{"product_id":"taselisib-bhb21901085","title":"Taselisib","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\u003eTaselisib, also known as GDC-0032 or RG-7604, is a potent PI3K inhibitor that targets PIK3CA mutations, with K\u003csub\u003ei\u003c\/sub\u003e values of 0.12 nM, 0.29 nM, 0.97 nM and 9.1 nM against PI3Kδ, PI3Kα, PI3Kγ and PI3Kβ, respectively. It is supplied as a white to off-white solid (C24H28N8O2, MW 460.53) at 99.75% 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\u003e1282512-48-4\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eMolecular Formula\u003c\/th\u003e\n\u003ctd\u003eC24H28N8O2\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eMolecular Weight\u003c\/th\u003e\n\u003ctd\u003e460.53 g\/mol\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003ePurity\u003c\/th\u003e\n\u003ctd\u003e99.75%\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\u003eWhite to off-white\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eSMILES\u003c\/th\u003e\n\u003ctd\u003eCC(C)N1C(C2=CN3C(C(C(OCC3)=C4)=CC=C4C5=CN(C(C)(C(N)=O)C)N=C5)=N2)=NC(C)=N1\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eTarget\u003c\/th\u003e\n\u003ctd\u003ePI3Kδ, PI3Kα, PI3Kγ, PI3Kβ\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: 25 mg\/mL (54.29 mM; Requires sonication and warming and heat to 60°C; 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, 1 year; -20°C, 6 months.\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[3]\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\u003ePI3Kδ\u003c\/span\u003e\u003c\/p\u003e\n\u003cp\u003e\u003cspan\u003e0.12 nM (Ki)\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\u003e0.29 nM (Ki)\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\u003e0.97 nM (Ki)\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\u003e9.1 nM (Ki)\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]. \u003ca target=\"_blank\" rel=\"noopener\" href=\"https:\/\/www.ncbi.nlm.nih.gov\/pubmed\/26589432\"\u003eZachary S. Zumsteg, et al. Taselisib (GDC-0032), a Potent β-Sparing Small Molecule Inhibitor of PI3K, Radiosensitizes Head and Neck Squamous Carcinomas Containing Activating PIK3CA Alterations. Clin Cancer Res. 2016 Apr 15; 22(8): 2009–2019.\u003c\/a\u003e\u003c\/p\u003e\n\u003cp\u003e [2]. \u003ca target=\"_blank\" rel=\"noopener\" href=\"https:\/\/www.ncbi.nlm.nih.gov\/pubmed\/25472943\"\u003eMarian M. Deuker, et al. PI3′-Kinase Inhibition Forestalls the Onset of MEK1\/2 Inhibitor Resistance in BRAF-Mutated Melanoma. Cancer Discov. 2015 Feb; 5(2): 143–153.\u003c\/a\u003e\u003c\/p\u003e\n\u003cp\u003e [3]. \u003ca target=\"_blank\" rel=\"noopener\" href=\"https:\/\/www.ncbi.nlm.nih.gov\/pubmed\/23662903\"\u003eNdubaku CO, et al. Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust in vivo antitumor activity. J Med Chem. 2013 Jun 13;56(11):4597-610.\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":67604892320109,"sku":"HY-13898-5MG","price":93.0,"currency_code":"USD","in_stock":true},{"title":"10 mg","offer_id":67605190246765,"sku":"HY-13898-10MG","price":146.0,"currency_code":"USD","in_stock":true},{"title":"25 mg","offer_id":67605190279533,"sku":"HY-13898-25MG","price":240.0,"currency_code":"USD","in_stock":true},{"title":"50 mg","offer_id":67605190312301,"sku":"HY-13898-50MG","price":330.0,"currency_code":"USD","in_stock":true},{"title":"100 mg","offer_id":67605190345069,"sku":"HY-13898-100MG","price":594.0,"currency_code":"USD","in_stock":true},{"title":"200 mg","offer_id":67605190377837,"sku":"HY-13898-200MG","price":990.0,"currency_code":"USD","in_stock":true},{"title":"500 mg","offer_id":67605190410605,"sku":"HY-13898-500MG","price":0.0,"currency_code":"USD","in_stock":true},{"title":"1 g","offer_id":67605190443373,"sku":"HY-13898-1G","price":0.0,"currency_code":"USD","in_stock":true},{"title":"1 mL x 10 mM (in DMSO)","offer_id":67605190476141,"sku":"HY-13898-1MLX10MM","price":94.0,"currency_code":"USD","in_stock":true}],"thumbnail_url":"\/\/cdn.shopify.com\/s\/files\/1\/0949\/7424\/7277\/files\/hy-13898.gif?v=1790972961","url":"https:\/\/www.ebiohippo.com\/products\/taselisib-bhb21901085","provider":"BioHippo","version":"1.0","type":"link"}