Gemcitabine

別名：LY-188011, NSC 613327

製品コード：S1714 純度：99.98%

Gemcitabine, a nucleic acid synthesis inhibitor, is a very potent and specific deoxycytidine analogue, used as chemotherapy. Gemcitabine induces a potent p53-dependent apoptosis.

CAS No. 95058-81-4

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 29500	国内在庫あり
50mg	JPY 22000	国内在庫あり
200mg	JPY 55500	国内在庫あり
1g	JPY 145500	国内在庫あり

代表番号: 045-509-1970\|電子メール：sales@selleck.co.jp よく尋ねられる質問

文献中Selleckの製品使用例（279）

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製品安全説明書

現在のバッチを見る：純度： 99.98%

99.98

Gemcitabine関連製品

関連ターゲット	tRNA synthetase RdRp DNA synthesis helicase ribonucleotide reductase	もっと見る
関連製品	Pidnarulex (CX-5461) SCR7 Favipiravir (T-705) RK-33 Carmofur Triapine (3-AP) B02 BMH-21 YK-4-279 Bergapten Tegafur (FT-207) Azaguanine-8 Halofuginone Adenine HCl Mizoribine Cyclocytidine HCl Thymidine APX-3330 Nedaplatin 6-Thio-dG Flupirtine maleate JH-RE-06 Pritelivir (BAY 57-1293) TK216 Amenamevir Madrasin Tubercidin BC-LI-0186 CRT0044876 PFM01 Adenine ML216	もっと見る
関連化合物ライブラリー	FDA-approved Drug Library Natural Product Library Apoptosis Compound Library DNA Damage/DNA Repair compound Library Cell Cycle compound library	もっと見る

シグナル伝達経路

DNA/RNA Synthesisシグナル伝達経路

DNA/RNA Synthesis阻害剤の選択性比較

阻害剤	Citation	tRNA synthetase	RdRp	DNA synthesis	helicase	YB-1	ribonucleotide reductase	ribonucleotide reductase	PCNA	その他
ART899	0
ART812	0
ART558	0
SU056	2					+
VV116	0		+
BC-LI-0186	1	+++
Acelarin (NUC-1031)	0			++++
Suramin sodium salt	1		++							SirT1,SirT2,Topoisomerase II
ML216	3				+
Halofuginone	11	+++								Smad3
Clevudine	1
Nedaplatin	3			✔
Triapine (3-AP)	17						✔	✔
RP-6685	0
H3B-8800	0
Basic Orange 14	0
AOH1996	0								✔
Didox	0						✔	✔
Phen-DC3 Trifluoromethanesulfonate	0				✔
Robinetin	0			✔
Metarrestin	0									PNC
Brr2 Inhibitor C9	0				✔
Triglycidyl Isocyanurate (Teroxirone)	0			✔						p53
RK-33	21				✔
Oxolinic acid	0			✔						bacterial DNA gyrase,dopamine uptake
Favipiravir (T-705)	24		✔
YK-4-279	14				✔
Blasticidin S HCl	29			✔						protein synthesis
CX-3543(Quarfloxin)	0

1. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation. 2. "✔" indicates inhibitory effect, but without specific value.

Cell Data

Cell Lines	Assay Type	Incubation Time	活性情報	PMID
SW1573	Cytotoxicity assay	72 hrs	Cytotoxicity against SW1573 cells after 72 hrs by SRB assay, IC50 = 8.3 μM.	17419604
A549	Cytotoxicity assay	72 hrs	Cytotoxicity against A549 cells after 72 hrs by SRB assay, IC50 = 13.1 μM.	17419604
OVCAR8	Antiproliferative assay	72 hrs	Antiproliferative activity against p53 deficient human OVCAR8 cells after 72 hrs by proliferative assay, IC50 = 0.0026 μM.	18469809
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	Gemcitabine, a nucleic acid synthesis inhibitor, is a very potent and specific deoxycytidine analogue, used as chemotherapy. Gemcitabine induces a potent p53-dependent apoptosis.

In Vitro
In vitro	Gemcitabine results in 50% inhibition of growth in the CCRF-CEM human leukemia cell culture assay with IC50 of 1 ng/ml. Gemcitabine combined with deoxycytidine provides about a 1000-fold decrease in biological activity. ^[1] Gemcitabine combined with C225 results in additive cytotoxic effects that increased with increasing gemcitabine concentrations in human pancreatic carcinoma L3.6pl cells. ^[2] Gemcitabine combined with Cisplatin results in synergistic effect in wild-type A2780 and cisplatin-resistant ADDP cells. ^[3]
細胞実験	細胞株	PC cells
	濃度	1 μM
	反応時間	72 h
	実験の流れ	Cells were treated with different concentrations of gemcitabine.
実験結果図	Methods	Biomarkers	結果図	PMID
	Western blot	p70S6K1 / p-S6 / HIF-1α PARP / Cleaved PARP / Cleaved caspase-3 / phopho-p38 / p38 / p-JNK / JNK / p-c-Jun		27765914
	Immunofluorescence	Bim1		27177084
	Growth inhibition assay	Cell viability		27765914

In Vivo
In Vivo	Gemcitabine combined with C225 results in growth inhibition, tumor regression, and abrogation of metastasis in L3.6pl tumors established in the pancreas of nude mice. Gemcitabine treatment alone reduces median tumor volume from 538 to 152 mm³. Gemcitabine reduces the production of vascular endothelial growth factor and interleukin 8 in gemcitabine-treated tumors. ^[2] Gemcitabine is able to dramatically and specifically reduces the number of myeloid suppressor cells found in the spleens of animals bearing large tumors with no significant reductions in CD4(+) T cells, CD8(+) T cells, NK cells, macrophages, or B cells. ^[4] Gemcitabine combined with curcumin shows significant reductions in volume (P = 0.008 versus control; P = 0.036 versus gemcitabine alone), Ki-67 proliferation index (P = 0.030 versus control), NF-kappaB activation, and expression of NF-kappaB-regulated gene products (cyclin D1, c-myc, Bcl-2, Bcl-xL, cellular inhibitor of apoptosis protein-1, cyclooxygenase-2, matrix metalloproteinase, and vascular endothelial growth factor) compared with tumors from control mice treated with olive oil only. Gemcitabine combined with Curcumin is also highly effective in suppressing angiogenesis as indicated by a decrease in CD31(+) microvessel density. ^[5]
動物実験	動物モデル	Female BALB/c nude mice
	投与量	5 mg/kg
	投与経路	i.p.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT06320301	Recruiting	Biliary Tract Cancer\|Gemox Chemotherapy	Sun Yat-Sen Memorial Hospital of Sun Yat-Sen University\|Suzhou Suncadia Biopharmaceuticals Co. Ltd.	April 1 2024	Phase 2
NCT06046794	Not yet recruiting	Cancer Of Pancreas	Institut Paoli-Calmettes	February 1 2024	Not Applicable
NCT06199466	Recruiting	Metastatic Pancreatic Cancer	M.D. Anderson Cancer Center\|280Bio Inc	January 22 2024	Phase 1
NCT06055348	Not yet recruiting	Serous Ovarian Cancer\|Advanced Ovarian Cancer	Biocity Biopharmaceutics Co. Ltd.	October 30 2023	Phase 1\|Phase 2

参考
[1] Hertel LW, et al. Cancer Res, 1990, 50(14), 4417-4422. [2] Bruns CJ, et al. Clin Cancer Res, 2000, 6(5), 1936-1948. [3] Peters GJ, et al. Semin Oncol, 1995, 22(4 Suppl 11), 72-79. [4] Suzuki E, et al. Clin Cancer Res, 2005, 11(18), 6713-6721. [5] Kunnumakkara AB, et al. Cancer Res, 2007, 67(8), 3853-3861. [6] Gu J, et al. Mol Cancer. 2022 May 10;21(1):112. + 展開

参考

+ 展開

化学情報

分子量	263.2	化学式	C₉H₁₁F₂N₃O₄
CAS No.	95058-81-4	SDF	Download Gemcitabine SDFをダウンロードする
Smiles	C1=CN(C(=O)N=C1N)C2C(C(C(O2)CO)O)(F)F
保管	powder, 4°C (in the dark) ; in solvent，-80°C (in the dark)	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	powder, 4°C (in the dark) ; in solvent，-80°C (in the dark)	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	１ケ月-20°Cin solvent

In vitro
Batch:

DMSO : 53 mg/mL ( (201.36 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。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo Batch: Add solvents to the product individually and in order.					投与溶液組成計算機
	Clear solution	5%DMSO 1 Corn oil	5.0mg/ml (19.00mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
	Clear solution	5%DMSO 1 40%PEG300 Click to order 2 5%Tween 80 Click to order 3 50%ddH2O	2.5mg/ml (9.50mM)	Taking the 1 mL working solution as an example, add 50 μL of 50 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 Corn oil	4.0mg/ml (15.20mM)	Taking the 1 mL working solution as an example, add 50 μL of 80 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 Click to order 2 5%Tween 80 Click to order 3 50%ddH2O	2.65mg/ml (10.07mM)	Taking the 1 mL working solution as an example, add 50 μL 53 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

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）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

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。

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よくある質問（FAQ）

質問1:
What is the difference between gemcitabine(S1714 ) and Gemcitabine HCl (S1149)?

回答
Gemcitabine HCl is the HCl salt form of Gemcitabine. They have the same biological activities. The free base(S1714) dissolves better in DMSO, and the hydrochloride (S1149) dissolves better in water.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):