Research Area
Product Type
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CP-724714 Chemical Structure
BIBW2992 (Afatinib)
BIBW2992 (Afatinib, Tomtovok, Tovok) irreversibly inhibits EGFR/HER2 including EGFRwt, EGFR L858R , EGFR L858R/T790M and HER2 with IC50 of 0.5 nM, 0.4 nM, 10 nM, 14 nM, respectively.
CI-1033 (Canertinib)
CI-1033 is a potent tyrosine kinase inhibitor of EGFR and erbB2 with IC50 of 1.5 nM and 9.0 nM, respectively.
Lapatinib Ditosylate (Tykerb)
Lapatinib (Tyverb, GW-572016, GW-2016) is a potent purified EGFR and ErbB-2 inhibitor with IC50 of 10.2 and 9.8 nM, respectively.
BMS-599626 (AC480)
BMS-599626 (AC480) is a highly selective pan-HERKinase inhibitor with IC50 of 20 and 30 nM for the inhibition of HER1and HER2, respectively.
CUDC-101
CUDC-101 is a potent multitargeted HDAC, EGFR and HER2 inhibitor with IC50 of 4.4, 2.4, and 15.7 nM, respectively.
Neratinib (HKI-272)
Neratinib (HKI-272) is an orally available, irreversible tyrosine kinase inhibitor with IC50 of 59 nM and 92 nM for HER2 and EGFR, respectively.
AZD8931
AZD8931 is a novel potent reversible small molecule epidermal growth factor receptor, ERBB2 (HER2) and ERBB3 inhibitor with an IC50 of 4, 3, 4 nM, respectively.
AV-412
AV-412 is a second-generation, orally bioavailable dual EGFR/HER2 tyrosine kinase inhibitor.
Arry-380
ARRY-380 is an orally bioavailable, potent, selective, small-molecule tyrosine kinase HER2 inhibitor with an IC50 of 8 nM.
Linifanib (ABT-869)
Linifanib (ABT869) is a structurally novel, potent RTK and VEGF and PDGF receptor families inhibitor for, PDGFR-β, KDR, and CSF-1R, with IC50 of 0.2 nM, 2 nM, 4 nM, and 7 nM, respectively.
Biological Activity
CP-724714 is an orally available, small molecule, potent HER-2 tyrosine kinase inhibitor under development for the treatment of advanced HER2-overexpressing cancers. [1]
It inhibits HER2-chimera phosphorylation with an IC50 of 15 ng/ml (32 nM), and is＞500-fold selective for HER2 relative to other kinases (e.g. EGFR, PDGFR, IGF-1R, VEGFR-2, abl, src). Antitumor activity of CP-724714 was observed in murine xenografts of human adenocarcinomas of breast (BT-474 and MDAMB-453), pancreas (Panc-1), lung (Calu-3), and ovary (SKOV-3). [1,3]
Additionally, CP-724714 showed a favorable nonclinical toxicity profile with no apparent effects on cardiac tissue. On the basis of these promising preclinical results, CP-724714 was advanced to phase I clinical trials and is potentially another option for women with Her2-driven breast cancer. [2,3]
References on CP-724714
- [1] Cancer Res 2007;67:9887-9893
- [2] Clin Cancer Res 2007;13:1238-1245
- [3] Cancer Chemother Pharmacol 2008;62:97–109
Product Information
| Molecular Weight (WM): | 469.53 |
|---|---|
| Formula: | C27H27N5O3 |
| CAS No.: | 537705-08-1 |
| Synonyms: |
N/A
|
| Dissolve in (25°C): | DMSO ≥94mg/mL |
| Water <1mg/mL | |
| Ethanol ≥94mg/mL | |
| Storage: | 2 years-20°CPowder |
| 1 week-4°Cin DMSO | |
| 1 month-80°in DMSO |
Quality Control & MSDS
Research Area
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After starved in primary serum, rat Schwann cells was stimulated for 15 minutes with a soluble form of neuregulin 1 type III to activate ErbB2. Activity of ErbB2 was determined by phosphorylation on Tyr1248. CP-724714 was applied at different concentrations, but achieved strong RTK inhibition already at very low concentrations. - After starved in primary serum, rat Schwann cells was stimulated for 15 minutes with a soluble form of neuregulin 1 type III to activate ErbB2. Activity of ErbB2 was determined by phosphorylation on Tyr1248. CP-724714 was applied at different concentrations, but achieved strong RTK inhibition already at very low concentrations.
Data independently produced by Reto Baumann from ETH Zurich CP-724714 purchased from Selleck
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Click to enlarge
For MTT assays, cells (2,000 ~ 5,000 cells/well) were subcultured into 96-well plates according to their growth properties. Cell proliferation was assayed at 72 hr after treatment of CP-724714 by adding 20 μl of 5 mg/ml 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) solution per 100 μl of growth medium. After incubating for 3-4 h at 37°C, the media were removed and 150 µl/well of MTT solvent (either absolute DMSO or isopropanol containing 4 mM HCl and 0.1% Nonidet-40) was added to dissolve the formazan.
For MTT assays, cells (2,000 ~ 5,000 cells/well) were subcultured into 96-well plates according to their growth properties. Cell proliferation was assayed at 72 hr after treatment of CP-724714 by adding 20 μl of 5 mg/ml 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) solution per 100 μl of growth medium. After incubating for 3-4 h at 37°C, the media were removed and 150 µl/well of MTT solvent (either absolute DMSO or isopropanol containing 4 mM HCl and 0.1% Nonidet-40) was added to dissolve the formazan.
Data independently produced by Dr. Yong-Weon Yi from Georgetown University Medical Center---CP-724714 purchased from Selleck. CP-724714 purchased from Selleck
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| After starved in primary serum, rat Schwann cells was stimulated for 15 minutes with a soluble form of neuregulin 1 type III to activate ErbB2. Activity of ErbB2 was determined by phosphorylation on Tyr1248. CP-724714 was applied at different concentrations, but achieved strong RTK inhibition already at very low concentrations. |
Data independently produced by Reto Baumann from ETH Zurich
For MTT assays, cells (2,000 ~ 5,000 cells/well) were subcultured into 96-well plates according to their growth properties. Cell proliferation was assayed at 72 hr after treatment of CP-724714 by adding 20 μl of 5 mg/ml 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) solution per 100 μl of growth medium. After incubating for 3-4 h at 37°C, the media were removed and 150 µl/well of MTT solvent (either absolute DMSO or isopropanol containing 4 mM HCl and 0.1% Nonidet-40) was added to dissolve the formazan. |
Data independently produced by Dr. Yong-Weon Yi from Georgetown University Medical Center---CP-724714 purchased from Selleck.
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