CB-103

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

CB-103是一种口服活性的Notch信号通路抑制剂，具有抗肿瘤活性。 CB-103 在人 T 细胞急性淋巴细胞白血病癌细胞系中表现出阻断 NOTCH 信号传导的能力，并在 GSI 耐药 T-ALL 细胞系中表现出抗肿瘤功效。

CB-103 is a orally active inhibitor of notch signaling pathway, with anti-tumor activity. CB-103 has shown the ability to block NOTCH signaling in human T cell acute lymphoblastic leukemia cancer cell lines, and?exhibits anti-tumor efficacy in GSI resistant T-ALL cell lines.CB-103?inhibits growth of GSI/Mab resistant triple negative breast cancer, and?exhibits anti-tumor activity in xenograft models of human T-ALL and mouse mammary tumors.(In Vitro):CB-103 acts as a pan-NOTCH inhibitor by targeting NOTCH transcriptional activation complex.CB-103 can block NOTCH signaling in human T cell acute lymphoblastic leukemia cancer cell lines.CB-103 exhibits anti-tumor efficacy in GSI resistant T-ALL cell lines.(In Vivo):CB-103 inhibits NOTCH dependent cellular processes in mice.CB-103 blocks in vivo growth of PDX models of T-ALL.CB-103 (25 mg/kg; i.p./p.o.; 2x daily; for 2 weeks) inhibits growth of GSI/Mab resistant triple negative breast cancer.CB-103 exhibits anti-tumor activity in xenograft models of human T-ALL and mouse mammary tumors.

Limantrafin acts as a pan-NOTCH inhibitor by targeting NOTCH transcriptional activation complex.Limantrafin can block NOTCH signaling in human T cell acute lymphoblastic leukemia cancer cell lines.Limantrafin exhibits anti-tumor efficacy in GSI resistant T-ALL cell lines. Cell Viability Assay Cell Line:RPMI 8402, KOPTK1, PANC1, nRas driven melanoma cells Concentration:10 μM Incubation Time:4 days, 6 days Result:Caused a significant reduction in their growth potential.

Limantrafin inhibits NOTCH dependent cellular processes in mice.Limantrafin blocks in vivo growth of PDX models of T-ALL.Limantrafin (25 mg/kg; i.p./p.o.; 2x daily; for 2 weeks) inhibits growth of GSI/Mab resistant triple negative breast cancer.Limantrafin exhibits anti-tumor activity in xenograft models of human T-ALL and mouse mammary tumors. Animal Model:NSG mice, triple negative breast cancer mouse xenograft model Dosage:25 mg/kg Administration:Oral administration/Intraperitoneal injection; 2x daily; for 2 weeks Result:Inhibited growth of GSI/Mab resistant triple negative breast cancer.

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Neuroscience

Gamma-secretase

notch

Cancer

Breast Cancer;Colorectal Cancer;Cholangiocellular Carcinoma;Sarcoma;Desmoid Tumour;Adenoid Cystic Carcinoma;Non-hodgkin Lymphoma;Glomus Tumor, Malignant

218457-67-1

242.32

C15H18N2O

>98% (HPLC)

DMSO:230 mg/mL (949.16 mM; Need ultrasonic)

CC(C)(C)c1ccc(Oc2ccc(N)cn2)cc1

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(-20℃)

With Ice Pack

≥ 2 years