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[CAS NO. 122111-03-9] Gemcitabinehydrochloride

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Catalog:	HY-B0003
Brand:	MCE
CAS:	122111-03-9

Overview

MDL	MFCD01735988
Molecular Weight	299.66
Molecular Formula	C9H12ClF2N3O4
SMILES	O[C@H]1C(F)(F)[C@H](N2C(N=C(N)C=C2)=O)O[C@@H]1CO.Cl

For research use only. We do not sell to patients.

80 Publications Citing Use of MCE

[1]Nature. 2019 Oct;574(7777):264-267.
[2]Cell Res. 2020 Jul;30(7):574-589.
[3]Adv Mater. 2021 May;33(18):e2100949.
[4]Gastroenterology. 2021 Nov;161(5):1601-1614.e23.
[5]Sci Transl Med. 2021 Jan 20;13(577):eaba7401.
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[10]Theranostics. 2021 Mar 24;11(12):5650-5674.
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[12]Br J Pharmacol. 2021 Jun;178(12):2496-2515.
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Summary

Gemcitabine Hydrochloride (LY 188011 Hydrochloride) is a pyrimidine nucleoside analog antimetabolite and an antineoplastic agent. Gemcitabine Hydrochloride inhibits DNA synthesis and repair, resulting in autophagy and apoptosis ^[1] ^[2] .

IC50 & Target

DNA synthesis ^[1]

In Vitro

Gemcitabine Hydrochloride (purchased from MedChem Express, 0.003-1 μM; 3 days) kills both mouse and human senescent cells effectively and potently ^[4] .
Gemcitabine Hydrochloride inhibits the growth of BxPC-3, Mia Paca-2, PANC-1, PL-45 and AsPC-1 cells with IC ₅₀ s of 37.6, 42.9, 92.7, 89.3 and 131.4 nM, respectively ^[1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay ^[4]

Cell Line:	Non-senescent and replication-induced senescent new born dermal fibroblasts (NBFs)
Concentration:	0.003, 0.01, 0.03, 0.1, 0.3, 1 μM
Incubation Time:	3 days
Result:	Killed replication-induced senescent NBFs for 3 days with 11.0% cell viability.

In Vivo

Gemcitabine Hydrochloride can be administered via endotracheal spray in rats without marked toxicity with a maximum tolerated dose of 4 mg/kg once a week for 9 weeks. The toxicity of Gemcitabine is lower via lung than oral administration at dosages of 2, 4, and 6 mg/kg ^[2] .
Treatment of the LSL-Kras ^G12D/+ ; LSL-Trp53 ^R172H ; Pdx-1-Cre mice with either Gemcitabine (50 mg/kg, i.p.) or the combination DMAPT/Gemcitabine Hydrochloride significantly increases the median survival time by more than 30 days compared to the placebo group (254.5 or 255 days vs. 217.5 days, respectively) ^[3] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture and light

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility

In Vitro:

H ₂ O : 33.33 mg/mL ( 111.23 mM ; Need ultrasonic)

DMSO : 25 mg/mL ( 83.43 mM ; ultrasonic and warming and heat to 60°C)

DMF : 2.5 mg/mL ( 8.34 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.3371 mL	16.6856 mL	33.3712 mL
5 mM	0.6674 mL	3.3371 mL	6.6742 mL
10 mM	0.3337 mL	1.6686 mL	3.3371 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: PBS

Solubility: 60 mg/mL (200.23 mM); Clear solution; Need ultrasonic
2.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.08 mg/mL (6.94 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.08 mg/mL (6.94 mM); Clear solution
4.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.08 mg/mL (6.94 mM); Clear solution

* All of the co-solvents are available by MCE.

References

[1] Wang H, et al. Enhanced efficacy of Gemcitabine by indole-3-carbinol in pancreatic cell lines: the role of human equilibrativenucleoside transporter 1. Anticancer Res. 2011 Oct;31(10):3171-80
[2] Gagnadoux F, et al. Safety of pulmonary administration of gemcitabine in rats. J Aerosol Med. 2005 Summer;18(2):198-206
[3] Lou M, et al. Physical interaction between human ribonucleotide reductase large subunit and thioredoxin increases colorectal cancer malignancy. J Biol Chem. 2017 Jun 2;292(22):9136-9149.
[4] Yip-Schneider MT, et al. Dimethylaminoparthenolide and Gemcitabine: a survival study using a genetically engineered mouse model of pancreatic cancer. BMC Cancer. 2013 Apr 17;13:194.

Synonyms

Cytidine, 2′-deoxy-2′,2′-difluoro-, hydrochloride (1:1)

Cytidine, 2′-deoxy-2′,2′-difluoro-, monohydrochloride

LY 188011 hydrochloride

Gemcitabine hydrochloride

Gemzar

Gemsar

Gemcitera

GEMORAL

2′-Deoxy-2′,2′-difluorocytidine monohydrochloride

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