货号	规格	价格	上海	北京	珠海	重庆	武汉
S81460-2mg买3赠1	98.20%	￥300.00 S81460-2mg ￥300.00 现货（买3赠1）	5 5	-	-	-	-
S81460-5mg买3赠1	98.20%	￥400.00 S81460-5mg ￥400.00 现货（买3赠1）	5 5	-	-	-	-
S81460-10mg买3赠1	98.20%	￥650.00 S81460-10mg ￥650.00 现货（买3赠1）	6 6	-	-	-	-
S81460-25mg买3赠1	98.20%	￥1200.00 S81460-25mg ￥1200.00 现货（买3赠1）	6 6	-	-	-	-
S81460-50mg买3赠1	98.20%	￥1700.00 S81460-50mg ￥1700.00 现货（买3赠1）	5 5	-	-	-	-
S81460-100mg买3赠1	≥98%	￥2900.00 S81460-100mg ￥2900.00 2-3天（买3赠1）	0 货期：2-3天	-	-	-	-

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产品描述：

CCF642 is a potent protein disulfide isomerases (PDI) inhibitor with an IC50 of 2.9 μM. CCF642 causes acute endoplasmic reticulum (ER) stress in multiple myeloma cells accompanied by apoptosis-inducing calcium release. CCF642 has broad anti-multiple myeloma activity

靶点：

IC50: 2.9 μM (PDI);Others

体外研究：

CCF642 (3 μM; 0.5-6 hours) increases PERK dimerization by phosphorylation and IRE1-α oligomerization within 30 minutes in KMS-12-PE confirming accumulation of misfolded ER proteins. CCF642, a bone marrow-sparing compound, exhibits a submicromolar IC50 in 10 of 10 multiple myeloma cell lines (MM1.S, MM1.R, KMS-12-PE, KMS-12-BM, NCI-H929, U266, RPMI 8226, JJN-3, HRMM.09-luc, 5TGM1-luc). Western Blot Analysis Cell Line: MM1.S cells Concentration: 3 μM Incubation Time: 0.5, 1, 2, 4, 6 hours Result: Increased PERK dimerization by phosphorylation and IRE1-α oligomerization within 30 minutes in KMS-12-PE confirming accumulation of misfolded ER proteins.

体内研究：

CCF642 (10 mg/kg; i.p.; three times a week; for 24 days) significantly prolongs life of 5TGM1-luc-bearing mice and suppresses 5TGM1-luc growth as determined by life imaging. Animal Model: C57BL/KaLwRij mice of 6 to 8 weeks of age with 5TGM1-luc Dosage: 10 mg/kg Administration: i.p.; three times a week; for 24 days Result: Significantly prolonged life of 5TGM1-luc–bearing mice and suppressed 5TGM1-luc growth as determined by life imaging.

参考文献：

1. Vatolin S et al. Novel Protein Disulfide Isomerase Inhibitor with Anticancer Activity in Multiple Myeloma. Cancer Res. 2016 Jun 1;76(11):3340-50.

溶解性：

soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.642 ml	13.212 ml	26.424 ml
5 mM	0.528 ml	2.642 ml	5.285 ml
10 mM	0.264 ml	1.321 ml	2.642 ml
50 mM	0.053 ml	0.264 ml	0.528 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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