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Calicheamicin

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Calicheamicin
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Size Price Stock
100mg$5250Check With Us
200mg$7875Check With Us
500mg$13250Check With Us
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Cat #: V17445 CAS #: 108212-75-5 Purity ≥ 98%

Description: Calicheamicin, formerly known as Calicheamicin gamma(1,I) or Calichemicin gamma1, is an potent enediyne antitumor antibiotics derived from the bacterium Micromonospora echinospora.

References: Damelin M, et al. Anti-EFNA4 Calicheamicin Conjugates Effectively Target Triple-Negative Breast and Ovarian Tumor-Initiating Cells to Result in Sustained Tumor Regressions. Clin Cancer Res. 2015 Sep 15;21(18):4165-73

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Molecular Weight (MW)1368.35
Molecular FormulaC55H74IN3O21S4
CAS No.108212-75-5
SMILES CodeO=C(S[C@@H]1[C@@H](C)O[C@@H](ON[C@@H]2[C@@H](C)OC(O[C@@H](C#C/C=C\C#C[C@@]3(O)C4)C(/C3=C\CSSSC)=C(NC(OC)=O)C4=O)[C@H](O[C@H]5C[C@H](OC)[C@@H](NCC)CO5)[C@H]2O)C[C@@H]1O)C6=C(OC)C(OC)=C(O[C@H]7[C@H](O)[C@H](OC)[C@@H](O)[C@H](C)O7)C(I)=C6C
SynonymsCalichemicin gamma1; Calicheamicin gamma(1)I; Calicheamicin; Calicheamicin gamma(1,I);
ProtocolIn VitroPF-06647263 (anti-EFNA4-ADC) is generated via conjugation of hE22 lysine residues to the AcButDMH-N-Ac-calicheamicin-γ1 linker-payload with an average drug-to-antibody ratio (DAR) of 4.6. PF-06647263 elicits antigen- and concentration-dependent cytotoxicity, as exposure to PF-06647263 for 96 hours results in cell death (EC50= appr 1 ng/mL).
In VivoAn ADC comprising a humanized anti-EFNA4 monoclonal antibody conjugated to the DNA-damaging agent calicheamicin achieves sustained tumor regressions in both TNBC and ovarian cancer PDX in vivo. PF-06647263 (0.27, 0.36 mg/kg) results in significant tumor regressions in TNBC xenografts.
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
1mM0.7308 mL3.6540 mL7.3081 mL14.6161 mL
5mM0.1462 mL0.7308 mL1.4616 mL2.9232 mL
10mM0.0731 mL0.3654 mL0.7308 mL1.4616 mL
20mM0.0365 mL0.1827 mL0.3654 mL0.7308 mL
Quality Control Documentation
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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
Calculation Results:
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.