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CBR-5884 {[allProObj[0].p_purity_real_show]}

货号:A780427

CBR-5884是一种有效、选择性的磷酸甘油酸脱氢酶 (PHGDH) 抑制剂,IC50 为 33 μM。它能够抑制癌细胞中丝氨酸的合成,对具有高丝氨酸生物合成活性的癌细胞具有选择性毒性,尤其对黑素瘤和乳腺癌细胞系具有抑制作用。

CBR-5884 化学结构 CAS号:681159-27-3
CBR-5884 化学结构
CAS号:681159-27-3
CBR-5884 3D分子结构
CAS号:681159-27-3
CBR-5884 化学结构 CAS号:681159-27-3
CBR-5884 3D分子结构 CAS号:681159-27-3
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CBR-5884 纯度/质量文件 产品仅供科研

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CBR-5884 生物活性

描述 CBR-5884 is a noncompetitive 3-phosphoglycerate dehydrogenase (PHGDH) inhibitor with IC50=33 μM).

CBR-5884 细胞实验

Cell Line
Concentration Treated Time Description References
Breast cancer cell lines (MDA-MB-468, MDA-MB-436, HCC70, Hs578T) Breast cancer cell lines (MDA-MB-468, MDA-MB-436, HCC70, Hs578T) To evaluate the effect of CBR-5884 on the proliferation of breast cancer cell lines with high serine synthesis activity, results showed that CBR-5884 inhibited proliferation by 35% to 60% at 30 μM. Proc Natl Acad Sci U S A. 2016 Feb 16;113(7):1778-83.
Carney cells Carney cells To evaluate the acute toxicity of CBR-5884, results showed that CBR-5884 was not generally cytotoxic at concentrations up to 40 μM during the 3-h treatment period. Proc Natl Acad Sci U S A. 2016 Feb 16;113(7):1778-83.
LNT-229 cells LNT-229 cells Under both serum and serum-free conditions, CBR-5884 significantly inhibited cell proliferation. Br J Cancer. 2020 Apr;122(9):1391-1398.
LN-308 cells LN-308 cells Under both serum and serum-free conditions, CBR-5884 significantly inhibited cell proliferation. Br J Cancer. 2020 Apr;122(9):1391-1398.
G55 cells G55 cells Measurement of intracellular serine, glycine, asparagine, and tyrosine levels showed that CBR-5884 significantly reduced serine and glycine levels. Br J Cancer. 2020 Apr;122(9):1391-1398.
Candida albicans SC5314 Candida albicans SC5314 Test the inhibitory effect of CBR-5884 on cell growth, results showed that CBR-5884 inhibited cell growth at 170 µM. mBio. 2024 May 8;15(5):e0063324.
IOSE-80 cells IOSE-80 cells Evaluate the effect of CBR-5884 on IOSE-80 cells, results showed minimal effect on IOSE-80 cells Discov Oncol. 2024 May 11;15(1):154.
MDA-MB-231 cells MDA-MB-231 cells Evaluate the effect of CBR-5884 on MDA-MB-231 cells, results showed minimal effect on MDA-MB-231 cells Discov Oncol. 2024 May 11;15(1):154.
ID8 cells ID8 cells Evaluate the inhibitory effect of CBR-5884 on ID8 cells, results showed CBR-5884 effectively downregulated serine biosynthesis Discov Oncol. 2024 May 11;15(1):154.
SKOV3 cells SKOV3 cells Evaluate the inhibitory effect of CBR-5884 on SKOV3 cells, results showed CBR-5884 effectively downregulated serine biosynthesis Discov Oncol. 2024 May 11;15(1):154.
Human MOLM13 cell line Human MOLM13 cell line To evaluate the effect of CBR5884 on leukemia cell proliferation, results showed that CBR5884 significantly inhibited the proliferation and clonogenic ability of leukemia cells. Blood Adv. 2020 Aug 11;4(15):3626-3638.
Murine MLL-ENL-transformed primary HSPCs Murine MLL-ENL-transformed primary HSPCs To evaluate the effect of CBR5884 on leukemia cell proliferation, results showed that CBR5884 significantly inhibited the proliferation and clonogenic ability of leukemia cells. Blood Adv. 2020 Aug 11;4(15):3626-3638.

CBR-5884 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
BALB/c nude mice Xenograft tumor model established by subcutaneous injection of ID8 cells Intragastric administration 70 mg/kg Once daily for 12 consecutive days Evaluate the antitumor effect of CBR-5884 in vivo, results showed CBR-5884 significantly delayed tumor growth Discov Oncol. 2024 May 11;15(1):154.

CBR-5884 参考文献

[1]Mullarky E, Lucki NC, et al. Identification of a small molecule inhibitor of 3-phosphoglycerate dehydrogenase to target serine biosynthesis in cancers. Proc Natl Acad Sci U S A. 2016 Feb 16;113(7):1778-83.

CBR-5884 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.97mL

0.59mL

0.30mL

14.86mL

2.97mL

1.49mL

29.73mL

5.95mL

2.97mL

CBR-5884 技术信息

CAS号681159-27-3
分子式C14H12N2O4S2
分子量 336.39
SMILES Code O=C(C1=C(C)C(SC#N)=C(NC(C2=CC=CO2)=O)S1)OCC
MDL No. MFCD04451442
别名
运输蓝冰
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, sealed in dry, 2-8°C

溶解方案

DMSO: 50 mg/mL(148.64 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案 一
配制的工作液建议现用现配,短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案 一
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