Etoposide (VP-16-213)

Biological Activity

Etoposide (VP-16-213) is a semisynthetic derivative of podophyllotoxin, which inhibits DNA synthesis via topoisomerase II inhibition activity. Etoposide caused an increase in the mean fluorescence intensity of FasR in both subclones, and an induction of FasL in the ES subclone. Etoposide phosphate is rapidly absorbed and converted to etoposide. Bioavailability averages 68% at doses up to 150 mg/m2/day.

Product Citations

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  Chem Biol Drug Des. 2022 Jan;99(1):92-102.

  Identification of novel topoisomerase II alpha inhibitors by virtual screening, molecular docking, and bioassay
  Etoposide (VP-16-213) purchased from AbMole

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  BMC Biol. 2021 May 20;19(1):108.

  Very long intergenic non-coding (vlinc) RNAs directly regulate multiple genes in cis and trans
  Etoposide (VP-16-213) purchased from AbMole

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  Sci Rep. 2020 Feb 4;10(1):1794.

  A CRISPR/Cas13-based Approach Demonstrates Biological Relevance of Vlinc Class of Long Non-Coding RNAs in Anticancer Drug Response
  Etoposide (VP-16-213) purchased from AbMole

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  Nat Commun. 2019 Dec 20;10(1):5799.

  Novel approach reveals genomic landscapes of single-strand DNA breaks with nucleotide resolution in human cells.
  Etoposide (VP-16-213) purchased from AbMole

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  Gene. 2015 May 10;117-27.

  Identification of ADAM10 and ADAM17 with potential roles in the spermatogenesis of the Chinese mitten crab, Eriocheir sinensis.
  Etoposide (VP-16-213) purchased from AbMole

Customer Product Validations & Biological Datas

	Source	Gene (2015) . Figure .etoposide (Abmole, Shanghai, China)
	Method	Real time PCR and Western blot
	Cell Lines	tissue(testis)
	Concentrations	0, 30, 60, 90, 120 μM
	Incubation Time	0, 6, 12, 18, and 24 h
	Results	"Es-ADAM10 may be involved in the defense process in vivo at low etoposide concentrations, by the inhibition of spermatid apoptosis. However, Es-ADAM10 might also participate in the regulation of sperm quality. The Es-ADAM10 protein accumulated with etoposide concentration increasing (Fig. 8B). In addition, Es-ADAM10 reached peak at both the mRNA (Fig. 8C) and protein (Fig. 8D) levels after 12 h with 90 μM etoposide, indicating that etoposide induced EsADAM10 in a time- and concentration-dependent manner."

Chemical Information

Molecular Weight	588.56
Formula	C29H32O13
CAS Number	33419-42-0
Solubility (25°C)	DMSO 42 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] Chyuan-Chuan Wu, et al. Structural basis of type II topoisomerase inhibition by the anticancer drug etoposide

[2] K R Hande. Etoposide: four decades of development of a topoisomerase II inhibitor

[3] N C Phillips. Oral etoposide

[4] R A Fleming, et al. Etoposide: an update

[5] K R Hande. Etoposide pharmacology