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。


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