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| 品牌 | absin | CAS | 1188910-76-0 |
|---|---|---|---|
| 分子式 | C24H22F3N5O5 | 纯度 | ＞98% |
| 分子量 | 517.46 | 货号 | abs810259 |
| 规格 | 10mg | 供货周期 | 现货 |
| 主要用途 | is a highly potent inhibitor of BRAF | 应用领域 | 化工,生物产业,农林牧渔,制药/生物制药,综合 |
CEP-32496 1188910-76-0
| 产品描述 | |
| 描述 | Agerafenib is a highly potent inhibitor of BRAF(V600E/WT) and c-Raf with Kd of 14 nM/36 nM and 39 nM, also potent to Abl-1, c-Kit, Ret, PDGFRβ and VEGFR2, respectively; insignificant affinity for MEK-1, MEK-2, ERK-1 and ERK-2. |
| 纯度 | >98% |
| 储存/保存方法 | Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution. |
| 基本信息 | |
| 别名 | CEP32496；CEP 32496；RXDX-105；CEP-32496 |
| 外观 | Powder |
| 可溶性/溶解性 | DMSO 9 mg/mL (17.39 mM) 15% Captisol 15 mg/mL |
| 生物活性 | |
| 靶点 | c-Kit,LCK,PDGFRβ,RET,Abl1,, |
| In vitro(体外研究) | CEP-32496 inhibits A375 cell (BRAFV600E) proliferation with EC50 of 78 nM. CEP-32496 exhibits more sensitive cytotoxicity for tumor cell lines (A375, SK-MEL-28, Colo-205, Colo-679, and HT-144) expressing mutant BRAF than those expressing wild-type BRAF (HCT116, Hs578T, LNCaP, DU145, and PC-3). CEP-32496 inhibits mitogen-activated protein (MAP)/extracellular signal-regulated (ER) kinase (MEK) phosphorylation (pMEK) in human melanoma (A375) and colorectal cancer (Colo-205) cell lines with IC50 of 78 nM and 60 nM, respectively. |
| In vivo(体内研究) | CEP-32496 exhibits good stability in mouse, dog, monkey, and human liver microsomal preparations with measured intrinsic clearance values of 1/2 > 60 min in all assays. CEP-32496 (30 mg/kg, orally, BID) exhibits tumor stasis and a 40% incidence of partial tumor regressions (PRs) in Colo-205 xenograft mouse model, whereas the 100 mg/kg dose group exhibits both tumor stasis and an 80% incidence of PRs. CEP-32496 (30 mg/kg, orally, BID) leads to a 50% and 75% inhibition of normalized pMEK in tumor lysates at the 2 hours and 6 hours postdose time point, respectively, while a 55 mg/kg dose results in a 75% to 57% inhibition of pMEK at 2 hours through 10 hours post administration in Colo-205 xenograft mouse model. CEP-32496 is orally bioavailable in multiple preclinical species (>95% in rats, dogs, and monkeys). CEP-32496 (100 mg/kg) results in inhibition of pMEK and pERK and sustained tumor stasis and regressions in BRAF(V600E) colon carcinoma xenografts in nude mice. |
| 研究领域 | |
| 研究领域 | CancerOncoproteins/suppressorsOncoproteinsGrowth factor receptors CancerSignal transductionProtein phosphorylationTyrosine kinasesReceptor tyrosine kinases Developmental BiologyOrganogenesisHematopoietic system development Developmental BiologyReproductionGerm cell markers ImmunologyCell Type MarkersCDCytokines NeuroscienceDevelopment NeuroscienceNeurotransmissionReceptors / ChannelsTyrosine Kinase Receptors Signal TransductionProtein PhosphorylationTyrosine KinasesReceptor Tyrosine Kinases Stem CellsGermline Stem CellsEmbryonic Germ Cells Stem CellsHematopoietic ProgenitorsSurface Molecules Stem CellsHematopoietic ProgenitorsHematopoietic Stem CellsHSC markers Stem CellsHematopoietic ProgenitorsMyeloidMast Cell Lineage Tags & Cell MarkersCell Type MarkersTumor Associated Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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