{"product_id":"rilzabrutinib-bhb21900268","title":"Rilzabrutinib","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\u003eRilzabrutinib, also known as PRN1008, is a reversible covalent, selective, orally active inhibitor of Bruton’s Tyrosine Kinase (BTK), with an IC\u003csub\u003e50\u003c\/sub\u003e of 1.3 nM. It is supplied as a white to off-white solid (C36H40FN9O3, MW 665.76) at 98.97% 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\u003e1575596-29-0\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eMolecular Formula\u003c\/th\u003e\n\u003ctd\u003eC36H40FN9O3\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eMolecular Weight\u003c\/th\u003e\n\u003ctd\u003e665.76 g\/mol\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003ePurity\u003c\/th\u003e\n\u003ctd\u003e98.97%\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\u003eNC1=C2C(C3=C(C=C(OC4=CC=CC=C4)C=C3)F)=NN([C@H]5CN(CCC5)C(\/C(C#N)=C\/C(C)(N6CCN(C7COC7)CC6)C)=O)C2=NC=N1\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eTarget\u003c\/th\u003e\n\u003ctd\u003eBTK, BMX, ITK, TEC, RLK, BLK, EGFR, ERBB2, ERBB4\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eSignaling Pathway\u003c\/th\u003e\n\u003ctd\u003eProtein Tyrosine Kinase\/RTK\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eSolubility\u003c\/th\u003e\n\u003ctd\u003eIn Vitro: DMSO: ≥ 130 mg\/mL (195.27 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) * \"≥\" means soluble, but saturation unknown.\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\u003c\/h3\u003e\n\u003cp\u003e\u003csup\u003e[1]\u003c\/sup\u003e\u003csup\u003e[2]\u003c\/sup\u003e\u003c\/p\u003e\n\u003cp\u003e\u003c\/p\u003e\n\u003ctable\u003e\u003ctbody\u003e\u003ctr\u003e\n\u003ctd\u003e\n\u003cp\u003e\u003cspan\u003eBTK\u003c\/span\u003e\u003c\/p\u003e\n\u003cp\u003e\u003cspan\u003e1.3 nM (IC\u003csub\u003e50\u003c\/sub\u003e)\u003c\/span\u003e\u003c\/p\u003e\n\u003c\/td\u003e\n\u003ctd\u003e\n\u003cp\u003e\u003cspan\u003eBMX\u003c\/span\u003e\u003c\/p\u003e\n\u003cp\u003e\u003cspan\u003e1.0 nM (IC\u003csub\u003e50\u003c\/sub\u003e)\u003c\/span\u003e\u003c\/p\u003e\n\u003c\/td\u003e\n\u003ctd\u003e\n\u003cp\u003e\u003cspan\u003eITK\u003c\/span\u003e\u003c\/p\u003e\n\u003cp\u003e\u003cspan\u003e440 nM (IC\u003csub\u003e50\u003c\/sub\u003e)\u003c\/span\u003e\u003c\/p\u003e\n\u003c\/td\u003e\n\u003ctd\u003e\n\u003cp\u003e\u003cspan\u003eTEC\u003c\/span\u003e\u003c\/p\u003e\n\u003cp\u003e\u003cspan\u003e0.8 nM (IC\u003csub\u003e50\u003c\/sub\u003e)\u003c\/span\u003e\u003c\/p\u003e\n\u003c\/td\u003e\n\u003ctd\u003e\n\u003cp\u003e\u003cspan\u003eRLK\u003c\/span\u003e\u003c\/p\u003e\n\u003cp\u003e\u003cspan\u003e1.2 nM (IC\u003csub\u003e50\u003c\/sub\u003e)\u003c\/span\u003e\u003c\/p\u003e\n\u003c\/td\u003e\n\u003ctd\u003e\n\u003cp\u003e\u003cspan\u003eBLK\u003c\/span\u003e\u003c\/p\u003e\n\u003cp\u003e\u003cspan\u003e6.3 nM (IC\u003csub\u003e50\u003c\/sub\u003e)\u003c\/span\u003e\u003c\/p\u003e\n\u003c\/td\u003e\n\u003ctd\u003e\n\u003cp\u003e\u003cspan\u003eEGFR\u003c\/span\u003e\u003c\/p\u003e\n\u003cp\u003e\u003cspan\u003e520 nM (IC\u003csub\u003e50\u003c\/sub\u003e)\u003c\/span\u003e\u003c\/p\u003e\n\u003c\/td\u003e\n\u003ctd\u003e\n\u003cp\u003e\u003cspan\u003eERBB2\u003c\/span\u003e\u003c\/p\u003e\n\u003cp\u003e\u003cspan\u003e3900 nM (IC\u003csub\u003e50\u003c\/sub\u003e)\u003c\/span\u003e\u003c\/p\u003e\n\u003c\/td\u003e\n\u003ctd\u003e\n\u003cp\u003e\u003cspan\u003eERBB4\u003c\/span\u003e\u003c\/p\u003e\n\u003cp\u003e\u003cspan\u003e11.3 nM (IC\u003csub\u003e50\u003c\/sub\u003e)\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\/28636208\/\"\u003eSmith PF, et al. A phase I trial of PRN1008, a novel reversible covalent inhibitor of Bruton's tyrosine kinase, in healthy volunteers. Br J Clin Pharmacol. 2017 Nov;83(11):2367-2376.\u003c\/a\u003e\u003c\/p\u003e\n\u003cp\u003e [2]. Hill RJ, Bradshaw JM, Bisconte A, Tam D, Owens TD, Brameld KA, Smith PF, Funk JO, Goldstein DM, Nunn PA. Preclinical Characterization of PRN1008, a Novel Reversible Covalent Inhibitor of BTK that Shows Efficacy in a RAT Model of Collagen-Induced Arthritis. Annals of the Rheumatic Diseases 2015; 74(Suppl 2): 216.\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":67604858208621,"sku":"HY-112166-5MG","price":360.0,"currency_code":"USD","in_stock":true},{"title":"10 mg","offer_id":67605053505901,"sku":"HY-112166-10MG","price":576.0,"currency_code":"USD","in_stock":true},{"title":"25 mg","offer_id":67605053538669,"sku":"HY-112166-25MG","price":1020.0,"currency_code":"USD","in_stock":true},{"title":"50 mg","offer_id":67605053571437,"sku":"HY-112166-50MG","price":1440.0,"currency_code":"USD","in_stock":true},{"title":"100 mg","offer_id":67605053604205,"sku":"HY-112166-100MG","price":2016.0,"currency_code":"USD","in_stock":true},{"title":"200 mg","offer_id":67605053636973,"sku":"HY-112166-200MG","price":0.0,"currency_code":"USD","in_stock":true},{"title":"500 mg","offer_id":67605053669741,"sku":"HY-112166-500MG","price":0.0,"currency_code":"USD","in_stock":true},{"title":"1 mL x 10 mM (in DMSO)","offer_id":67605053702509,"sku":"HY-112166-1MLX10MM","price":527.0,"currency_code":"USD","in_stock":true}],"thumbnail_url":"\/\/cdn.shopify.com\/s\/files\/1\/0949\/7424\/7277\/files\/hy-112166.gif?v=1790972887","url":"https:\/\/www.ebiohippo.com\/products\/rilzabrutinib-bhb21900268","provider":"BioHippo","version":"1.0","type":"link"}