VS-5584 CAS NO.1246560-33-7

Min.Order: 1 Gram
Payment Terms: T/T,

Product Details

Keywords

VS-5584
1246560-33-7

Quick Details

ProName: VS-5584
CasNo: 1246560-33-7
Appearance: white powder
Application: for laboratory research
DeliveryTime: within 3 days after payment
PackAge: Aluminium foil bag packing
Port: Shanghai,Guangzhou, Hongkong
ProductionCapacity: 1 Kilogram/Day
Purity: >99%
Storage: keep away from heat, sparks and flames
Transportation: by air; by sea; by express
LimitNum: 1 Gram
Heavy metal: <0.002%
Grade: Industrial Grade

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Details

Technical Data

Molecular Weight (MW)	354.41
Formula	C₁₇H₂₂N₈O
CAS No.	1246560-33-7
Synonyms	N/A

Solubility (25°C)	DMSO 71 mg/mL
	Water <1 mg/mL
	Ethanol 3 mg/mL
Storage	2 years -20℃Powder
Storage	6 months-80℃in DMSO

Chemical Name	2-Pyrimidinamine, 5-[8-methyl-9-(1-methylethyl)-2-(4-morpholinyl)-9H-purin-6-yl]-

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Biological Activity

Description	VS-5584 (SB2343) is a potent and selective dual PI3K/mTOR inhibitor for mTOR, PI3Kα/β/δ/γ with IC50 of 3.4 nM and 2.6-21 nM, respectively.
Targets	mTOR	PI3Kα	PI3Kα-H1047	PI3Kβ	PI3Kδ	PI3Kγ
IC50	3.4 nM	2.6 nM	3.3 nM	21 nM	2.7 nM	3.0 nM ^[1]
In vitro	VS-5584 is an ATP-competitive inhibitor which selectively inhibits PI3K/mTOR signaling with equivalent low nanomolar potency against all human Class I PI3K isoforms and mTOR kinase. VS-5584 is approximately 10-fold selective for cancer stem cells with an EC50 of 15 nM in HMLE breast cancer cells. VS-5584 preferentially decreases CD44^Hi/CD24^Lo cells in an HMLER immortalized mammary cancer cell line. In SUM159 cells, VS-5584 effectively eliminates the cancer stem cell side population. ^[1] A large human cancer cell line panel screen (436 lines) reveals broad antiproliferative sensitivity and that cells harboring mutations in PI3KCA are generally more sensitive toward VS-5584 treatment. In the FLT3-ITD harboring MV4-11 cells, VS-5584 blocks pAkt (S473) and pAkt (T308) with IC50 of 12 and 13 nM, respectively. The IC50 of VS-5584 for pS6 (S240/244), pAkt (S473), and pAkt (T308) are 20, 23, and 15 nM, respectively. ^[2]
In vivo	In mice bearing triple negative breast cancer tumors, oral dosing of VS-5584 decreases tumor cancer stem cells and induces tumor regression in taxane-resistant models. ^[1] In a PTEN^null human prostate PC3 xenograft model, treatment with VS-5584 leads to significant tumor growth inhibition (TGI) of 79% and 113% for 11 and 25 mg/kg, respectively. In a FLT3-ITD AML xenograft model, VS-5584 treatment induces dose-dependent inhibition of tumor growth (28% for 3.7 mg/kg and 76% for 11 mg/kg). ^[2]
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