Powder: -20°C for 3 years | In solvent: -80°C for 1 year
CP-724714 (CP724714) is an effective and selective HER2/ErbB2 inhibitor (IC50: 10 nM), <640-fold selectivity against EGFR, Abl, InsR, PDGFR, IRG-1R, Src, VEGFR2, c-Met etc.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 37.00 | |
2 mg | In stock | $ 53.00 | |
5 mg | In stock | $ 87.00 | |
10 mg | In stock | $ 159.00 | |
25 mg | In stock | $ 287.00 | |
50 mg | In stock | $ 477.00 | |
100 mg | In stock | $ 695.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 91.00 |
Description | CP-724714 (CP724714) is an effective and selective HER2/ErbB2 inhibitor (IC50: 10 nM), >640-fold selectivity against EGFR, Abl, InsR, PDGFR, IRG-1R, Src, VEGFR2, c-Met etc. |
Targets&IC50 | HER2:10 nM, ErbB2:10 nM |
In vitro | CP-724714 is obvious selectively against EGFR (IC50: 6.4 μM). CP-724714 is >1,000-fold less potent for IGF-1R, IR, VGFR2, PDGFRβ, Src, ZAP-70, JNK-2/3, and CDK-2/5. CP-724714 markedly reduces the EGF-induced autophosphorylation of the chimera containing the erbB2 kinase domain (IC50: 32 nM). CP-724714 inhibits the proliferation of erbB2-amplified cells including BT-474 (IC50: 0.25 μM) and SKBR3 (IC50: 0.95 μM). CP-724714 (1 μM) induces the accumulation of cells in G1 phase and a marked reduction in S-phase in BT-474 cells. CP-724714 inhibits TC transport in membrane vesicles expressing human bile salt export pump (IC50: 16 μM) and inhibits the major efflux transporter in bile canaliculi, MDR1 (IC50: 28 μM). |
In vivo | CP-724714 (25 mg/kg) is rapidly absorbed after p.o. administration and causes reduction of tumor erbB2 receptor phosphorylation after dosing in FRE-erbB2 or BT-474 xenografts. CP-724,714 induces apoptosis in FRE-erbB2 xenograft-bearing (s.c.) mice and shows 50% tumor growth inhibition at 50 mg/kg, without mortality or weight loss. In MDA-MB-453, MDA-MB-231, LoVo (colon), and Colo-205 (colon) xenografts, CP-724714 also has great antitumor activity. In BT-474 xenografts, CP-724714 (30/100 mg/kg) reduces the extracellular signal-regulated kinase and Akt phosphorylation. |
Synonyms | CP724714, CP 724714 |
Molecular Weight | 469.54 |
Formula | C27H27N5O3 |
CAS No. | 383432-38-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 55 mg/mL (117.14 mM)
You can also refer to dose conversion for different animals. More
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CP-724714 383432-38-0 Angiogenesis Apoptosis JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR mice CP724714 Epidermal growth factor receptor autophosphorylation athymic inhibit cycle HER1 ErbB-1 Inhibitor oral cell CP 724714 selective inhibitor