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CP-724714 - 10mM in DMSO, high purity , CAS No.537705-08-1(DMSO)

COA

Grade & Purity:

10mM in DMSO

Cas Number: 537705-08-1(DMSO)
Molecular Weight: 469.53

In stock

Item Number

C408213

Grouped product items
SKU	Size	Availability	Price	Qty
C408213-1ml	1ml	Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!	$610.90

HER2/ErbB2 Selective Inhibitors

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Compound libraries (12325)

Basic Description

Synonyms	(E)-2-methoxy-N-(3-(4-(3-methyl-4-(6-methylpyridin-3-yloxy)phenylamino)quinazolin-6-yl)allyl)acetamide
Specifications & Purity	10mM in DMSO
Biochemical and Physiological Mechanisms	CP-724714 is a potent, selective inhibitor of HER2/ErbB2 with IC50 of 10 nM, >640-fold selectivity against EGFR, InsR, IRG-1R, PDGFR, VEGFR2, Abl, Src, c-Met etc in cell-free assays. Phase 2.
Storage Temp	Store at -80°C
Shipped In	Dry ice packs + Cold packs This product requires cold chain shipping. Ground and other economy services are not available.
Product Description	Information CP-724714 is a potent, selective inhibitor ofHER2/ErbB2withIC50of 10 nM, >640-fold selectivity against EGFR, InsR, IRG-1R, PDGFR, VEGFR2, Abl, Src, c-Met etc in cell-free assays. Phase 2. In vitro CP-724,714 is marked selectively against EGFR with IC50 of 6.4 μM. CP-724,714 is >1,000-fold less potent for IR, IGF-1R, PDGFRβ, VGFR2, abl. Src, c-Met c-jun NH2-terminal kinase (JNK)-2, JNK-3, ZAP-70, cyclin-dependent kinase (CDK)-2, and CDK-5. CP-724,714 potently reduces the EGF-induced autophosphorylation of the chimera containing the erbB2 kinase domain with IC50 of 32 nM, but is markedly less potent against EGFR in transfected NIH3T3 cells. CP-724,714 sensitively inhibits the proliferation of erbB2-amplified cells including BT-474 and SKBR3, with IC50 of 0.25 and 0.95 μM. CP-724,714 induces the accumulation of cells in G1 phase and a marked reduction in S-phase in BT-474 cells at 1 μM. CP-724,714 likely exerts its hepatotoxicity via both hepatocellular injury and hepatobiliary cholestatic mechanisms. CP-724,714 displays inhibition of cholyl-lysyl fluorescein and taurocholate (TC) efflux into canaliculi in cryopreserved and fresh cultured human hepatocytes, respectively. CP-724,714 inhibits TC transport in membrane vesicles expressing human bile salt export pump with IC50 of 16 μM and inhibits the major efflux transporter in bile canaliculi, MDR1, with IC50 of ~28 μM. In vivo CP-724,714 (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 weight loss or mortality. CP-724,714 also has great antitumor activity in MDA-MB-453, MDA-MB-231, LoVo (colon), and Colo-205 (colon) xenografts. Furthermore, CP-724,714 (30 or 100 mg/kg) reduces the extracellular signal–regulated kinase and Akt phosphorylation in BT-474 xenografts. Cell Data cell lines： Concentrations：0.1 nM - 10 μM. Incubation Time：6 to 7 days. Powder Purity:≥99%

Names and Identifiers

Smiles	COCC(=O)NC/C=C/C1=CC=C2N=CN=C(NC3=CC=C(OC4=CC=C(C)N=C4)C(=C3)C)C2=C1
Molecular Weight	469.53

Certificates（CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):

Analytical Chart:

Chemical and Physical Properties

Solubility	Solubility (25°C) In vitro DMSO: 5 mg/mL warmed with 50ºC Water: bath (19.66 mM); Water: Insoluble; Ethanol: Insoluble;

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