D4-abiraterone

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D4-abiraterone
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Cat #: V32637 CAS #: 154229-21-7 Purity ≥ 99%

Description: D4-abiraterone is an active metabolite of abiraterone Δ4-Abiraterone (D4A) which is a CYP17A1 inhibitor and an androgen receptor antagonist (IC50 of 5.3 nM). Abiraterone (formerly CB-7598; Zytiga) is an approved anticancer medication acting as an irreversible and selective CYP17 inhibitor.

References: Li Z, et al. Conversion of abiraterone to D4A drives anti-tumour activity in prostate cancer. Nature. 2015 Jul 16;523(7560):347-51.

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Molecular Weight (MW)347.49
Molecular FormulaC24H29NO
CAS No.154229-21-7
SMILES CodeO=C1CC[C@@]2(C)C(CC[C@]3([H])[C@]2([H])CC[C@@]4(C)[C@@]3([H])CC=C4C5=CN=CC=C5)=C1
SynonymsD4A; CB 7627; Δ4-Abiraterone; Abiraterone D4A metabolite; D4-abiraterone;
ProtocolIn VitroD4-abiraterone (D4A ) (10 mM) nearly completely blocks conversion from D4-androstenedione (AD) to 5α-androstanedione and other 5α-reduced androgens. The affinity of D4-abiraterone for mutant (expressed in LNCaP, half-maximum inhibitory concentration (IC50=5.3 nM)) and wild type (expressed in LAPC4, IC50=7.9 nM) androgen receptor (AR) is greater than that of abiraterone (Abi) (IC50=418 and >500 nM, respectively). Compare with Abi, D4-abiraterone clearly better suppresses PSA, TMPRSS2 and FKBP5 expression in LNCAP, LAPC4 and C4-2 cell lines. D4-abiraterone also inhibits AR target gene expression in a dose-dependent manner.
In VivoD4-abiraterone (D4A) is tenfold more potent than abiraterone (Abi) in blocking conversion from dehydroepiandrosterone (DHEA) by 3β-hydroxysteroid dehydrogenase (3βHSD) to D4-androstenedione (AD) in LNCaP and VCaP xenografts. 0.1 μM D4-abiraterone is equivalent to 1 μM Abi for blocking AD accumulation at 48 h in both LNCaP and VCaP xenografts. Progression is significantly delayed in the D4-abiraterone group compare with the Abi acetate group (P=0.011). D4-abiraterone treatment increases progression-free survival compare with Abi acetate.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Preparing Stock Solutions
Solvent volume to be added Mass (the weight of a compound)
Mother liquor concentration 1mg5mg10mg20mg
1mM2.8778 mL14.3889 mL28.7778 mL57.5556 mL
5mM0.5756 mL2.8778 mL5.7556 mL11.5111 mL
10mM0.2878 mL1.4389 mL2.8778 mL5.7556 mL
20mM0.1439 mL0.7194 mL1.4389 mL2.8778 mL
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The dilution calculator equation
Concentration(start) × Volume(start) = Concentration(final) × Volume(final)

This equation is commonly abbreviated as: C1 V1 = C2 V2

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Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals
Step Two: Enter the in vivo formulation
%DMSO + % + %Tween 80 + %ddH2O

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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid concentration mg/mL) ,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation: Take µL DMSO master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH2O,mix and clarify.
Note:
  • (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
  • (2) Be sure to add the solvent(s) in order.