào) 379231-04-6 SDF Download Saracatinib (AZD0530) SDF
Smiles CN1CCN(CC1)CCOC2=CC3=C(C(=C2)OC4CCOCC4)C(=NC=N3)NC5=C(C=CC6=C5OCO6)Cl
儲(chǔ)存條件(自收到貨起)

體外溶解度
批次：

DMSO : 100 mg/mL ( (184.49 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開封DMSO)

Ethanol : 100 mg/mL (184.49 mM)

Water : Insoluble

摩爾濃度計(jì)算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請(qǐng)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

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

動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請(qǐng)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）

mg/kg g μL 只

第二步：請(qǐng)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(qǐng)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(qǐng)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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常見問題及建議解決方法

問題 1:
What is the half-life of Saracatinib?

回答：
Based on the following paper, the half-life of Saracatinib in vivo is around 40hours and it reaches its peak lever around 2-4 hours after dosing: http://clincancerres.aacrjournals.org/content/16/19/4876.long

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