貨號(hào)	規(guī)格	價(jià)格	上海	北京	武漢	南京
S80151-1mg	99.6%	￥323.00 S80151-1mg ￥323.00 現(xiàn)貨	8 8	-	-	-
S80151-2mg	99.6%	￥578.00 S80151-2mg ￥578.00 現(xiàn)貨	7 7	-	-	-
S80151-5mg	99.6%	￥1020.00 S80151-5mg ￥1020.00 現(xiàn)貨	8 8	-	-	-
S80151-10mg	99.6%	￥1700.00 S80151-10mg ￥1700.00 現(xiàn)貨	4 4	-	-	-
S80151-25mg	99.6%	￥3230.00 S80151-25mg ￥3230.00 現(xiàn)貨	5 5	-	-	-
S80151-50mg	≥99%	￥5100.00 S80151-50mg ￥5100.00 2-3天	0 貨期：2-3天	-	-	-
S80151-100mg	≥99%	￥6885.00 S80151-100mg ￥6885.00 2-3天	0 貨期：2-3天	-	-	-

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產(chǎn)品介紹

Agerafenib (CEP-32496; RXDX-105) is a highly potent and orally efficacious inhibitor of BRAFV600E with a Kd of 14 nM.

產(chǎn)品描述：

Agerafenib (CEP-32496; RXDX-105) is a highly potent and orally efficacious inhibitor of BRAFV600E with a Kd of 14 nM.

靶點(diǎn)：

Braf:36 nM (Kd);CRAF:39 nM (Kd);BRafV600E:14 nM (Kd);c-Kit:2 nM (Kd);Ret:2 nM (Kd);LCK:2 nM (Kd);Abl-1:3 nM (Kd);VEGFR-2:8 nM (Kd);CSF-1R:9 nM (Kd);EPHA2:14 nM (Kd);EGFR:22 nM (Kd);c-Met:513 nM (Kd);JAK-2:4700 nM (Kd);MEK-1:7100 nM (Kd);MEK-2:8300 nM (Kd);Raf;c-RET;Bcr-Abl;PDGFR;Src;c-Kit

體內(nèi)研究：

Oral administration of Agerafenib (CEP-32496) to Colo-205 tumor xenograft-bearing mice results in significant inhibition of pMEK in tumor cell lysates. For instance, a single 30 mg/kg (po) dose of Agerafenib leads to a 50 and 75% inhibition of normalized pMEK in tumor lysates at the 2 and 6 h postdose time point, respectively (p<0.03), while a 55 mg/kg (po) dose resulted in a 75% to 57% (p<0.03) inhibition of pMEK at 2 through 10 h post administration, with normalization to baseline by 24 h. Agerafenib exhibits an exceptional PK profile in mouse, dog, and cynomolgus monkey. Administration of Agerafenib to beagle dogs (single dose of 1 mg/kg iv and 10 mg/kg po) results in low clearance (CL=5.0 (mL/min)/kg) and excellent bioavailability (%F=100). Similarly, in cynomolgus monkey, the administration of Agerafenib (single dose of 1 mg/kg iv and 10 mg/kg po) leads to high oral exposure due to low clearance (CL=6.7 mL/min/kg) and excellent bioavailability (%F=100)

參考文獻(xiàn)：

1. Rowbottom MW, et al. Identification of 1-(3-(6,7-dimethoxyquinazolin-4-yloxy)phenyl)-3-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)urea hydrochloride (CEP-32496), a highly potent and orally efficacious inhibitor of V-RAF murine sarcoma viral on

溶解性：

DMSO : 50 mg/mL (96.63 mM; Need ultrasonic)

保存條件：

-20℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	1.933 ml	9.663 ml	19.325 ml
5 mM	0.387 ml	1.933 ml	3.865 ml
10 mM	0.193 ml	0.966 ml	1.933 ml
50 mM	0.039 ml	0.193 ml	0.387 ml

注意：

部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶(hù)參考交流研究之用。

參考文獻(xiàn)

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