Calicheamicin - ≥98% , CAS No.108212-75-5

CAS: 108212-75-5 Cat. No.: C579375 Formula: C₅₅H₇₄IN₃O₂₁S₄ Molecular Weight: 1368.34 EC Number: 813-745-9

GRADE & PURITY ≥98%

Synonyms

Calicheamicin γ1

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

Overview

Calicheamicin is an antitumor antibiotic and is a DNA synthesis inhibitor. It also is a cytotoxic agent that causes double-strand DNA breaks.

In vitro activity:

PF-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: ~1 ng/mL) .

In vivo activity:

PF-06647263 (0.27, 0.36 mg/kg) results in significant tumor regressions in TNBC xenografts. An 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.  

Specifications

Synonyms

Calicheamicin γ1

Specifications & Purity

≥98%

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

This product requires cold chain shipping. Ground and other economy services are not available.

Action Type

INHIBITOR

Purity

≥98%

Names and Identifiers

Pubchem Sid

528770345

Isomeric SMILES

CCNC1COC(CC1OC)OC2C(C(C(OC2OC3C#CC=CC#CC4(CC(=O)C(=C3C4=CCSSSC)NC(=O)OC)O)C)NOC5CC(C(C(O5)C)SC(=O)C6=C(C(=C(C(=C6OC)OC)OC7C(C(C(C(O7)C)O)OC)O)I)C)O)O

Molecular Weight

1368.34

Reaxy-Rn

32076945

Reaxys-RN_link_address

https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=32076945&ln=

Chemical and Physical Properties

• Solubility: DMSO: 100 mg/mL (73.08 mM)