Gemcitabine

Biological Activity

Gemcitabine(LY-188011; NSC 613327) is a DNA synthesis inhibitor with IC50 of 50 nM, 40 nM, 18 nM and 12 nM in PANC1, MIAPaCa2, BxPC3 and Capan2 cells, respectively.

Product Citations

• 

  Oncol Lett. 2022 May;23(5):163.

  AK4P1 is a cancer-promoting pseudogene in pancreatic adenocarcinoma cells whose transcripts can be transmitted by exosomes
  Gemcitabine purchased from AbMole

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  Universitat Freiburg im Breisgau. 2020 Jul.

  Investigation of chemotherapy-induced non-coding RNA expression alterations in clinical breast cancer management
  Gemcitabine purchased from AbMole

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  Biosci Rep. 2020 Jul 31;40(7):BSR20200730.

  NLRP3 augmented resistance to gemcitabine in triple-negative breast cancer cells via EMT/IL-1β/Wnt/β-catenin signaling pathway
  Gemcitabine purchased from AbMole

• 

  Biosci Rep. 2020 Jul 31;40(7):BSR20200730.

  NLRP3 augmented resistance to gemcitabine in triple-negative breast cancer cells via EMT/IL-1β/Wnt/β-catenin signaling pathway
  Gemcitabine purchased from AbMole

• 

  Int J Oncol. 2020 Jan;56(1):47-68.

  Circulating non‑coding RNA‑biomarker potential in neoadjuvant chemotherapy of triple negative breast cancer?
  Gemcitabine purchased from AbMole

Customer Product Validations & Biological Datas

	Source	Biosci Rep (2020), Figure 2, Gemcitabine (Abmole Bioscience)
	Method	MTT assay for cell cytotoxicity
	Cell Lines	TNBC cell lines
	Concentrations	0, 1, 3, 5 nm
	Incubation Time	48 h
	Results	Next, the cytotoxicity in each group was monitored with MTT when the cells were treated with 0, 1, 3 and 5 nm gemcitabine and findings tended to prove that agonized NLRP3 could better resist the inhibitory effect of growing gemcitabine, in other words, higher expression of NLRP3 decreased the cytotoxicity and added to the gemcitabine resistance while inhibition of NLRP3 increased cytotoxicity in TNBCC, helping to alleviate the drug resistance

	Source	Biosci Rep (2020), Figure 1, Gemcitabine (Abmole Bioscience)
	Method	Cell culture and treatment
	Cell Lines	TNBC cell lines
	Concentrations	0, 1, 3, 5 nM
	Incubation Time	72 h
	Results	The linear graph presented the cytotoxicity at 72 h when exposed to different concentrations. It showed that highest cell viability was seen in agonist group with higher NLRP3 and lowest in antagonist group, suggesting that the higher expression of NLRP3, the less sensitive to different gemcitabine doses

	Source	Bioscience Reports (2020 Jul). Figure 1. Gemcitabine (Abmole Bioscience)
	Method	Cell culture
	Cell Lines	TNBC cell lines
	Concentrations	0, 1, 3, 5 nM
	Incubation Time	72 h
	Results	It showed that highest cell viability was seen in agonist group with higher NLRP3 and lowest in antagonist group, suggesting that the higher expression of NLRP3, the less sensitive to different gemcitabine doses

Chemical Information

Molecular Weight	263.2
Formula	C9H11F2N3O4
CAS Number	95058-81-4
Solubility (25°C)	DMSO ≥ 30 mg/mL
Storage	-20°C, protect from light, sealed

Conversion of different model animals based on BSA (PMID: 27057123)

Species	Mouse	Rat	Rabbit	Guinea pig	Hamster	Dog
Weight (kg)	0.02	0.15	1.8	0.4	0.08	10
Body Surface Area (m2)	0.007	0.025	0.15	0.05	0.02	0.5
Km factor	3	6	12	8	5	20

Animal A (mg/kg) = Animal B (mg/kg) multiplied by	Animal B Km
	Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the K_m factor for a mouse and then divide by the K_m factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Binenbaum Y, et al. Drug Resist Updat. Gemcitabine resistance in pancreatic ductal adenocarcinoma.