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Protein Tyrosine Kinase
VEGFR inhibitor
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c-Met inhibitor
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Apoptosis related activator
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Axl inhibitor
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FLT inhibitor
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TAM receptors (Tyro-3,Axl,and Mertk) inhibitor
Cabozantinib (XL184)
僅限科研使用
Cabozantinib (XL184)
別名: BMS-907351 中文名稱：卡博替尼
Cabozantinib是一種有效的VEGFR2抑制劑，在無細(xì)胞試驗中IC50為0.035 nM，也能有效抑制c-Met、 Ret、 Kit、Flt-1/3/4、Tie2和AXL，IC50分別為1.3 nM，4 nM，4.6 nM，12 nM/11.3 nM/6 nM，14.3 nM 和 7 nM。Cabozantinib 在結(jié)腸癌細(xì)胞中可通過AKT/GSK-3β/NF-κB信號通路誘導(dǎo)PUMA依賴的凋亡。
Cabozantinib (XL184) Chemical Structure
CAS: 849217-68-1
產(chǎn)品質(zhì)控
批次：
純度：
99.99%
99.99
Cabozantinib (XL184)相關(guān)產(chǎn)品
相關(guān)信號通路圖
細(xì)胞實驗數(shù)據(jù)示例
| 細(xì)胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻(xiàn)信息(PMID) |
|---|---|---|---|---|---|
| BAF3 | Function assay | 0.01 to 10 uM | 1 hr | Inhibition of TEL-fused wild type Ret (unknown origin) phosphorylation at Y1062/Y905 expressed in mouse BAF3 cells at 0.01 to 10 uM after 1 hr by Western blot analysis | 26652860 |
| BAF3 | Function assay | 0.01 to 10 uM | 1 hr | Inhibition of TEL-fused Ret S891A mutant (unknown origin) phosphorylation at Y1062/Y905 expressed in mouse BAF3 cells at 0.01 to 10 uM after 1 hr by Western blot analysis | 26652860 |
| BAF3 | Function assay | 0.01 to 10 uM | 1 hr | Inhibition of TEL-fused Ret S891A mutant (unknown origin) expressed in mouse BAF3 cells assessed as suppression of phosphorylation of PLCgamma at Y783 at 0.01 to 10 uM after 1 hr by Western blot analysis | 26652860 |
| BAF3 | Function assay | 0.01 to 10 uM | 1 hr | Inhibition of TEL-fused Ret S891A mutant (unknown origin) expressed in mouse BAF3 cells assessed as suppression of phosphorylation of Shc at Y317 at 0.01 to 10 uM after 1 hr by Western blot analysis | 26652860 |
| TT | Function assay | 1 to 10 uM | 4 hrs | Inhibition of RET C634W mutant in human TT cells assessed as suppression of PLCgamma phosphorylation at Y783 at 1 to 10 uM after 4 hrs by Western blot analysis | 26652860 |
| TT | Function assay | 1 to 10 uM | 4 hrs | Inhibition of RET C634W mutant in human TT cells assessed as suppression of ERK phosphorylation at T202/Y204 at 1 to 10 uM after 4 hrs by Western blot analysis | 26652860 |
| TT | Function assay | 1 to 10 uM | 4 hrs | Inhibition of RET C634W mutant in human TT cells assessed as suppression of AKT phosphorylation at T308/S473 at 1 to 10 uM after 4 hrs by Western blot analysis | 26652860 |
| TT | Function assay | 1 uM | 4 hrs | Inhibition of autophosphorylation of RET C634W mutant at Y1062 in human TT cells at 1 uM after 4 hrs by Western blot analysis | 26652860 |
| TT | Apoptosis assay | 1 uM | 96 hrs | Induction of apoptosis in human TT cells expressing Ret C634W mutant at 1 uM after 96 hrs by annexinV/PI staining-based flow cytometric analysis | 26652860 |
| A549 | Cytotoxicity assay | 10 uM | 72 hrs | Cytotoxicity against human A549 cells at 10 uM after 72 hrs by Incucyte live-cell imaging analysis | 29407963 |
| E98NT? | Growth Inhibition Assay | 0.01-10 μM | IC50=89 nM | 23484006 | |
| TT | Function assay | 1 uM | Inhibition of Ret-driven oncogenic transformation of human TT cells at 1 uM by soft agar assay | 26652860 | |
| BaF3 | Growth inhibition assay | 48 hrs | Inhibition of TEL-fused Ret S891A mutant (unknown origin) expressed in mouse BaF3 cells assessed as cell growth inhibition after 48 hrs by MTT assay, GI50 = 0.01 μM. | 26652860 | |
| BA/F3 | Growth inhibition assay | 48 hrs | Inhibition of wild type TEL-fused RET (unknown origin) expressed in mouse BA/F3 cells assessed as cell growth inhibition after 48 hrs by MTT assay, GI50 = 0.05 μM. | 26652860 | |
| TT | Growth inhibition assay | 10 days | Inhibition of RET C634W mutant in human TT cells assessed as cell growth inhibition after 10 days by MTT assay, GI50 = 0.12 μM. | 26652860 | |
| BA/F3 | Growth inhibition assay | 48 hrs | Inhibition of TEL-fused Ret V804M mutant (unknown origin) expressed in mouse BA/F3 cells assessed as cell growth inhibition after 48 hrs by MTT assay, GI50 = 0.89 μM. | 26652860 | |
| BaF3 | Growth inhibition assay | 48 hrs | Inhibition of TEL-fused Ret V804L mutant (unknown origin) expressed in mouse BaF3 cells assessed as cell growth inhibition after 48 hrs by MTT assay, GI50 = 0.91 μM. | 26652860 | |
| Nthy-ori 3-1 | Cytotoxicity assay | 10 days | Cytotoxicity against human Nthy-ori 3-1 cells after 10 days by MTT assay, GI50 = 4.93 μM. | 26652860 | |
| TT | Function assay | 4 hrs | Inhibition of autophosphorylation of RET C634W mutant at Y905 in human TT cells at 1 uM after 4 hrs by Western blot analysis | 26652860 | |
| PC3 | Function assay | 1 to 3 hrs | Inhibition of c-Met phosphorylation in human PC3 cells incubated for 1 to 3 hrs, IC50 = 1.9 μM. | 26717201 | |
| MDA-MB-231 | Function assay | 1 to 3 hrs | Inhibition of AXL phosphorylation in human MDA-MB-231 cells incubated for 1 to 3 hrs, IC50 = 5 μM. | 26717201 | |
| BAF3 | Function assay | 1 to 3 hrs | Inhibition of FLT3 (unknown origin) phosphorylation transfected in mouse BAF3 cells incubated for 1 to 3 hrs, IC50 = 7.5 μM. | 26717201 | |
| MDA-MB-231 | Function assay | 1 to 3 hrs | Inhibition of KIT (unknown origin) phosphorylation transfected in human MDA-MB-231 cells incubated for 1 to 3 hrs, IC50 = 42 μM. | 26717201 | |
| BA/F3 | Function assay | 48 hrs | Inhibition of KDR (unknown origin) expressed in mouse BA/F3 cells assessed as reduction in cell viability after 48 hrs by Cell titre glo-based luminescence assay, IC50 = 0.014 μM. | 26874741 | |
| Sf21 | Function assay | 15 mins | Inhibition of recombinant His-tagged human KDR expressed in insect Sf21 cells preincubated for 15 mins followed by substrate addition measured after 20 mins by HTRF assay, IC50 = 0.016 μM. | 26874741 | |
| BA/F3 | Function assay | 48 hrs | Inhibition of KIF5B/RET (unknown origin) expressed in mouse BA/F3 cells assessed as reduction in cell viability after 48 hrs by Cell titre glo-based luminescence assay, IC50 = 0.19 μM. | 26874741 | |
| BA/F3 | Function assay | 48 hrs | Inhibition of KIF5B/RET (unknown origin) expressed in mouse BA/F3 cells assessed as reduction in cell viability after 48 hrs by Cell titre glo-based luminescence assay, IC50 = 0.19 μM. | 26874741 | |
| BA/F3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against mouse BA/F3 cells expressing TPR-Met after 72 hrs by CCK8 assay, IC50 = 0.0219 μM. | 27068889 | |
| Sf21 | Function assay | 60 mins | Inhibition of wild type N-terminal GST-tagged recombinant human RET (658 residues) expressed in insect Sf21 cells using poly(Glu,Tyr)4:1 as substrate incubated for 60 mins by ELISA, IC50 = 0.003 μM. | 27131066 | |
| Sf21 | Function assay | 60 mins | Inhibition of N-terminal GST-tagged recombinant human RET V804M mutant (658 residues) expressed in insect Sf21 cells using poly(Glu,Tyr)4:1 as substrate incubated for 60 mins by ELISA, IC50 = 0.811 μM. | 27131066 | |
| BaF3 | Function assay | 72 hrs | Inhibition of CCDC6-RET (unknown origin) expressed in mouse BaF3 cells assessed as inhibition of cell proliferation after 72 hrs by SRB/CCK-8 assay, IC50 = 0.889 μM. | 27131066 | |
| BaF3 | Function assay | 72 hrs | Inhibition of CCDC6-RET (unknown origin) expressed in mouse BaF3 cells assessed as inhibition of cell proliferation after 72 hrs by SRB/CCK-8 assay, IC50 = 0.889 μM. | 27131066 | |
| HepG2 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay, IC50 = 0.012 μM. | 28412159 | |
| EBC1 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human EBC1 cells after 72 hrs by MTT assay, IC50 = 0.0514 μM. | 28412159 | |
| H1299 | Growth inhibition assay | 72 hrs | Growth inhibition of human H1299 cells incubated for 72 hrs by CCK8 assay, IC50 = 1.919 μM. | 28651979 | |
| MCF7 | Growth inhibition assay | 72 hrs | Growth inhibition of human MCF7 cells incubated for 72 hrs by CCK8 assay, IC50 = 2.889 μM. | 28651979 | |
| A549 | Growth inhibition assay | 72 hrs | Growth inhibition of human A549 cells incubated for 72 hrs by CCK8 assay, IC50 = 4.205 μM. | 28651979 | |
| T47D | Growth inhibition assay | 72 hrs | Growth inhibition of human T47D cells incubated for 72 hrs by CCK8 assay, IC50 = 4.448 μM. | 28651979 | |
| H460 | Growth inhibition assay | 72 hrs | Growth inhibition of human H460 cells incubated for 72 hrs by CCK8 assay, IC50 = 5.669 μM. | 28651979 | |
| HuH7 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HuH7 cells after 48 hrs by MTT assay, IC50 = 4.348 μM. | 29057042 | |
| A498 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human A498 cells after 48 hrs by MTT assay, IC50 = 8.456 μM. | 29057042 | |
| NCI-H727 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human NCI-H727 cells after 48 hrs by MTT assay, IC50 = 14.01 μM. | 29057042 | |
| BAF3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against mouse BAF3 cells harboring TRP-MET after 72 hrs by CCK-8 assay, IC50 = 0.024 μM. | 29146452 | |
| EBC1 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human EBC1 cells after 72 hrs by MTT assay, IC50 = 0.0048 μM. | 30248654 | |
| MKN45 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MKN45 cells after 72 hrs by MTT assay, IC50 = 0.0069 μM. | 30248654 | |
| SNU5 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human SNU5 cells after 72 hrs by MTT assay, IC50 = 0.0121 μM. | 30248654 | |
| BAF3 | Function assay | 72 hrs | Inhibition of TPR-tagged met (unknown origin) expressed in mouse BAF3 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay, IC50 = 0.01986 μM. | 30248654 | |
| NCI-H460 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTT assay, IC50 = 0.0401 μM. | 30248654 | |
| MGHU3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MGHU3 cells after 72 hrs by CellTiter-Glo assay | 30309671 | |
| RT112 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human RT112 cells after 72 hrs by CellTiter-Glo assay | 30309671 | |
| MDA-MB-231 | Growth Inhibition Assay | IC50= 6421 nM | 21926191 | ||
| SNU-16 | Growth Inhibition Assay | IC50=1149 nM | 21926191 | ||
| SNU-1? | Growth Inhibition Assay | IC50=5223 nM | 21926191 | ||
| Hs746T? | Growth Inhibition Assay | IC50=9.9 nM | 21926191 | ||
| SNU-5? | Growth Inhibition Assay | IC50= 19 nM | 21926191 | ||
| U87MG | Growth Inhibition Assay | IC50=1851 nM | 21926191 | ||
| H441? | Growth Inhibition Assay | IC50=21700 nM | 21926191 | ||
| H69 | Growth Inhibition Assay | IC50=20200 nM | 21926191 | ||
| PC3 | Growth Inhibition Assay | IC50=10800 nM | 21926191 | ||
| MTC-TT | Growth Inhibition Assay | IC50=0.04 + 0.03 μM | 21470995 | ||
| MZ-CRC | Growth Inhibition Assay | IC50> 5 μM | 21470995 | ||
| TPC-1 | Growth Inhibition Assay | IC50=0.06 + 0.02 μM | 21470995 | ||
| NIH-3T3/TPR-Met | Function assay | Inhibition of cell proliferation in mouse NIH-3T3/TPR-Met cells, IC50 = 1 μM. | 24996144 | ||
| BA/F3 | Growth inhibition assay | Inhibition of TEL-fused VEGFR2 (unknown origin) expressed in mouse BA/F3 cells assessed as cell growth inhibition, GI50 = 0.003 μM. | 26652860 | ||
| Ba/F3 | Function assay | Inhibition of RET (unknown origin) transfected in mouse Ba/F3 cells assessed as reduction in cell viability by CellTiter-Glo luminescence assay, GI50 = 0.07 μM. | 27814560 | ||
| TT | Function assay | Inhibition of RET C634W mutant in human TT cells assessed as reduction in cell viability by CellTiter-Glo luminescence assay, GI50 = 0.26 μM. | 27814560 | ||
| Ba/F3 | Function assay | Inhibition of RET V804M mutant (unknown origin) transfected in mouse Ba/F3 cells assessed as reduction in cell viability by CellTiter-Glo luminescence assay, GI50 = 0.74 μM. | 27814560 | ||
| Nthy-ori 3-1 | Cytotoxicity assay | Cytotoxicity against human Nthy-ori 3-1 cells assessed as reduction in cell viability by CellTiter-Glo luminescence assay, GI50 = 2.92 μM. | 27814560 | ||
| 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 | ||
| 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 | ||
| BT-12 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 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 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) | 29435139 | ||
| U-2 OS | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells | 29435139 | ||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells | 29435139 | ||
| Rh41 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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 | ||
| Rh18 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 29435139 | ||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells | 29435139 | ||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells | 29435139 | ||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells | 29435139 | ||
| 點擊查看更多細(xì)胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | Cabozantinib是一種有效的VEGFR2抑制劑，在無細(xì)胞試驗中IC50為0.035 nM，也能有效抑制c-Met、 Ret、 Kit、Flt-1/3/4、Tie2和AXL，IC50分別為1.3 nM，4 nM，4.6 nM，12 nM/11.3 nM/6 nM，14.3 nM 和 7 nM。Cabozantinib 在結(jié)腸癌細(xì)胞中可通過AKT/GSK-3β/NF-κB信號通路誘導(dǎo)PUMA依賴的凋亡。 | ||||||
|---|---|---|---|---|---|---|---|
| 靶點 |
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| 體外研究(In Vitro) | ||||
| 體外研究活性 | XL184是多種受體酪氨酸激酶小分子抑制劑，尤其抑制c-Met 和VEGFR2。XL-184也有效作用于Ret, Kit, FLT1, FLT3, FLT4, Tie2, 和 AXL ， IC50分別為 4 nM, 4.6 nM, 12 nM, 11.3 nM, 6 nM, 14.3 nM, 和7 nM。XL184微弱抑制 RON 和PDGFR-β，IC50分別為 124 nM和 234 nM,而對FGFR1則幾乎沒有抑制活性，IC50 為5.294 μM。[1] XL184低濃度(0.1-0.5 μM) 時處理MPNST細(xì)胞，也顯著抑制組成型和誘導(dǎo)型Met磷酸化及其下游信號，且抑制 HGF誘導(dǎo)的MPNST細(xì)胞遷移和侵襲。XL184作用于細(xì)胞因子刺激的人臍靜脈內(nèi)皮細(xì)胞（HUVECs），也顯著抑制Met和VEGFR2磷酸化。雖然XL184濃度為0.1 μM時不能抑制MPNST細(xì)胞生長，但是濃度為5-10 μM 時則能顯著抑制MPNST細(xì)胞生長。[2] | |||
|---|---|---|---|---|
| 細(xì)胞實驗 | 細(xì)胞系 | ST88-14, STS26T, 和MPNST724 | ||
| 濃度 | 溶于DMSO,終濃度~10 μM | |||
| 孵育時間 | 48小時 | |||
| 方法 | 使用不同濃度XL184處理細(xì)胞48小時。通過MTS實驗使用CellTiter96 Aqueous 非放射性細(xì)胞增殖實驗試劑盒測定細(xì)胞生長。然后在 490 nm處測定吸光值。 | |||
| 實驗圖片 | 檢測方法 | 檢測指標(biāo) | 實驗圖片 | PMID |
| Western blot | p-MET(Y1234/1235) / MET / p-EGFR(Y1068) / EGFR / p-Gab1(Y627) / Gab1 / p-AKT(S473) / p-ERK / p-EIF4E p-MET / p-ERK / p-AKT |
|
29188469 | |
| Immunofluorescence | α-tubulin |
|
29520051 | |
| Growth inhibition assay | Cell viability |
|
23661005 | |
| 體內(nèi)研究(In Vivo) | ||
| 體內(nèi)研究活性 | XL184按 30 mg/kg 劑量處理攜帶自發(fā)胰島細(xì)胞瘤的RIP-Tag2 小鼠，擾亂 83%腫瘤血管, 降低周細(xì)胞和空基底膜袖，引起廣泛瘤內(nèi)缺氧和廣泛的腫瘤細(xì)胞凋亡，且停藥后延緩腫瘤血管再生長，與XL999相比更顯著抑制VEGFR而不是c-Met，導(dǎo)致血管降低43％，說明抑制VEGFR，也抑制放大抑制血管新生的其他功能相關(guān)的受體酪氨酸激酶（RTK）。XL184也降低原發(fā)腫瘤的侵襲和減少轉(zhuǎn)移。[1] XL184 每天按30 mg/kg劑量處理SCID小鼠，顯著廢除人 MPNST移植瘤生長和轉(zhuǎn)移。[2] XL184 處理乳腺癌，肺癌膠質(zhì)瘤模型，抑制腫瘤生長，這種作用存在劑量依賴性，降低腫瘤和內(nèi)皮細(xì)胞增殖，促進(jìn)凋亡。XL184按100 mg/kg 和 10 mg/kg劑量分別單獨處理攜帶MDA-MB-231腫瘤的小鼠和攜帶C6腫瘤的大鼠，持續(xù)抑制腫瘤生長。[3] | |
|---|---|---|
| 動物實驗 | Animal Models | 攜帶自發(fā)胰島腫瘤的RIP-TAG2轉(zhuǎn)基因小鼠。 |
| Dosages | ~60 mg/kg | |
| Administration | 口服飼喂 | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT06156410 | Recruiting | Ewing Sarcoma|Osteosarcoma |
Children''s Hospital of Philadelphia|Children''s Hospital Colorado|Exelixis|Alex''s Lemonade Stand Foundation |
October 24 2023 | Phase 1 |
| NCT05249114 | Active not recruiting | Neuroendocrine Tumors |
Providence Health & Services|Exelixis|Advanced Accelerator Applications SA |
December 28 2022 | Phase 1 |
| NCT05444933 | Completed | Advanced Renal Cell Carcinoma |
Ipsen |
September 16 2022 | -- |
|
化學(xué)信息&溶解度
| 分子量 | 501.51 | 分子式 | C28H24FN3O5 |
| CAS號 | 849217-68-1 | SDF | Download Cabozantinib (XL184) SDF |
| Smiles | COC1=CC2=C(C=CN=C2C=C1OC)OC3=CC=C(C=C3)NC(=O)C4(CC4)C(=O)NC5=CC=C(C=C5)F | ||
| 儲存條件(自收到貨起) | |||
|
體外溶解度 |
DMSO : 100 mg/mL ( (199.39 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO) Water : Insoluble Ethanol : Insoluble |
摩爾濃度計算器 |
|
體內(nèi)溶解配方 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 | |||||
實驗計算
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）
mg/kg
g
μL
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(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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