AZD8931 (Sapitinib) 848942-61-0

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Molecular Weight:

473.93 AZD8931 is a reversible, ATP competitive inhibitor of EGFR, ErbB2 and ErbB3 with IC50 of 4 nM, 3 nM and 4 nM, more potent than Gefitinib or Lapatinib against NSCLC cell, 100-fold more selective for the ErbB family than MNK1 and Flt. Phase 2.


Biological Activity


AZD8931 shows different potency to NSCLC and SCCHN cell lines. AZD8931
has high sensitivity to PC-9 cells (EGFR activating mutation) with GI50
of 0.1 nM and low activity to NCI-1437 cells with GI50 above 10 μM.
AZD8931 exhibits more potency against phospho-EGFR, phospho-erbB2 and
phospho-erbB3 than either lapatinib or gefitinib in PE/CA-PJ41,
PE/CA-PJ49, DOK and FaDu cells.


AZD8931 reveals antitumor activity in BT474c, Calu-3, LoVo, FaDu and
PC-9 xenografts. AZD8931 could reduce p-Akt, Ki67 expression and p-ERK
in BT474c xenografts following acute treatment. AZD8931 also causes
induction of the M30 Apoptosis marker. Furthermore, AZD8931 shows
greater proapoptotic effect compared with gefitinib and lapatinib in
LoVo xenografts.


Isolated kinase assays


The intracellular kinase domains of human EGFR and erbB2 are cloned and
expressed in the baculovirus/Sf21 system. The inhibitory activity of
AZD8931 is determined with ATP at Km concentrations (0.4 mM for erbB2
and 2 mM for EGFR) using the ELISA method.


Method






To determine the antiproliferative activity against cell lines grown
in vitro, AZD8931 is tested in a panel of NSCLC and SCCHN cell lines.
Cells are incubated for 96 hours with AZD8931 (0.001-10 μM). Viable cell
number is determined by 4 hours of incubation with MTS Colorimetric
Assay reagent and absorbance measured at 490 nm on a spectrophotometer.






Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

Species	Baboon	Dog	Monkey	Rabbit	Guinea pig	Rat	Hamster	Mouse
Weight (kg)	12	10	3	1.8	0.4	0.15	0.08	0.02
Body Surface Area (m2)	0.6	0.5	0.24	0.15	0.05	0.025	0.02	0.007
Km factor	20	20	12	12	8	6	5	3

Animal A (mg/kg) = Animal B (mg/kg) multiplied by	Animal B Km
	Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×	mouse Km(3)	= 11.2 mg/kg
	rat Km(6)

Chemical Information

Molecular Weight (MW)	473.93
Formula	C23H25ClFN5O3
CAS No.	848942-61-0

Storage	3 years -20℃Powder
	6 months-80℃in solvent (DMSO, water, etc.)
Synonyms

Solubility (25°C) *	In vitro	DMSO	40 mg/mL (84.4 mM)
		Water	<1 mg/mL (
		Ethanol	<1 mg/mL (
	In vivo	30% PEG400/0.5% Tween80/5% propylene glycol	5 mg/mL
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Name	2-(4-(4-(3-chloro-2-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)piperidin-1-yl)-N-methylacetamide

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