AZ20 1233339-22-4

.cp_wz table {border-top: 1px solid #ccc;border-left:1px solid #ccc; } .cp_wz table td{border-right: 1px solid #ccc; border-bottom: 1px solid #ccc; padding: 5px 0px 0px 5px;} .cp_wz table th {border-right: 1px solid #ccc;border-bottom: 1px solid #ccc; padding: 5px 0px 0px 5px;}


Molecular Weight: 412.51 AZ20 is a novel potent and selective inhibitor of ATR kinase with IC50 of 5 nM, 8-fold selectivity over mTOR.




AZ20 shows good selectivity against all of the PI3K isoforms together with ATM and DNA-PK. In vitro, AZ20 decreases pChk1 Ser345, pChk1 Ser317 and pChk1 Ser296
levels in a concentration-dependent manner. Prolonged exposure with AZ20
increases γH2AX pan-nuclear staining, indicative of replication stress.
This is associated with S-phase arrest and increase in phospho-histone
H3. AZ20 induces growth inhibition and cell death in vitro and its
profile of activity is distinct from other cytotoxic agents. The
cytotoxic effect of AZ20 can be increased in combination with the
selective ATM inhibitor KU-60019.


Female nude mice bearing LoVo tumors are treated with AZ20 orally at a
dose of 25 mg/kg twice daily or 50 mg/kg once daily for 13 days, led to
significant tumor growth inhibition. This is associated
with a persistent elevation of γH2AX pan-nuclear staining in xenograft
tissue, but a transient increase in mouse bone marrow at therapeutic
doses, suggesting a favourable therapeutic index. AZ20 is
assessed for drug−drug interaction (DDI) potential specifically from
inhibition of cytochrome P450 enzymes. AZ20 is found to inhibit the
cytochrome 3A4-mediated Metabolism of midazolam by 50% at 10 μM. AZ20
has respectable bioavailability in a low dose rat PK study.


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)	412.51
Formula	C21H24N4O3S
CAS No.	1233339-22-4

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

Solubility (25°C) *	In vitro	DMSO	83 mg/mL (201.2 mM)
		Water	<1 mg/mL (
		Ethanol	3 mg/mL (7.27 mM)
* <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	1H-Indole, 4-[4-[(3R)-3-methyl-4-morpholinyl]-6-[1-(methylsulfonyl)cyclopropyl]-2-pyrimidinyl]-

Molarity Calculator
Dilution Calculator
Molecular Weight Calculator

Contact us if you need more details on 1233339-22-4 AZ20. We are ready to answer your questions on packaging, logistics, certification or any Other aspects about 1233339-22-4、AZ20 1233339-22-4. If these products fail to match your need, please contact us and we would like to provide relevant information.

Product Categories : PI3K/Akt/mTOR > ATM/ATR Inhibitor