{"product_id":"jbj-09-063-tfa-bhb21901283","title":"JBJ-09-063 TFA","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\u003eJBJ-09-063 TFA is a mutant-selective, allosteric EGFR inhibitor with IC\u003csub\u003e50\u003c\/sub\u003e values of 0.147 nM, 0.063 nM, 0.083 nM and 0.396 nM against EGFR L858R, EGFR L858R\/T790M, EGFR L858R\/T790M\/C797S and EGFRLT\/L747S, respectively. It effectively reduces phosphorylation of EGFR, Akt and ERK1\/2, and it is active across both EGFR tyrosine kinase inhibitor (TKI)-sensitive and -resistant models. It can be used in research on EGFR-mutant lung cancer\u003csup\u003e[1]\u003c\/sup\u003e. It is supplied as a white to off-white solid (C33H30F4N4O5S, MW 670.67) at 99.64% 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\u003eMolecular Formula\u003c\/th\u003e\n\u003ctd\u003eC33H30F4N4O5S\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eMolecular Weight\u003c\/th\u003e\n\u003ctd\u003e670.67 g\/mol\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003ePurity\u003c\/th\u003e\n\u003ctd\u003e99.64%\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\u003eO=C(NC1=NC=CS1)C(C2=CC(F)=CC=C2O)N(CC3=C4C=C(C5=CC=C(C6CCN(C)CC6)C=C5)C=C3)C4=O.O=C(O)C(F)(F)F\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eTarget\u003c\/th\u003e\n\u003ctd\u003eEGFR L858R, EGFR L858R\/T790M, EGFR L858R\/T790M\/C797S, EGFRLT\/L747S\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eSignaling Pathway\u003c\/th\u003e\n\u003ctd\u003eJAK\/STAT Signaling; Protein Tyrosine Kinase\/RTK\u003c\/td\u003e\n\u003c\/tr\u003e\n\u003ctr\u003e\n\u003cth\u003eSolubility\u003c\/th\u003e\n\u003ctd\u003eIn Vitro: DMSO: ≥ 100 mg\/mL (149.10 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\u003e4°C, sealed storage, away from moisture. In solvent: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture).\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[1]\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\u003eEGFR L858R\u003c\/span\u003e\u003c\/p\u003e\n\u003cp\u003e\u003cspan\u003e0.147 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 L858R\/T790M\u003c\/span\u003e\u003c\/p\u003e\n\u003cp\u003e\u003cspan\u003e0.063 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 L858R\/T790M\/C797S\u003c\/span\u003e\u003c\/p\u003e\n\u003cp\u003e\u003cspan\u003e0.083 nM (IC\u003csub\u003e50\u003c\/sub\u003e)\u003c\/span\u003e\u003c\/p\u003e\n\u003c\/td\u003e\n\u003ctd\u003e\n\u003cp\u003e\u003cspan\u003eEGFRLT\/L747S\u003c\/span\u003e\u003c\/p\u003e\n\u003cp\u003e\u003cspan\u003e0.396 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:\/\/pubmed.ncbi.nlm.nih.gov\/35422503\/\"\u003eTo C, et al. An allosteric inhibitor against the therapy-resistant mutant forms of EGFR in non-small cell lung cancer. Nat Cancer. 2022 Apr;3(4):402-417.\u003c\/a\u003e\u003c\/p\u003e\n\u003cp\u003e [2]. \u003ca target=\"_blank\" rel=\"noopener\" href=\"https:\/\/pubmed.ncbi.nlm.nih.gov\/35378251\/\"\u003eGero TW, Scott DA, et al. Quinazolinones as allosteric fourth-generation EGFR inhibitors for the treatment of NSCLC. Bioorg Med Chem Lett. 2022 Jul 15;68:128718.\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":67604900151661,"sku":"HY-147183A-5MG","price":540.0,"currency_code":"USD","in_stock":true},{"title":"10 mg","offer_id":67605224489325,"sku":"HY-147183A-10MG","price":960.0,"currency_code":"USD","in_stock":true},{"title":"25 mg","offer_id":67605224522093,"sku":"HY-147183A-25MG","price":1980.0,"currency_code":"USD","in_stock":true},{"title":"50 mg","offer_id":67605224554861,"sku":"HY-147183A-50MG","price":3060.0,"currency_code":"USD","in_stock":true},{"title":"100 mg","offer_id":67605224587629,"sku":"HY-147183A-100MG","price":4800.0,"currency_code":"USD","in_stock":true},{"title":"200 mg","offer_id":67605224620397,"sku":"HY-147183A-200MG","price":0.0,"currency_code":"USD","in_stock":true},{"title":"500 mg","offer_id":67605224653165,"sku":"HY-147183A-500MG","price":0.0,"currency_code":"USD","in_stock":true}],"thumbnail_url":"\/\/cdn.shopify.com\/s\/files\/1\/0949\/7424\/7277\/files\/hy-147183a.gif?v=1790972980","url":"https:\/\/www.ebiohippo.com\/products\/jbj-09-063-tfa-bhb21901283","provider":"BioHippo","version":"1.0","type":"link"}