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- 上海莼试
- CS-01Y65444
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- 详细信息
- 技术资料
- 库存：
43
- 英文名：
BMS-833923
- CAS号：
1059734-66-5
- 供应商：
上海莼试
- 保存条件：
Store at -20°C
- 规格：
5mg 10mg 50mg
使用方法：
1.本蛋白酶抑制剂混合物为100×的储存液，使用时按照1:100的比例加入到裂解液中(例如，1ml裂解液中加入10μl蛋白酶抑制剂混合物)，混匀后即可使用。根据需要，0.5M的EDTA也按照1:100的比例加入到裂解液中（如用于检测金属蛋白酶活性，则不宜添加EDTA）。含有蛋白酶抑制剂混合物的裂解液宜现用现配，不宜配制后冻存待后续使用。
2. 待所需的抑制剂添加完毕混匀后，就可以开始进行哺乳动物组织的裂解和蛋白提取。
商品属性：
产品描述：
分子式:C30H27N5O
分子量:473.57
溶解度:≥ 47.4 mg/mL in DMSO, ≥ 5.14 mg/mL in EtOH with ultrasonic and warming
储存条件: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
The Hedgehog (Hh) signaling is a critical pathway involved in embryonic development and in tissue maintenance and repair in adults. It consists of the Hh ligands, the transmembrane receptors Patched 1 and 2, the G-protein- coupled receptor-like protein SMO and the glioma-associated oncogene transcription factors GLI1 to 3. The aberrant activation of Hh pathway, both mutational and epigenetic, is found to be associated with multiple aspects of tumorigenesis in various tumor cells. As a smoothened inhibitor, BMS-833923 can block the binding of cyclopamine (a naturally occurring SMO inhibitor) to SMO. It showed potent Hh pathway inhibitory activity with IC50 values at nanomolar in multiple cell-based assays. BMS-833923 also potently inhibited Hh pathway in medulloblastoma and pancreatic carcinoma xenograft models [1, 2 and 3].In vitro, BMS-833923 inhibited the expression of GLI1 and PTCH1 in cell lines expressing wild-type SMO or activated mutant SMO with IC50 values in the range from 6 to 35 nM. In the FACS-based binding assays, it does-dependently suppressed cyclopamine binding to SMO with IC50 value of 21 nM. In the esophageal adenocarcinoma cell lines OE19 and OE33, treatment of BMS-833923 significantly reduced cell proliferation with IC50 values of both 10 μM. Besides that, BMS-833923 was found to inhibit the growth of multiple myeloma cells and the proportion of ALDH+ cancer stem cells. It also inhibited the growth of many other tumor cells derived from patients with hematological malignancies including ALL, AML and CML [3 and 4].In animal models with medulloblastoma and pancreatic carcinoma xenografts, administration of BMS-833923 at single oral dose showed robust inhibition of Hh pathway. In a rat model with gastroesophageal reflux disease, the administration of BMS-833923 at dose of 10 mg/kg/day resulted in the decreased development of both Barrett esophagus and esophageal adenocarcinoma by 35.7% [3 and 5].References:[1] Siu L L, Papadopoulos K P, Alberts S, et al. A first-in-human phase 1study of an oral hedgehog pathway antagonist, BMS-833923 (XL139), in subjects with advanced or metastatic solid tumors. Mol Cancer Ther, 2009, 8(12 Suppl): A55.[2] Justilien V, Fields A P. Molecular Pathways: Novel Approaches for Improved Therapeutic Targeting of Hedgehog Signaling in Cancer Stem Cells. Clinical Cancer Research, 2015, 21(3): 505-513.[3] Gendreau S B, Hawkins D, Ho C P, et al. Abstract B192: Preclinical characterization of BMS�\833923 (XL139), a hedgehog (HH) pathway inhibitor in early clinical development. Molecular Cancer Therapeutics, 2009, 8(12 Supplement): B192-B192.[4] Zaidi A H, Komatsu Y, Kelly L A, et al. Smoothened inhibition leads to decreased proliferation and induces apoptosis in esophageal adenocarcinoma cells. Cancer investigation, 2013, 31(7): 480-489.[5] Gibson M K, Zaidi A H, Davison J M, et al. Prevention of Barrett esophagus and esophageal adenocarcinoma by smoothened inhibitor in a rat model of gastroesophageal reflux disease. Annals of surgery, 2013, 258(1): 82-88.
注意事项：
抗逆滴加序列
每次向板内滴加抗原时，移液器滴头要与平面45度悬空，不要触碰到孔内的液体，由后向前依次滴加(即浓度由低往高滴加)。
抗感染反应期
抗原抗体在室温20~25℃下，必须反应30min以上，若环境温度低于室温，可将微量反应板置于恒温培养箱中，使二者充分反应。
旅游温度
磷酸盐缓冲液的pH值要在高压灭菌后进行滴定，往往在高压后pH值会有所改变，所以高压后再调一次pH值更为准确。磷酸盐缓冲液一经使用保存期不要超过3周。当pH<5.8时，红细胞会产生自凝现象;当pH>7.8时，图形洗脱加快，易造成肉眼观察产生误差;p H=7.2时，红细胞沉降最充分，图形最清晰。
当滴注 1%红细胞悬液时，应经常摇晃红细胞悬液，使红细胞均匀地分布在磷酸缓冲液中，以防止红细胞下降。
反应时间及温度
加入鸡红血球之后，反应板在室温(20~25℃)静置30~40min，对照孔血球下沉于孔底，即可判定结果。若室温达不到实验要求，需相应调整反应时间。当环境温度低于4℃时，红细胞发生自凝;高于37℃时，会发生反应物分离和红细胞溶血。
公司正在出售的产品：
1.本蛋白酶抑制剂混合物为100×的储存液，使用时按照1:100的比例加入到裂解液中(例如，1ml裂解液中加入10μl蛋白酶抑制剂混合物)，混匀后即可使用。根据需要，0.5M的EDTA也按照1:100的比例加入到裂解液中（如用于检测金属蛋白酶活性，则不宜添加EDTA）。含有蛋白酶抑制剂混合物的裂解液宜现用现配，不宜配制后冻存待后续使用。
2. 待所需的抑制剂添加完毕混匀后，就可以开始进行哺乳动物组织的裂解和蛋白提取。
商品属性：
| 货号 | CS-01Y65444 | 规格 | 5mg 10mg 50mg |
| CAS号 | 1059734-66-5 | 分子量 | 473.57 |
| 含量 | >98.00% | 别名 | BMS 833923;BMS833923;XL-139;XL139;XL 139 |
| 分子式 | C30H27N5O | 化学名 | |
| 产地 | 国产 | 用途 | 仅供科研研究实验 |
分子式:C30H27N5O
分子量:473.57
溶解度:≥ 47.4 mg/mL in DMSO, ≥ 5.14 mg/mL in EtOH with ultrasonic and warming
储存条件: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
The Hedgehog (Hh) signaling is a critical pathway involved in embryonic development and in tissue maintenance and repair in adults. It consists of the Hh ligands, the transmembrane receptors Patched 1 and 2, the G-protein- coupled receptor-like protein SMO and the glioma-associated oncogene transcription factors GLI1 to 3. The aberrant activation of Hh pathway, both mutational and epigenetic, is found to be associated with multiple aspects of tumorigenesis in various tumor cells. As a smoothened inhibitor, BMS-833923 can block the binding of cyclopamine (a naturally occurring SMO inhibitor) to SMO. It showed potent Hh pathway inhibitory activity with IC50 values at nanomolar in multiple cell-based assays. BMS-833923 also potently inhibited Hh pathway in medulloblastoma and pancreatic carcinoma xenograft models [1, 2 and 3].In vitro, BMS-833923 inhibited the expression of GLI1 and PTCH1 in cell lines expressing wild-type SMO or activated mutant SMO with IC50 values in the range from 6 to 35 nM. In the FACS-based binding assays, it does-dependently suppressed cyclopamine binding to SMO with IC50 value of 21 nM. In the esophageal adenocarcinoma cell lines OE19 and OE33, treatment of BMS-833923 significantly reduced cell proliferation with IC50 values of both 10 μM. Besides that, BMS-833923 was found to inhibit the growth of multiple myeloma cells and the proportion of ALDH+ cancer stem cells. It also inhibited the growth of many other tumor cells derived from patients with hematological malignancies including ALL, AML and CML [3 and 4].In animal models with medulloblastoma and pancreatic carcinoma xenografts, administration of BMS-833923 at single oral dose showed robust inhibition of Hh pathway. In a rat model with gastroesophageal reflux disease, the administration of BMS-833923 at dose of 10 mg/kg/day resulted in the decreased development of both Barrett esophagus and esophageal adenocarcinoma by 35.7% [3 and 5].References:[1] Siu L L, Papadopoulos K P, Alberts S, et al. A first-in-human phase 1study of an oral hedgehog pathway antagonist, BMS-833923 (XL139), in subjects with advanced or metastatic solid tumors. Mol Cancer Ther, 2009, 8(12 Suppl): A55.[2] Justilien V, Fields A P. Molecular Pathways: Novel Approaches for Improved Therapeutic Targeting of Hedgehog Signaling in Cancer Stem Cells. Clinical Cancer Research, 2015, 21(3): 505-513.[3] Gendreau S B, Hawkins D, Ho C P, et al. Abstract B192: Preclinical characterization of BMS�\833923 (XL139), a hedgehog (HH) pathway inhibitor in early clinical development. Molecular Cancer Therapeutics, 2009, 8(12 Supplement): B192-B192.[4] Zaidi A H, Komatsu Y, Kelly L A, et al. Smoothened inhibition leads to decreased proliferation and induces apoptosis in esophageal adenocarcinoma cells. Cancer investigation, 2013, 31(7): 480-489.[5] Gibson M K, Zaidi A H, Davison J M, et al. Prevention of Barrett esophagus and esophageal adenocarcinoma by smoothened inhibitor in a rat model of gastroesophageal reflux disease. Annals of surgery, 2013, 258(1): 82-88.
注意事项：
抗逆滴加序列
每次向板内滴加抗原时，移液器滴头要与平面45度悬空，不要触碰到孔内的液体，由后向前依次滴加(即浓度由低往高滴加)。
抗感染反应期
抗原抗体在室温20~25℃下，必须反应30min以上，若环境温度低于室温，可将微量反应板置于恒温培养箱中，使二者充分反应。
旅游温度
磷酸盐缓冲液的pH值要在高压灭菌后进行滴定，往往在高压后pH值会有所改变，所以高压后再调一次pH值更为准确。磷酸盐缓冲液一经使用保存期不要超过3周。当pH<5.8时，红细胞会产生自凝现象;当pH>7.8时，图形洗脱加快，易造成肉眼观察产生误差;p H=7.2时，红细胞沉降最充分，图形最清晰。
当滴注 1%红细胞悬液时，应经常摇晃红细胞悬液，使红细胞均匀地分布在磷酸缓冲液中，以防止红细胞下降。
反应时间及温度
加入鸡红血球之后，反应板在室温(20~25℃)静置30~40min，对照孔血球下沉于孔底，即可判定结果。若室温达不到实验要求，需相应调整反应时间。当环境温度低于4℃时，红细胞发生自凝;高于37℃时，会发生反应物分离和红细胞溶血。
公司正在出售的产品：
| Recombnant Human ACF2 | 跨膜蛋白158封闭多肽 |
| 甲基化组蛋白H3(di methyl K9)封闭多肽 | KIAA1143 Antibody Blocking Peptide |
| 形成素2封闭多肽（成蛋白） | tsg101 Antibody Blocking Peptide |
| KLHDC7B蛋白封闭多肽 | L Antibody Blocking Peptide |
| 嗜中性粒细胞胞浆因子4封闭多肽 | HPS2 Antibody Blocking Peptide |
| 基质金属蛋白酶-9封闭多肽 | Connexin 30.3 Antibody Blocking Peptide |
| 红细胞膜蛋白4.2封闭多肽 | GALNTL4 Antibody Blocking Peptide |
| 衍生透明质酸相关蛋白封闭多肽 | 溶质载体转运蛋白家族26成员8封闭多肽 |
| KIAA1143蛋白封闭多肽 | ITIH1 Antibody Blocking Peptide |
| 肿瘤易感基因101蛋白封闭多肽 | EPB42 Antibody Blocking Peptide |
| HPS2蛋白封闭多肽 | MMP9 Antibody Blocking Peptide |
| 周斑蛋白封闭多肽 | NCF4 Antibody Blocking Peptide |
| 间隙连接蛋白30.3封闭多肽 | BMS-833923KLHDC7B Antibody Blocking Peptide |
| GALNTL4蛋白封闭多肽 | FMN2 Antibody Blocking Peptide |
| TMEM158 Antibody Blocking Peptide | Histone H3 (di methyl K9) Antibody Blocking Peptide |
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BMS-833923
￥600 - 3200
