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Cytoskeletal Signaling
HDAC inhibitor
-
PI3K inhibitor
-
Apoptosis related activator
Fimepinostat (CUDC-907)
僅限科研使用
Fimepinostat (CUDC-907)
中文名稱：非美諾司他
CUDC-907是一種PI3K和HDAC雙重抑制劑，作用于PI3Kα和HDAC1/2/3/10，IC50分別為19 nM和1.7 nM/5 nM/1.8 nM/2.8 nM。CUDC-907 在乳腺癌細(xì)胞中可誘導(dǎo)細(xì)胞周期阻滯與凋亡。Phase 1。
Fimepinostat (CUDC-907) Chemical Structure
CAS: 1339928-25-4
產(chǎn)品質(zhì)控
批次：
純度：
99.97%
99.97
Fimepinostat (CUDC-907)相關(guān)產(chǎn)品
相關(guān)信號通路圖
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(PMID) |
|---|---|---|---|---|---|
| MV4-11 | Antiproliferative assay | 25 to 50 nM | 72 hrs | Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability at 25 to 50 nM after 72 hrs by tryphan blue assay | 32212730 |
| human Glioma cells (HF2476) | Cytotoxicity assay | 72 h | Cytotoxicity against human Glioma cells (HF2476) after 72 hrs by CelltiterGlo assay, EC50=0.7 nM | 26288699 | |
| human Glioma cells (HF2790)? | Cytotoxicity assay | 72 h | Cytotoxicity against human Glioma cells (HF2790) after 72 hrs by CelltiterGlo assay, EC50=0.7 nM | 26288699 | |
| human Glioma cells (HF2876)? | Cytotoxicity assay | 72 h | Cytotoxicity against human Glioma cells (HF2876) after 72 hrs by CelltiterGlo assay, EC50=0.7 nM | 26288699 | |
| human Glioma cells (HF3013) | Cytotoxicity assay | 72 h | Cytotoxicity against human Glioma cells (HF3013) after 72 hrs by CelltiterGlo assay, EC50=0.7 nM | 26288699 | |
| human Glioma cells (HF2885) | Cytotoxicity assay | 72 h | Cytotoxicity against human Glioma cells (HF2885) after 72 hrs by CelltiterGlo assay, EC50=0.7 nM | 26288699 | |
| human Glioma cells (HF2381) | Cytotoxicity assay | 72 h | Cytotoxicity against human Glioma cells (HF2381) after 72 hrs by CelltiterGlo assay, EC50=0.7 nM | 26288699 | |
| human Glioma cells (HF2303) | Cytotoxicity assay | 72 h | Cytotoxicity against human Glioma cells (HF2303) after 72 hrs by CelltiterGlo assay, EC50=0.7 nM | 26288699 | |
| MV4-11 | Cytotoxicity assay | 24 hrs | Cytotoxicity against human MV4-11 cells assessed as growth inhibition after 24 hrs by MTT assay, =0.00043μM. | 27186676 | |
| Sf9 | Function assay | 15 mins | Inhibition of full length C-terminal His-tagged human recombinant HDAC3/NCOR2 (395 to 489 residues) expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substr, =0.0018μM. | 27186676 | |
| Sf9 | Function assay | 15 mins | Inhibition of human recombinant HDAC10 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence assay, =0.0028μM. | 27186676 | |
| Sf9 | Function assay | 15 mins | Inhibition of full length human recombinant HDAC2 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence a, =0.005μM. | 27186676 | |
| Sf9 | Function assay | 15 mins | Inhibition of full length human recombinant HDAC11 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence , =0.0054μM. | 27186676 | |
| A2780S | Cytotoxicity assay | 24 hrs | Cytotoxicity against human A2780S cells assessed as growth inhibition after 24 hrs by MTT assay, =0.00615μM. | 27186676 | |
| HCT116 | Cytotoxicity assay | 24 hrs | Cytotoxicity against human HCT116 cells assessed as growth inhibition after 24 hrs by MTT assay, =0.00734μM. | 27186676 | |
| Sf9 | Function assay | 60 mins | Inhibition of full length recombinant human N-terminal GST-tagged p110 alpha/untagged p85 alpha expressed in baculovirus infected insect Sf9 cells using PI:3PS as substrate incubated for 60 mins by ADP-Glo luminescence assay, =0.019μM. | 27186676 | |
| Sf9 | Function assay | 15 mins | Inhibition of full length human recombinant HDAC6 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence a, =0.027μM. | 27186676 | |
| Sf9 | Function assay | 2 hrs | Inhibition of N-terminal His6-tagged recombinant full-length human p110delta/untagged recombinant full length human p85alpha expressed in baculovirus infected insect Sf9 cells incubated for 2 hrs by kinase-glo assay, =0.039μM. | 27186676 | |
| Sf9 | Function assay | 1 hr | Inhibition of recombinant human p110beta expressed in baculovirus infected insect Sf9 cells incubated for 1 hr by ADP-gloreagen assay, =0.054μM. | 27186676 | |
| A2780S | Function assay | 6 hrs | Inhibition of HDAC1/2/3 in human A2780S cells assessed as histone H3 acetylation incubated for 6 hrs by cytoblot assay, =0.12625μM. | 27186676 | |
| Sf9 | Function assay | 15 mins | Inhibition of full length C-terminal His-tagged human recombinant HDAC8 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after , =0.191μM. | 27186676 | |
| A2780S | Function assay | 6 hrs | Inhibition of HDAC6 in human A2780S cells assessed as tubulin acetylation incubated for 6 hrs by cytoblot assay, =0.22175μM. | 27186676 | |
| Sf9 | Function assay | 15 mins | Inhibition of N-terminal GST/C-terminal His-tagged human recombinant HDAC4 (627 to 1084 residues) expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrat, =0.409μM. | 27186676 | |
| Sf9 | Function assay | 15 mins | Inhibition of N-terminal GST-tagged human recombinant HDAC7 (518 to end residues) expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measu, =0.426μM. | 27186676 | |
| Sf9 | Function assay | 15 mins | Inhibition of C-terminal His-tagged human recombinant HDAC9 (604 to 1066 residues) expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition meas, =0.554μM. | 27186676 | |
| Sf9 | Function assay | 15 mins | Inhibition of human recombinant HDAC5 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence assay, =0.674μM. | 27186676 | |
| Sf9 | Function assay | 15 mins | Inhibition of recombinant C-terminal His/FLAG-tagged HDAC1 (unknown origin) expressed in baculovirus infected Sf9 insect cells using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr, =0.00036μM. | 31117517 | |
| Sf9 | Function assay | 15 mins | Inhibition of recombinant human full length C-terminal His-tagged HDAC8 expressed in baculovirus infected Sf9 insect cells using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr, =0.0014μM. | 31117517 | |
| Sf9 | Function assay | 15 mins | Inhibition of recombinant human full length HDAC2 expressed in baculovirus infected Sf9 insect cells using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr, =0.0016μM. | 31117517 | |
| HCT116 | Antiproliferative assay | 96 hrs | Antiproliferative activity against human HCT116 cells after 96 hrs by MTT assay, =0.005μM. | 31117517 | |
| HCT8 | Antiproliferative assay | 96 hrs | Antiproliferative activity against human HCT8 cells after 96 hrs by MTT assay, =0.005μM. | 31117517 | |
| U87 | Antiproliferative assay | 96 hrs | Antiproliferative activity against human U87 cells after 96 hrs by MTT assay, =0.007μM. | 31117517 | |
| Capan2 | Antiproliferative assay | 96 hrs | Antiproliferative activity against human Capan2 cells after 96 hrs by MTT assay, =0.007μM. | 31117517 | |
| MDA-MB-453 | Antiproliferative assay | 96 hrs | Antiproliferative activity against human MDA-MB-453 cells after 96 hrs by MTT assay, =0.009μM. | 31117517 | |
| Bel7402 | Antiproliferative assay | 96 hrs | Antiproliferative activity against human Bel7402 cells after 96 hrs by MTT assay, =0.013μM. | 31117517 | |
| HepG2 | Antiproliferative assay | 96 hrs | Antiproliferative activity against human HepG2 cells after 96 hrs by MTT assay, =0.015μM. | 31117517 | |
| NCI-H1299 | Antiproliferative assay | 96 hrs | Antiproliferative activity against human NCI-H1299 cells after 96 hrs by MTT assay, =0.025μM. | 31117517 | |
| MCF7 | Antiproliferative assay | 96 hrs | Antiproliferative activity against human MCF7 cells after 96 hrs by MTT assay, =0.041μM. | 31117517 | |
| HGC27 | Antiproliferative assay | 96 hrs | Antiproliferative activity against human HGC27 cells after 96 hrs by MTT assay, =0.041μM. | 31117517 | |
| Sf9 | Function assay | 15 mins | Inhibition of recombinant human full length HDAC11 expressed in baculovirus infected Sf9 insect cells using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr, =0.132μM. | 31117517 | |
| NCI-H460 | Antiproliferative assay | 96 hrs | Antiproliferative activity against human NCI-H460 cells after 96 hrs by MTT assay, =0.15μM. | 31117517 | |
| SW1990 | Antiproliferative assay | 96 hrs | Antiproliferative activity against human SW1990 cells after 96 hrs by MTT assay, =0.18μM. | 31117517 | |
| K562 | Antiproliferative assay | 96 hrs | Antiproliferative activity against human K562 cells after 96 hrs by MTT assay, =0.28μM. | 31117517 | |
| Sf9 | Function assay | 15 mins | Inhibition of recombinant human full length HDAC4 expressed in baculovirus infected Sf9 insect cells using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr, =0.445μM. | 31117517 | |
| DU145 | Antiproliferative assay | 96 hrs | Antiproliferative activity against human DU145 cells after 96 hrs by MTT assay, =0.56μM. | 31117517 | |
| HuH7 | Antiproliferative assay | 96 hrs | Antiproliferative activity against human HuH7 cells after 96 hrs by MTT assay, =0.56μM. | 31117517 | |
| Sf9 | Function assay | Inhibition of recombinant full length human N-terminal GST-tagged PI3K p110alpha/untagged p85alpha expressed in baculovirus infected insect Sf9 cells by ADP-Glo luminescent assay, =0.019μM. | 28494256 | ||
| Sf9 | Function assay | Inhibition of recombinant full length human N-terminal GST-tagged PI3K p110delta/untagged p85alpha expressed in baculovirus infected insect Sf9 cells by ADP-Glo luminescent assay, =0.039μM. | 28494256 | ||
| Sf9 | Function assay | Inhibition of recombinant full length human N-terminal GST-tagged PI3K p110beta/untagged p85alpha expressed in baculovirus infected insect Sf9 cells by ADP-Glo luminescent assay, =0.054μM. | 28494256 | ||
| 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 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 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 | ||
| U-2 OS | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS 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 | ||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 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 | ||
| Rh18 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 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 | ||
| 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 | ||
| Rh30 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 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 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) | 29435139 | ||
| BT-12 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 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 | ||
| DAOY | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells | 29435139 | ||
| MG 63 (6-TG R) | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) 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 | ||
| Rh41 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells | 29435139 | ||
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD 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 | ||
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells | 29435139 | ||
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for SK-N-SH cells | 29435139 | ||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for SJ-GBM2 cells | 29435139 | ||
| Daoy | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for Daoy cells | 29435139 | ||
| Sf9 | Function assay | Inhibition of recombinant human full-length N-terminal GST-tagged p110alpha/untagged full-length p85alpha expressed in baculovirus infected Sf9 cells using PIP2 as substrate by ADP-glo luminescence assay, =0.019μM. | 30418766 | ||
| Sf9 | Function assay | Inhibition of recombinant human full-length N-terminal GST-tagged p110delta/untagged full-length p85alpha expressed in baculovirus infected Sf9 cells using PIP2 as substrate by ADP-glo luminescence assay, =0.039μM. | 30418766 | ||
| Sf9 | Function assay | Inhibition of recombinant human full-length N-terminal GST-tagged p110beta/untagged full-length p85alpha expressed in baculovirus infected Sf9 cells using PIP2 as substrate by ADP-glo luminescence assay, =0.054μM. | 30418766 | ||
| 點(diǎn)擊查看更多細(xì)胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | CUDC-907是一種PI3K和HDAC雙重抑制劑，作用于PI3Kα和HDAC1/2/3/10，IC50分別為19 nM和1.7 nM/5 nM/1.8 nM/2.8 nM。CUDC-907 在乳腺癌細(xì)胞中可誘導(dǎo)細(xì)胞周期阻滯與凋亡。Phase 1。 | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 靶點(diǎn) |
|
| 體外研究(In Vitro) | ||||
| 體外研究活性 | PI3K/HDAC Inhibitor 抑制其他PI3K亞型，如 PI3Kβ, PI3Kγ, PI3Kδ和 PI3KɑE545K ， IC50 分別為 54, 311, 39 和62 nM。而且, PI3K/HDAC Inhibitor 也抑制HDAC亞型HDAC8, HDAC6 和 HDAC11，IC50分別為191, 27 和 5.4 nM。此外, PI3K/HDAC Inhibitor 低效抑制其他類型 HDAC 酶活性。PI3K/HDAC Inhibitor 抑制一系列B細(xì)胞淋巴瘤生長，如Granta 519, DOHH2, RL, Pfeiffer, SuDHL4, Daudi 和 Raji，IC50 分別為 7, 1, 2, 4, 3, 15 和 9 nM。PI3K/HDAC Inhibitor 也阻斷 骨髓瘤增殖，如RPMI8226, OPM-2 和 ARH77，IC50分別為 2, 1 和5 nM。PI3K/HDAC Inhibitor 作用于多發(fā)性骨髓瘤和B細(xì)胞淋巴瘤，具有有效抗癌活性。[1] |
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|---|---|---|---|---|
| 實(shí)驗(yàn)圖片 | 檢測方法 | 檢測指標(biāo) | 實(shí)驗(yàn)圖片 | PMID |
| Western blot | AKT / p-AKT / P-p70S6K1 / Ac-H3K9 / p-MEK / p-ERK / p-STAT3 / MCL-1 / Bcl-2 / Bcl-xl / PARP p-PRAS40 / p-4EBP1 / p-S6 / c-Myc / Cleaved PARP / Caspase-3 / Celaved caspase-3 SYK / BTK / Bcl-10 / MyD88 / IRAK4 |
|
30353642 | |
| Immunofluorescence | γ-H2AX / 53BP1 RAD51 |
|
29760046 | |
| Growth inhibition assay | Cell viability |
|
28147336 | |
| 體內(nèi)研究(In Vivo) | ||
| 體內(nèi)研究活性 | PI3K/HDAC Inhibitor 口服給藥犬類具有生物有效性。PI3K/HDAC Inhibitor 治療小鼠腫瘤具有長的半衰期。PI3K/HDAC Inhibitor 作用于移植瘤，誘導(dǎo)凋亡，且抑制癌細(xì)胞增殖。在高效性研究中， PI3K/HDAC Inhibitor 按最大耐受劑量(MTD)處理，作用于NHL和MM模型，比單獨(dú)藥劑PI3K或HDAC抑制劑參考化合物或兩者聯(lián)用更有效。而且, PI3K/HDAC Inhibitor 按MTD劑量處理，比PI3Kδ選擇性抑制劑CAL-101更有效。[1] |
|
|---|---|---|
| 動(dòng)物實(shí)驗(yàn) | Animal Models | 攜帶NHL和 MM模型的小鼠 |
| Dosages | 100 mg/kg | |
| Administration | 口服處理 | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT02909777 | Active not recruiting | Lymphoma|Neuroblastoma|Brain Tumor|Solid Tumor |
Dana-Farber Cancer Institute|Curis Inc. |
October 2016 | Phase 1 |
| NCT02307240 | Completed | Triple-Negative Breast Cancer|High-grade Serous Ovarian Cancer|Solid Tumors|NUT Midline Carcinoma |
Curis Inc. |
November 2014 | Phase 1 |
| NCT01742988 | Completed | Lymphoma|Relapsed Lymphoma|Refractory Lymphoma|Relapsed and/or Refractory Lymphoma|Relapsed Ddiffuse Large B-Cell Lymphoma (DLBCL)|Refractory Diffuse Large B-Cell Lymphoma (DLBCL)|Relapsed and/or Refractory Diffuse Large B-Cell Lymphoma (DLBCL)|Double-hit Lymphoma (DHL)|Triple-hit Lymphoma (THL)|Double-expressor Lymphoma (DEL)|High-grade B-cell Lymphoma (HGBL) |
Curis Inc.|The Leukemia and Lymphoma Society |
December 2012 | Phase 1 |
|
化學(xué)信息&溶解度
| 分子量 | 508.55 | 分子式 | C23H24N8O4S |
| CAS號 | 1339928-25-4 | SDF | Download Fimepinostat (CUDC-907) SDF |
| Smiles | CN(CC1=CC2=C(S1)C(=NC(=N2)C3=CN=C(C=C3)OC)N4CCOCC4)C5=NC=C(C=N5)C(=O)NO | ||
| 儲存條件(自收到貨起) | |||
|
體外溶解度 |
DMSO : 100 mg/mL ( (196.63 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(jì)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(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
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）
mg/kg
g
μL
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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常見問題及建議解決方法
問題 1:
How to solve CUDC-907 for in vivo studies (p.o.)?
回答：
If you decided to take P.O. as your administration route, we suggest you to use 1% CMC-Na to dilute CUDC-907 as a suspension solution for gavage.
問題 2:
What is the half-life of CUDC-907 in vivo?
回答：
GUDC-907 is said to have a long half-life in mouse tumor model: http://cancerres.aacrjournals.org/content/72/8_Supplement/3744.short, however, its not formally published and we have no detail of how long it is.
