產(chǎn)品目錄

規(guī)格	10mM*1mLinDMSO50mg 5mg 10mg 100mg
CAS	1564268-08-1
別名	N/A
化學(xué)名	N/A
分子式	C25H33N5O3
分子量	451.56
溶解度	DMSO : 150 mg/mL (332.18 mM)
儲(chǔ)存條件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

BAY1238097 is a potent and selective inhibitor of BET binding to histones and has strong anti-proliferative activity in different AML (acute myeloid leukemia) and MM (multiple myeloma) models through down-regulation of c-Myc levels and its downstream transcriptome (IC50 <100 nM in a TR-FRET assay).

BAY 1238097 shows strong inhibitory activity (IC50 < 100 nM) in a TR-FRET assay using BET BRD4 bromodomain 1 and an acetylated peptide derived from histone H4. In the NanoBRET assay, the interaction between BRD4 (IC50=63 nM), BRD3 or BRD2 (IC50=609 nM) and H4 (IC50=2430 nM) is inhibited[1]. BAY 1238097 has in vitro anti-tumour activity in lymphoma models. BAY 1238097 affects the gene expression of GCB DLBCL cells. At the gene level, 143 probes (121 annotated transcripts) are downregulated and 71 (59 annotated transcripts) are upregulated. BTK, CCDC86, CCND2, CD19, CD27, FAIM, FCMR (FAIM3), IL7R, IRAK1, MAPK13, MYB, MYC, PDE4B, TNFRSF13B, TNFRSF17 are among the top downregulated genes. Beside histone-coding genes, the upregulated genes include CCL5, CDKN2C, CD69, JUN, and MKNK2[2].

BAY 1238097 shows strong efficacy in the AML models THP-1, MOLM-13 and KG-1, with T/C between 13 and 20%. BAY 1238097 is also active in MM models in a human IGH-cyclin D1 translocated MOLP-8 model with a T/C of 3%. In this model, BAY 1238097 is well tolerated at 10 mg/kg applied over 14 days, with no body weight loss measured. BAY 1238097 is also active against the FGFR/MMSET translocated model NCIH929, with 19% T/C versus 49% T/C for the standard-of-care lenalidomide. BAY 1238097 is well tolerated applied at 12 mg/kg for 9 days (maximum body weight loss 6%)[1]. BAY 1238097 has in vivo anti-tumour activity in lymphoma models[2].

[1]. Lejeune, P., et al. (2015) Abstract 3524: BAY 1238097, a novel BET inhibitor with strong efficacy in hematological tumor models. Cancer Research, 75(15 Suppl), 884. [2]. Bernasconi E, et al. Preclinical evaluation of the BET bromodomain inhibitor BAY 1238097 for the treatment of lymphoma. Br J Haematol. 2017 Sep;178(6):936-948.

特別提醒：

1. 本產(chǎn)品僅供科研使用。請(qǐng)勿用于醫(yī)藥、臨床診斷或治療，食品及化妝品等用途。請(qǐng)勿存放于普通住宅區(qū)。

2. 為了您的安全和健康，請(qǐng)穿好實(shí)驗(yàn)服并佩戴一次性手套和口罩操作。

原創(chuàng)作者：上海莼試生物技術(shù)有限公司

在線咨詢(xún)

留言注意事項(xiàng)：

1.遵守中華人民共和國(guó)有關(guān)法律、法規(guī)，尊重網(wǎng)上道德，承擔(dān)一切因您的行為而直接或間接引起的法律責(zé)任。

2.請(qǐng)您真實(shí)的反映產(chǎn)品的情況,不要捏造、誣蔑、造謠。如對(duì)產(chǎn)品有任何疑問(wèn),也可以留言咨詢(xún)。

3.未經(jīng)本站同意，任何人不得利用本留言簿發(fā)布個(gè)人或團(tuán)體的具有廣告性質(zhì)的信息或類(lèi)似言論。

您感興趣的產(chǎn)品*
您的單位*
聯(lián)系人*
聯(lián)系電話(huà)*
詳細(xì)地址*
常用郵箱*
請(qǐng)輸入您對(duì)我們的意見(jiàn)或建議*
驗(yàn)證碼*

同類(lèi)產(chǎn)品

YW3-56 (hydrochloride) (technical grade) UNC2170 (maleate) TSI-01 Tubastatin A (trifluoroacetate salt) Valproic Acid Acyl-D-Glucuronide Trichostatin C α-Amanitin Tiopronin-d3 Tolcapone-d4 XAV-939

訂購(gòu)流程

訂貨流程

產(chǎn)品訂購(gòu)說(shuō)明:

1、報(bào)價(jià)含普票、運(yùn)費(fèi)。

2、常用試劑備貨充足，除對(duì)溫度要求極其嚴(yán)格的產(chǎn)品當(dāng)天可發(fā)貨。

3、進(jìn)口原裝產(chǎn)品要3-6周的貨期，詳細(xì)情況請(qǐng)咨詢(xún)客服。

4、訂貨時(shí)間為工作日每周一至周五16:00之前。

5、如需代為檢測(cè)，標(biāo)本對(duì)環(huán)境溫度高，可聯(lián)系客服安排專(zhuān)人取樣（限省內(nèi)客戶(hù)）。

6、代測(cè)免收代測(cè)費(fèi)，一周出結(jié)果。

7、產(chǎn)品因運(yùn)輸途中包裝破損請(qǐng)拒絕簽收，做退回。我們將在24小時(shí)之內(nèi)為您補(bǔ)發(fā) 損壞產(chǎn)品。

8、如因單位財(cái)務(wù)制度原因，可申請(qǐng)先發(fā)貨，報(bào)賬后付款（此條款僅限醫(yī)院、學(xué)校信譽(yù)良好客戶(hù)）。

付款方式

普票匯款信息

賬戶(hù) 名：上海生物

開(kāi) 戶(hù) 行：中國(guó)銀行山東省分行營(yíng)業(yè)部

賬號(hào)：2169 2341 6278

為方便廣大客戶(hù)辦理貨款我公司提供多個(gè)銀行的賬戶(hù)，學(xué)校、醫(yī)院客戶(hù)購(gòu)買(mǎi)產(chǎn)品如因單位財(cái)務(wù)制度原因可先發(fā)貨待報(bào)賬后匯款，請(qǐng)及時(shí)告知銷(xiāo)售人員已做具體操作。