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PF-4708671
PF-4708671 is a cell-permeable inhibitor of p70 ribosomal S6 kinase (S6K1 isoform) with Ki/IC50 of 20 nM/160 nM in cell-free assays, 400-fold greater selectivity for S6K1 than S6K2, and 4- and >20-fold selectivity for S6K1 than MSK1 and RSK1/2, respectively. First S6K1-specific inhibitor to be reported.
CAS No. 1255517-76-0
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製品安全説明書
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純度：
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PF-4708671関連製品
| 関連ターゲット | p70 S6K p70 S6K1 RSK1 RSK2 RSK3 RSK4 | もっと見る |
|---|---|---|
| 関連製品 | BI-D1870 LY2584702 LY2584702 Tosylate LJI308 LJH685 | もっと見る |
| 関連化合物ライブラリー | Kinase Inhibitor Library PI3K/Akt Inhibitor Library Apoptosis Compound Library Cell Cycle compound library NF-κB Signaling Compound Library | もっと見る |
シグナル伝達経路
S6 Kinase阻害剤の選択性比較
Cell Data
| Cell Lines | Assay Type | Concentration | Incubation Time | 活性情報 | PMID |
|---|---|---|---|---|---|
| BHT-101 | Growth Inhibition Assay | IC50=0.82024 μM | SANGER | ||
| UACC-893 | Growth Inhibition Assay | IC50=5.19886 μM | SANGER | ||
| A427 | Growth Inhibition Assay | IC50=5.72567 μM | SANGER | ||
| OCUB-M | Growth Inhibition Assay | IC50=6.66102 μM | SANGER | ||
| SW684 | Growth Inhibition Assay | IC50=7.52268 μM | SANGER | ||
| SK-LMS-1 | Growth Inhibition Assay | IC50=9.01302 μM | SANGER | ||
| CP50-MEL-B | Growth Inhibition Assay | IC50=9.30419 μM | SANGER | ||
| NCI-H1651 | Growth Inhibition Assay | IC50=10.0276 μM | SANGER | ||
| ABC-1 | Growth Inhibition Assay | IC50=10.1037 μM | SANGER | ||
| OE19 | Growth Inhibition Assay | IC50=10.1733 μM | SANGER | ||
| DSH1 | Growth Inhibition Assay | IC50=10.8879 μM | SANGER | ||
| SW13 | Growth Inhibition Assay | IC50=11.9319 μM | SANGER | ||
| MDA-MB-453 | Growth Inhibition Assay | IC50=12.1603 μM | SANGER | ||
| 647-V | Growth Inhibition Assay | IC50=12.3582 μM | SANGER | ||
| NCI-H2342 | Growth Inhibition Assay | IC50=12.3995 μM | SANGER | ||
| LB2241-RCC | Growth Inhibition Assay | IC50=12.5779 μM | SANGER | ||
| UACC-257 | Growth Inhibition Assay | IC50=13.4453 μM | SANGER | ||
| NCI-H661 | Growth Inhibition Assay | IC50=13.6449 μM | SANGER | ||
| FADU | Growth Inhibition Assay | IC50=13.6992 μM | SANGER | ||
| A2780 | Growth Inhibition Assay | IC50=13.8041 μM | SANGER | ||
| NCI-H1793 | Growth Inhibition Assay | IC50=14.4085 μM | SANGER | ||
| TE-8 | Growth Inhibition Assay | IC50=15.3465 μM | SANGER | ||
| HGC-27 | Growth Inhibition Assay | IC50=16.1644 μM | SANGER | ||
| MMAC-SF | Growth Inhibition Assay | IC50=17.3727 μM | SANGER | ||
| Calu-6 | Growth Inhibition Assay | IC50=18.1513 μM | SANGER | ||
| HUTU-80 | Growth Inhibition Assay | IC50=18.3959 μM | SANGER | ||
| SAS | Growth Inhibition Assay | IC50=18.6455 μM | SANGER | ||
| IST-MES1 | Growth Inhibition Assay | IC50=18.6508 μM | SANGER | ||
| C3A | Growth Inhibition Assay | IC50=18.7919 μM | SANGER | ||
| ES3 | Growth Inhibition Assay | IC50=18.8364 μM | SANGER | ||
| HSC-2 | Growth Inhibition Assay | IC50=19.6541 μM | SANGER | ||
| T47D | Growth Inhibition Assay | IC50=20.1485 μM | SANGER | ||
| EW-7 | Growth Inhibition Assay | IC50=20.8588 μM | SANGER | ||
| LN-405 | Growth Inhibition Assay | IC50=20.8965 μM | SANGER | ||
| U031 | Growth Inhibition Assay | IC50=21.4802 μM | SANGER | ||
| A549 | Growth Inhibition Assay | IC50=21.8491 μM | SANGER | ||
| RMG-I | Growth Inhibition Assay | IC50=22.2668 μM | SANGER | ||
| BT-474 | Growth Inhibition Assay | IC50=22.6551 μM | SANGER | ||
| NB69 | Growth Inhibition Assay | IC50=23.152 μM | SANGER | ||
| NB7 | Growth Inhibition Assay | IC50=24.188 μM | SANGER | ||
| HCC1569 | Growth Inhibition Assay | IC50=24.6125 μM | SANGER | ||
| MEL-JUSO | Growth Inhibition Assay | IC50=24.6908 μM | SANGER | ||
| MDA-MB-175-VII | Growth Inhibition Assay | IC50=25.2517 μM | SANGER | ||
| HCC1419 | Growth Inhibition Assay | IC50=25.6003 μM | SANGER | ||
| Ca9-22 | Growth Inhibition Assay | IC50=25.6432 μM | SANGER | ||
| KGN | Growth Inhibition Assay | IC50=25.7547 μM | SANGER | ||
| LB373-MEL-D | Growth Inhibition Assay | IC50=26.1938 μM | SANGER | ||
| NCI-H1755 | Growth Inhibition Assay | IC50=26.8841 μM | SANGER | ||
| D-423MG | Growth Inhibition Assay | IC50=27.0715 μM | SANGER | ||
| DK-MG | Growth Inhibition Assay | IC50=28.7846 μM | SANGER | ||
| NCI-H1623 | Growth Inhibition Assay | IC50=28.8342 μM | SANGER | ||
| KU-19-19 | Growth Inhibition Assay | IC50=28.995 μM | SANGER | ||
| C-33-A | Growth Inhibition Assay | IC50=29.2198 μM | SANGER | ||
| SCC-4 | Growth Inhibition Assay | IC50=30.3354 μM | SANGER | ||
| MG-63 | Growth Inhibition Assay | IC50=30.5994 μM | SANGER | ||
| LNCaP-Clone-FGC | Growth Inhibition Assay | IC50=31.4921 μM | SANGER | ||
| CAPAN-1 | Growth Inhibition Assay | IC50=31.5286 μM | SANGER | ||
| GI-ME-N | Growth Inhibition Assay | IC50=31.5353 μM | SANGER | ||
| RERF-LC-MS | Growth Inhibition Assay | IC50=32.6747 μM | SANGER | ||
| KLE | Growth Inhibition Assay | IC50=33.4334 μM | SANGER | ||
| KNS-81-FD | Growth Inhibition Assay | IC50=33.5008 μM | SANGER | ||
| DOK | Growth Inhibition Assay | IC50=34.6612 μM | SANGER | ||
| ACHN | Growth Inhibition Assay | IC50=35.1588 μM | SANGER | ||
| KYSE-520 | Growth Inhibition Assay | IC50=35.2361 μM | SANGER | ||
| SBC-5 | Growth Inhibition Assay | IC50=35.5116 μM | SANGER | ||
| NCI-H28 | Growth Inhibition Assay | IC50=35.6695 μM | SANGER | ||
| ES7 | Growth Inhibition Assay | IC50=36.2249 μM | SANGER | ||
| A172 | Growth Inhibition Assay | IC50=36.4187 μM | SANGER | ||
| UM-UC-3 | Growth Inhibition Assay | IC50=37.8746 μM | SANGER | ||
| LXF-289 | Growth Inhibition Assay | IC50=38.0047 μM | SANGER | ||
| KP-4 | Growth Inhibition Assay | IC50=38.4739 μM | SANGER | ||
| TE-1 | Growth Inhibition Assay | IC50=39.6589 μM | SANGER | ||
| G-402 | Growth Inhibition Assay | IC50=40.061 μM | SANGER | ||
| 786-0 | Growth Inhibition Assay | IC50=40.9096 μM | SANGER | ||
| K5 | Growth Inhibition Assay | IC50=41.3686 μM | SANGER | ||
| SK-N-DZ | Growth Inhibition Assay | IC50=41.3823 μM | SANGER | ||
| OVCAR-4 | Growth Inhibition Assay | IC50=41.7568 μM | SANGER | ||
| T84 | Growth Inhibition Assay | IC50=42.1263 μM | SANGER | ||
| GCIY | Growth Inhibition Assay | IC50=43.0803 μM | SANGER | ||
| BB49-HNC | Growth Inhibition Assay | IC50=43.3348 μM | SANGER | ||
| SNU-C2B | Growth Inhibition Assay | IC50=43.6436 μM | SANGER | ||
| TE-6 | Growth Inhibition Assay | IC50=43.8894 μM | SANGER | ||
| 23132-87 | Growth Inhibition Assay | IC50=44.2978 μM | SANGER | ||
| DMS-53 | Growth Inhibition Assay | IC50=44.3384 μM | SANGER | ||
| ONS-76 | Growth Inhibition Assay | IC50=44.7661 μM | SANGER | ||
| DMS-273 | Growth Inhibition Assay | IC50=44.943 μM | SANGER | ||
| COLO-824 | Growth Inhibition Assay | IC50=45.8775 μM | SANGER | ||
| DMS-114 | Growth Inhibition Assay | IC50=45.8927 μM | SANGER | ||
| YKG-1 | Growth Inhibition Assay | IC50=46.0355 μM | SANGER | ||
| RH-18 | Growth Inhibition Assay | IC50=46.3733 μM | SANGER | ||
| NCI-H1355 | Growth Inhibition Assay | IC50=46.618 μM | SANGER | ||
| NCI-H2170 | Growth Inhibition Assay | IC50=47.7584 μM | SANGER | ||
| OC-314 | Growth Inhibition Assay | IC50=47.8478 μM | SANGER | ||
| NCI-H2030 | Growth Inhibition Assay | IC50=47.8906 μM | SANGER | ||
| 22RV1 | Growth Inhibition Assay | IC50=47.9015 μM | SANGER | ||
| G-401 | Growth Inhibition Assay | IC50=48.4415 μM | SANGER | ||
| YAPC | Growth Inhibition Assay | IC50=49.8073 μM | SANGER | ||
| SW1573 | Growth Inhibition Assay | IC50=50.2435 μM | SANGER | ||
| COLO-792 | Growth Inhibition Assay | IC50=50.6237 μM | SANGER | ||
| KNS-62 | Growth Inhibition Assay | IC50=50.7508 μM | SANGER | ||
| NB5 | Growth Inhibition Assay | IC50=51.4509 μM | SANGER | ||
| CP66-MEL | Growth Inhibition Assay | IC50=51.6408 μM | SANGER | ||
| CaR-1 | Growth Inhibition Assay | IC50=52.0606 μM | SANGER | ||
| CAL-54 | Growth Inhibition Assay | IC50=52.1102 μM | SANGER | ||
| 8305C | Growth Inhibition Assay | IC50=52.315 μM | SANGER | ||
| Calu-3 | Growth Inhibition Assay | IC50=52.3733 μM | SANGER | ||
| AU565 | Growth Inhibition Assay | IC50=52.5509 μM | SANGER | ||
| CW-2 | Growth Inhibition Assay | IC50=52.8654 μM | SANGER | ||
| BEN | Growth Inhibition Assay | IC50=53.7862 μM | SANGER | ||
| NCI-H1975 | Growth Inhibition Assay | IC50=53.8966 μM | SANGER | ||
| HCT-116 | Growth Inhibition Assay | IC50=54.0327 μM | SANGER | ||
| SH-4 | Growth Inhibition Assay | IC50=54.138 μM | SANGER | ||
| NCI-H1693 | Growth Inhibition Assay | IC50=54.2103 μM | SANGER | ||
| BPH-1 | Growth Inhibition Assay | IC50=55.2892 μM | SANGER | ||
| CAMA-1 | Growth Inhibition Assay | IC50=55.8116 μM | SANGER | ||
| A388 | Growth Inhibition Assay | IC50=56.0985 μM | SANGER | ||
| C2BBe1 | Growth Inhibition Assay | IC50=56.2634 μM | SANGER | ||
| GAMG | Growth Inhibition Assay | IC50=56.5955 μM | SANGER | ||
| MKN28 | Growth Inhibition Assay | IC50=56.8013 μM | SANGER | ||
| VA-ES-BJ | Growth Inhibition Assay | IC50=56.8745 μM | SANGER | ||
| HuCCT1 | Growth Inhibition Assay | IC50=57.0492 μM | SANGER | ||
| BFTC-905 | Growth Inhibition Assay | IC50=57.2898 μM | SANGER | ||
| LS-123 | Growth Inhibition Assay | IC50=57.5668 μM | SANGER | ||
| LB996-RCC | Growth Inhibition Assay | IC50=58.0287 μM | SANGER | ||
| NCI-H1048 | Growth Inhibition Assay | IC50=58.2188 μM | SANGER | ||
| COR-L105 | Growth Inhibition Assay | IC50=58.7337 μM | SANGER | ||
| OVCAR-8 | Growth Inhibition Assay | IC50=59.1716 μM | SANGER | ||
| SK-N-FI | Growth Inhibition Assay | IC50=59.3207 μM | SANGER | ||
| MES-SA | Growth Inhibition Assay | IC50=59.4509 μM | SANGER | ||
| SCC-9 | Growth Inhibition Assay | IC50=59.4753 μM | SANGER | ||
| EFO-27 | Growth Inhibition Assay | IC50=59.943 μM | SANGER | ||
| GT3TKB | Growth Inhibition Assay | IC50=60.6048 μM | SANGER | ||
| HCC38 | Growth Inhibition Assay | IC50=61.4379 μM | SANGER | ||
| MLMA | Growth Inhibition Assay | IC50=61.6163 μM | SANGER | ||
| D-566MG | Growth Inhibition Assay | IC50=63.5224 μM | SANGER | ||
| SF295 | Growth Inhibition Assay | IC50=63.6655 μM | SANGER | ||
| ES4 | Growth Inhibition Assay | IC50=64.4719 μM | SANGER | ||
| CAKI-1 | Growth Inhibition Assay | IC50=64.5721 μM | SANGER | ||
| OAW-28 | Growth Inhibition Assay | IC50=64.9647 μM | SANGER | ||
| NCI-H460 | Growth Inhibition Assay | IC50=65.0897 μM | SANGER | ||
| JAR | Growth Inhibition Assay | IC50=65.5516 μM | SANGER | ||
| SNU-449 | Growth Inhibition Assay | IC50=65.7616 μM | SANGER | ||
| D-392MG | Growth Inhibition Assay | IC50=65.9434 μM | SANGER | ||
| EW-22 | Growth Inhibition Assay | IC50=66.395 μM | SANGER | ||
| GCT | Growth Inhibition Assay | IC50=67.0443 μM | SANGER | ||
| NOS-1 | Growth Inhibition Assay | IC50=67.6867 μM | SANGER | ||
| RH-1 | Growth Inhibition Assay | IC50=68.5559 μM | SANGER | ||
| HuH-7 | Growth Inhibition Assay | IC50=69.1002 μM | SANGER | ||
| NUGC-3 | Growth Inhibition Assay | IC50=70.9644 μM | SANGER | ||
| IST-SL1 | Growth Inhibition Assay | IC50=71.2324 μM | SANGER | ||
| SHP-77 | Growth Inhibition Assay | IC50=72.119 μM | SANGER | ||
| SW1116 | Growth Inhibition Assay | IC50=72.1407 μM | SANGER | ||
| LK-2 | Growth Inhibition Assay | IC50=72.8612 μM | SANGER | ||
| U-2-OS | Growth Inhibition Assay | IC50=73.1828 μM | SANGER | ||
| KYSE-150 | Growth Inhibition Assay | IC50=73.6118 μM | SANGER | ||
| U251 | Growth Inhibition Assay | IC50=73.8168 μM | SANGER | ||
| HT-1080 | Growth Inhibition Assay | IC50=74.2574 μM | SANGER | ||
| NCI-H1437 | Growth Inhibition Assay | IC50=74.6326 μM | SANGER | ||
| HPAF-II | Growth Inhibition Assay | IC50=74.6415 μM | SANGER | ||
| Becker | Growth Inhibition Assay | IC50=75.1105 μM | SANGER | ||
| PANC-10-05 | Growth Inhibition Assay | IC50=75.2865 μM | SANGER | ||
| TYK-nu | Growth Inhibition Assay | IC50=75.3102 μM | SANGER | ||
| SKG-IIIa | Growth Inhibition Assay | IC50=75.3341 μM | SANGER | ||
| NCI-H1993 | Growth Inhibition Assay | IC50=75.7397 μM | SANGER | ||
| S-117 | Growth Inhibition Assay | IC50=75.755 μM | SANGER | ||
| HuO9 | Growth Inhibition Assay | IC50=76.0048 μM | SANGER | ||
| CAL-51 | Growth Inhibition Assay | IC50=76.1006 μM | SANGER | ||
| BT-20 | Growth Inhibition Assay | IC50=76.2168 μM | SANGER | ||
| LB831-BLC | Growth Inhibition Assay | IC50=76.3217 μM | SANGER | ||
| LB1047-RCC | Growth Inhibition Assay | IC50=76.7619 μM | SANGER | ||
| ES8 | Growth Inhibition Assay | IC50=78.0073 μM | SANGER | ||
| UMC-11 | Growth Inhibition Assay | IC50=78.0884 μM | SANGER | ||
| NCI-H226 | Growth Inhibition Assay | IC50=78.1315 μM | SANGER | ||
| IGROV-1 | Growth Inhibition Assay | IC50=78.555 μM | SANGER | ||
| BHY | Growth Inhibition Assay | IC50=79.596 μM | SANGER | ||
| MKN45 | Growth Inhibition Assay | IC50=80.3174 μM | SANGER | ||
| IA-LM | Growth Inhibition Assay | IC50=80.3511 μM | SANGER | ||
| WM-115 | Growth Inhibition Assay | IC50=81.4114 μM | SANGER | ||
| VMRC-RCZ | Growth Inhibition Assay | IC50=81.4425 μM | SANGER | ||
| NCI-H2291 | Growth Inhibition Assay | IC50=81.6842 μM | SANGER | ||
| MCF7 | Growth Inhibition Assay | IC50=83.2897 μM | SANGER | ||
| 639-V | Growth Inhibition Assay | IC50=84.6129 μM | SANGER | ||
| RT4 | Growth Inhibition Assay | IC50=85.2403 μM | SANGER | ||
| NCI-H2405 | Growth Inhibition Assay | IC50=85.2997 μM | SANGER | ||
| CAL-33 | Growth Inhibition Assay | IC50=85.6315 μM | SANGER | ||
| BT-549 | Growth Inhibition Assay | IC50=85.9382 μM | SANGER | ||
| HT-1197 | Growth Inhibition Assay | IC50=88.1077 μM | SANGER | ||
| G-361 | Growth Inhibition Assay | IC50=88.1474 μM | SANGER | ||
| LS-411N | Growth Inhibition Assay | IC50=89.3388 μM | SANGER | ||
| HT-144 | Growth Inhibition Assay | IC50=89.5992 μM | SANGER | ||
| DJM-1 | Growth Inhibition Assay | IC50=89.8845 μM | SANGER | ||
| CAL-12T | Growth Inhibition Assay | IC50=90.7895 μM | SANGER | ||
| MKN7 | Growth Inhibition Assay | IC50=91.3551 μM | SANGER | ||
| HuP-T3 | Growth Inhibition Assay | IC50=96.1004 μM | SANGER | ||
| SK-MG-1 | Growth Inhibition Assay | IC50=96.1348 μM | SANGER | ||
| NCI-H2347 | Growth Inhibition Assay | IC50=98.1042 μM | SANGER | ||
| SW872 | Growth Inhibition Assay | IC50=100.456 μM | SANGER | ||
| COLO-829 | Growth Inhibition Assay | IC50=100.553 μM | SANGER | ||
| MC-IXC | Growth Inhibition Assay | IC50=100.615 μM | SANGER | ||
| 他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい | |||||
生物活性
| 製品説明 | PF-4708671 is a cell-permeable inhibitor of p70 ribosomal S6 kinase (S6K1 isoform) with Ki/IC50 of 20 nM/160 nM in cell-free assays, 400-fold greater selectivity for S6K1 than S6K2, and 4- and >20-fold selectivity for S6K1 than MSK1 and RSK1/2, respectively. First S6K1-specific inhibitor to be reported. | ||
|---|---|---|---|
| Targets |
|
| In Vitro | ||||
| In vitro | PF-4708671 is a piperazinyl-pyrimidine analogue and the first S6K1-specific inhibitor. PF-4708671 does not significantly inhibit the activity of the closely related S6K2 isoform or a number of other AGC kinases (Akt1, Akt2, PKA, PKCα, PKCϵ, PRK2, ROCK2, RSK1, RSK2 or SGK1) . PF-4708671 prevents the S6K1-mediated phosphorylation of S6 protein in response to IGF-1 (insulin-like growth factor 1), while having no effect upon the PMA-induced phosphorylation of substrates of the highly related RSK (p90 ribosomal S6 kinase) and MSK (mitogen- and stress-activated kinase) kinases. PF-4708671 is also found to induce phosphorylation of the T-loop and hydrophobic motif of S6K1, an effect that is dependent upon mTORC1 (mTOR complex 1). PF-4708671 does not affect activity of mTORC1. [1] | |||
|---|---|---|---|---|
| 実験結果図 | Methods | Biomarkers | 結果図 | PMID |
| Western blot | pS6 / S6 / pS6K / S6K1 / pAKT / AKT p-mTOR / mTOR / p-p70S6K / p70S6K |
|
28626016 | |
| Growth inhibition assay | Cell viability |
|
30423811 | |
化学情報
| 分子量 | 390.41 | 化学式 | C19H21F3N6 |
| CAS No. | 1255517-76-0 | SDF | Download PF-4708671 SDFをダウンロードする |
| Smiles | CCC1=CN=CN=C1N2CCN(CC2)CC3=NC4=C(N3)C=C(C=C4)C(F)(F)F | ||
| 保管 | |||
|
In vitro |
DMSO : 30 mg/mL ( (76.84 mM)； 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。) Ethanol : 8 mg/mL Water : Insoluble |
モル濃度計算器 |
|
in vivo Add solvents to the product individually and in order. |
投与溶液組成計算機 | ||||
実験計算
投与溶液組成計算機(クリア溶液)
ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）
mg/kg
g
μL
匹
ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結果：
投与溶媒濃度： mg/ml;
DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )
投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH2O，を加え完全に溶解させます。
投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。
注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。
技術サポート
ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。
他に質問がある場合は、お気軽にお問い合わせください。
* 必須
よくある質問（FAQ）
質問1:
Whether the in vivo formula "30% PEG400+0.5% Tween80+5% Propylene glycol" for S2163 is suitable for i.p. or not?
回答
The formula "30% PEG400+0.5% Tween80+5% Propylene glycol" on our website is an oral one. It is a suspension.
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