{"product_id":"pqr530-bhb21900163","title":"PQR530","description":"\u003cdiv class=\"bhp-desc\"\u003e\n\u003cstyle\u003e.bhp-desc{font-size:16px;color:#1a1a1a;line-height:1.7}.bhp-desc h2{font-size:18px;font-weight:700;color:#003366;margin:24px 0 10px;padding-bottom:6px;border-bottom:2px solid #003366}.bhp-desc p{margin:0 0 12px}.bhp-desc .bhp-spec-table{width:100%;border-collapse:collapse;margin:12px 0 18px}.bhp-desc .bhp-spec-table th{width:36%;text-align:left;padding:8px 12px;background:#e8f0fb;color:#003366;font-weight:600;vertical-align:top;border:1px solid #ccd9f0}.bhp-desc .bhp-spec-table td{padding:8px 12px;vertical-align:top;border:1px solid #ccd9f0}.bhp-desc .bhp-warning-box{background:#fff8e6;border-left:4px solid #e6a817;padding:10px 14px;margin:10px 0 14px;border-radius:0 4px 4px 0}.bhp-desc .bhp-cat-pill{display:inline-block;background:#003366;color:#fff;border-radius:20px;padding:3px 12px;font-size:13px;margin-bottom:10px}\u003c\/style\u003e\n\u003cspan class=\"bhp-cat-pill\"\u003eInhibitors\u003c\/span\u003e\u003ch2\u003eCompound Overview\u003c\/h2\u003e\n\u003cp\u003ePQR530 is a potent, ATP-competitive, orally bioavailable, brain-penetrant dual pan-PI3K\/mTORC1\/2 inhibitor, with subnanomolar K\u003csub\u003ed\u003c\/sub\u003e values toward PI3Kα and mTOR of 0.84 nM and 0.33 nM, respectively. It shows antitumor activity\u003csup\u003e[1][2]\u003c\/sup\u003e. It is supplied as a light yellow to yellow solid (C18H23F2N7O2, MW 407.42) at 99.98% purity.\u003c\/p\u003e\n\u003ch2\u003ePhysical \u0026amp; Chemical Properties\u003c\/h2\u003e\n\u003ctable class=\"bhp-spec-table\"\u003e\u003ctbody\u003e\n\u003ctr\u003e\n\u003cth\u003eCAS Number\u003c\/th\u003e\n\u003ctd\u003e1927857-61-1\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eMolecular Formula\u003c\/th\u003e\n\u003ctd\u003eC18H23F2N7O2\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eMolecular Weight\u003c\/th\u003e\n\u003ctd\u003e407.42 g\/mol\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003ePurity\u003c\/th\u003e\n\u003ctd\u003e99.98%\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eAppearance\u003c\/th\u003e\n\u003ctd\u003eSolid\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eColor\u003c\/th\u003e\n\u003ctd\u003eLight yellow to yellow\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eSMILES\u003c\/th\u003e\n\u003ctd\u003eFC(C1=CC(N)=NC=C1C2=NC(N3CCOCC3)=NC(N4[C@H](COCC4)C)=N2)F\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eTarget\u003c\/th\u003e\n\u003ctd\u003emTOR, PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ, PI3KC2β\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eSignaling Pathway\u003c\/th\u003e\n\u003ctd\u003ePI3K\/Akt\/mTOR\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eSolubility\u003c\/th\u003e\n\u003ctd\u003eIn Vitro: DMSO: 33.33 mg\/mL (81.81 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eStorage\u003c\/th\u003e\n\u003ctd\u003ePowder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 2 years; -20°C, 1 year.\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eShipping\u003c\/th\u003e\n\u003ctd\u003eRoom temperature in continental US; may vary elsewhere.\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003c\/tbody\u003e\u003c\/table\u003e\n\u003ch2\u003eBiological Activity\u003c\/h2\u003e\n\u003ch3 style=\"font-size:16px;font-weight:700;color:#003366;margin:16px 0 8px\"\u003eIC50 \u0026amp; Target\u003csup\u003e[2]\u003c\/sup\u003e\n\u003c\/h3\u003e\n\u003cp\u003e\u003c\/p\u003e\n\u003ctable\u003e\u003ctbody\u003e\u003ctr\u003e\n\u003ctd\u003e\n\u003cp\u003e\u003cspan\u003emTOR\u003c\/span\u003e\u003c\/p\u003e\n\u003cp\u003e\u003cspan\u003e0.33 nM (Kd)\u003c\/span\u003e\u003c\/p\u003e\n\u003c\/td\u003e\n\u003ctd\u003e\n\u003cp\u003e\u003cspan\u003ePI3Kα\u003c\/span\u003e\u003c\/p\u003e\n\u003cp\u003e\u003cspan\u003e0.84 nM (Kd)\u003c\/span\u003e\u003c\/p\u003e\n\u003c\/td\u003e\n\u003ctd\u003e\n\u003cp\u003e\u003cspan\u003ePI3Kβ\u003c\/span\u003e\u003c\/p\u003e\n\u003cp\u003e\u003cspan\u003e6.1 nM (Kd)\u003c\/span\u003e\u003c\/p\u003e\n\u003c\/td\u003e\n\u003ctd\u003e\n\u003cp\u003e\u003cspan\u003ePI3Kγ\u003c\/span\u003e\u003c\/p\u003e\n\u003cp\u003e\u003cspan\u003e10 nM (Kd)\u003c\/span\u003e\u003c\/p\u003e\n\u003c\/td\u003e\n\u003ctd\u003e\n\u003cp\u003e\u003cspan\u003ePI3Kδ\u003c\/span\u003e\u003c\/p\u003e\n\u003cp\u003e\u003cspan\u003e11 nM (Kd)\u003c\/span\u003e\u003c\/p\u003e\n\u003c\/td\u003e\n\u003ctd\u003e\n\u003cp\u003e\u003cspan\u003ePI3KC2β\u003c\/span\u003e\u003c\/p\u003e\n\u003cp\u003e\u003cspan\u003e100 nM (Kd)\u003c\/span\u003e\u003c\/p\u003e\n\u003c\/td\u003e\n\u003c\/tr\u003e\u003c\/tbody\u003e\u003c\/table\u003e\n\u003ch2\u003eLiterature Cited\u003c\/h2\u003e\n\u003cp style=\"font-size:14px;color:#555;margin:0 0 10px\"\u003e\u003cem\u003eSources cited in this description and in the In Vitro \u0026amp; In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.\u003c\/em\u003e\u003c\/p\u003e\n\u003cp\u003e [1]. Denise Rageot, et al. Abstract 140: Discovery and biological evaluation of PQR530, a highly potent dual pan-PI3K\/mTORC1\/2 inhibitor. Cancer Res 2017;77(13 Suppl).\u003c\/p\u003e\n\u003cp\u003e [2]. \u003ca target=\"_blank\" rel=\"noopener\" href=\"https:\/\/pubmed.ncbi.nlm.nih.gov\/31244112\/\"\u003eRageot D, et al. (S)-4-(Difluoromethyl)-5-(4-(3-methylmorpholino)-6-morpholino-1,3,5-triazin-2-yl)pyridin-2-amine (PQR530), a Potent, Orally Bioavailable, and Brain-Penetrable Dual Inhibitor of Class I PI3K and mTOR Kinase. J Med Chem. 2019;62(13):6241-62\u003c\/a\u003e\u003c\/p\u003e\n\u003ch2\u003eSafety\u003c\/h2\u003e\n\u003cdiv class=\"bhp-warning-box\"\u003e\u003cp\u003e\u003cstrong\u003eFor Research Use Only.\u003c\/strong\u003e Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.\u003c\/p\u003e\u003c\/div\u003e\n\u003c\/div\u003e","brand":"MedChemExpress (MCE)","offers":[{"title":"5 mg","offer_id":67604856832365,"sku":"HY-107365-5MG","price":168.0,"currency_code":"USD","in_stock":true},{"title":"10 mg","offer_id":67605032370541,"sku":"HY-107365-10MG","price":240.0,"currency_code":"USD","in_stock":true},{"title":"25 mg","offer_id":67605032403309,"sku":"HY-107365-25MG","price":480.0,"currency_code":"USD","in_stock":true},{"title":"50 mg","offer_id":67605032436077,"sku":"HY-107365-50MG","price":708.0,"currency_code":"USD","in_stock":true},{"title":"100 mg","offer_id":67605032468845,"sku":"HY-107365-100MG","price":1140.0,"currency_code":"USD","in_stock":true},{"title":"200 mg","offer_id":67605032501613,"sku":"HY-107365-200MG","price":0.0,"currency_code":"USD","in_stock":true},{"title":"500 mg","offer_id":67605032534381,"sku":"HY-107365-500MG","price":0.0,"currency_code":"USD","in_stock":true},{"title":"1 mL x 10 mM (in DMSO)","offer_id":67605032567149,"sku":"HY-107365-1MLX10MM","price":185.0,"currency_code":"USD","in_stock":true}],"thumbnail_url":"\/\/cdn.shopify.com\/s\/files\/1\/0949\/7424\/7277\/files\/hy-107365.gif?v=1790972878","url":"https:\/\/www.ebiohippo.com\/products\/pqr530-bhb21900163","provider":"BioHippo","version":"1.0","type":"link"}