AZD8931 (Sapitinib) with factory price CAS NO.848942-61-0

FOB Price: USD: 100.00-200.00 /Gram Get Latest Price
Min.Order: 1 Gram
Payment Terms: T/T,Other
Available Specifications:
99%(1-10)Gram100/Gram1USD99%(10-50)Gram200/Gram10USD

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AZD8931 (Sapitinib) supplier in China
848942-61-0
Sapitinib factory

Quick Details

ProName: AZD8931 (Sapitinib) with factory price
CasNo: 848942-61-0
Molecular Formula: C23H25ClFN5O3
Appearance: solid
Application: API，Pharmaceutical intermediates
DeliveryTime: 1-2days after the payment
PackAge: 1g to 1kg or as your request
Port: Shanghai, Shenzhen
ProductionCapacity: 500 Kilogram/Month
Purity: 99%
Storage: 2℃-8℃
Transportation: DHL, UPS, FEDEX EMS or as your request
LimitNum: 1 Gram
Residue on Ignition: ≤0.01
Heavy Metal: ≤0.02
Valid Period: 3years

Superiority

We are a leading provider and manufacturer of pharmaceutical and chemical products. Mainly involves API, pharmaceutical intermediates, polypeptide, and natural extract etc。We are capable to supply you with any quantity of the mentioned products with fast and secure delivery to any of your desire address .and any part of world with good prices. . We export products to USA, Canada, Mexico, Brazil, United Kingdom, Japan, Russia, Germany, India, South Africa, Malta, Egypt, Armenia, Australia, Philippines, Belgium, Netherlands, Denmark, Bosnia and Herzegovina ect.

We work hard for getting sustainable development, and making contributions to our society and health industry of human being. Upholding international QC idea, we follow customers’ demands closely, and strive to offer customers stable qualities and excellent service. Through improving comprehensive strength continuously, we are working hard for get sustainable development! We persist in the management policy of People Oriented, and devote ourselves to providing the best products and services. The quality is the future market, the goodwill is the invisible market, the satisfaction of the customers is the eternal market. To center around the customers, providing the first-class products and services. To be guided by the market, create the perfect production and supply system. We welcome all kinds of cooperation with the friends all over the world on the fundamental business principle of "equality, mutual benefit and friendly cooperation”.

Process Capability : After-sale Service : We guarantee good quality products. . 100% refunded if parcel is not delivered or poor quality.

Details

we could support you:

1. best quality products;

2. competitive price in china market,

3. safe and fast shipping;

4. professional technical support;

5. samples order is welcomed

6. HNMR and HPLC will be offered after the order.

We are insisting on the tenet of "quality first, customer top, speed supreme, excellent quality and reasonable price", we would like to cooperate with you!

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Sapitinib (Synonyms: AZD-8931)

Description

Sapitinib (AZD-8931) is a reversible, ATP competitive EGFR inhibitor of with IC₅₀s of 4, 3 and 4 nM for EGFR, ErbB2 and ErbB3 in cells, respectively.

IC₅₀ & Target^[1]

EGFR

4 nM (IC₅₀)

ErbB2

3 nM (IC₅₀)

HER3

4 nM (IC₅₀)

In Vitro

AZD8931 shows potent inhibitory effect on erbB2 in the ligand-independent MCF-7 cl24 cells, with IC₅₀ of 59 nM^[1]. AZD8931 (1 μM) has no significant effect on EGFR expression level, but significantly inhibits phosphorylation of Akt in a time- and dose-dependent manner in both SUM149 and FC-IBC-02 cells. AZD8931 (0.01, 0.1, 1, or 2 μM) inhibits proliferation and induces apoptosis in human IBC cells^[2]. At the cellular level, AZD8931 inhibits EGF-stimulated phosphorylation of EGFR in the KB cell line (IC₅₀: 4 nM) and heregulin-stimulated phosphorylation of HER2 (IC₅₀: 3 nM) and HER3 (IC₅₀: 4 nM) in the MCF-7 cell line. However, AZD8931 exhibits no CYP P450 inhibition (IC₅₀ > 10 μM against 1A2, 2C9, 2C19, 2D6, and 3A4)^[3].

In Vivo

AZD8931 (6.25-50 mg/kg, p.o.) significantly inhibits BT474c (breast), Calu-3 (NSCLC), LoVo (colorectal), FaDu (SCCHN), and PC-9 (NSCLC) tumor xenograft growth. AZD8931 is active in xenograft tumor models responsive to EGFR inhibition alone (LoVo and PC-9) or EGFR or erbB2 inhibition (BT474c, Calu-3, and FaDu). AZD8931 causes pharmacodynamic changes in proliferation and apoptosis markers in human tumor xenograft models^[1]. AZD8931 (25 mg/kg, p.o.) significantly inhibits the growth of SUM149 and FC-IBC-02 cells in vivo in SCID mice^[2]. AZD8931 displays favorable oral pharmacokinetics in rat and dog (low clearance and good bioavailability) and low human hepatocyte turnover (Clint < 4.5 μL/min/106 cells). In nude mouse after oral administration at 50 mg/kg, AZD8931 shows improved exposure, and at at 100 mg/kg oral dose once daily, it shows potent tumor growth inhibition activity in the LoVo mouse xenograft model^[3].

Molecular Weight

473.93

Formula

C??H??ClFN?O?

CAS No.

848942-61-0

SMILES

O=C(CN1CCC(OC2=CC3=C(NC4=CC=CC(Cl)=C4F)N=CN=C3C=C2OC)CC1)NC

Shipping

Room temperature in continental US; may vary elsewhere

Storage