1902983-63-4
Chemical Structure
JP-11646
- CAS No.: 1902983-63-4
- Formula:C25H25N5O2S
- Molecular Weight:459.56
InChIKey: FQGGTIFOJIOPFG-JBLHJTENSA-N
SMILES: O=C1NC(/C(S1)=C/C2=CC=NC(N[C@H]3CC[C@@H](CC3)NCC4=CC=CC5=C4C=CC=C5)=N2)=O
Biological Activity: JP-11646 is a pan-PIM inhibitor with increased potency against PIM2 (IC50 = 0.5 nM). JP11646 is freely reversible and ATP non-competitive. JP-11646 results in a decrease of PIM1, 2, and 3 mRNA. JP-11646 can effectively inhibit cell viability in small cell lung cancer (SCLC) and large cell neuroendocrine carcinomas of the lung (LCNEC). JP-11646 can cause a decrease in p-4EBP-1 protein, increasing the cleavage of caspases while decreasing caspase-3. JP-11646 induces apoptosis or necroptosis in cells. JP-11646 leads to reductions in MYC paralogs. JP-11646 can be used for the study of SCLC, LCNEC, human acute leukemia (AML), multiple myeloma (MM), and triple-negative breast cancer (TNBC)[1][2][3][4][5].
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JP-11646 | 98.74% | JP-11646 is a pan-PIM inhibitor with increased potency against PIM2 (IC50 = 0.5 nM). JP11646 is freely reversible and ATP non-competitive. JP-11646 results in a decrease of PIM1, 2, and 3 mRNA. JP-11646 can effectively inhibit cell viability in small cell lung cancer (SCLC) and large cell neuroendocrine carcinomas of the lung (LCNEC). JP-11646 can cause a decrease in p-4EBP-1 protein, increasing the cleavage of caspases while decreasing caspase-3. JP-11646 induces apoptosis or necroptosis in cells. JP-11646 leads to reductions in MYC paralogs. JP-11646 can be used for the study of SCLC, LCNEC, human acute leukemia (AML), multiple myeloma (MM), and triple-negative breast cancer (TNBC). | ||||||||||||||||||||
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- [1]. Minton K, et al. P3. 02G. 04 JP11646-mediated PIM2 Inhibition Has Potent Antitumor Effects in Small Cell Lung Cancer and Large Cell Neuroendocrine Carcinoma of the Lung[J]. Journal of Thoracic Oncology, 2024, 19(10): S305-S306.
- [2]. Krista E. et al. Translational pharmacology approaches to explore the novel mechanism of a pan-PIM kinase inhibitor, JP-11646, in acute myeloid leukemia. [abstract]. In: Proceedings of the 106th Annual Meeting of the American Association for Cancer Research; 2015 Apr 18-22; Philadelphia, PA. Philadelphia (PA): AACR; Cancer Res 2015;75(15 Suppl):Abstract nr 681.
- [3]. Katsuta E, et al. Targeting PIM2 by JP11646 results in significant antitumor effects in solid tumors[J]. International journal of oncology, 2022, 61(4): 114.
- [4]. Nair JR, et al. Novel inhibition of PIM2 kinase has significant anti-tumor efficacy in multiple myeloma. Leukemia. 2017 Aug;31(8):1715-1726. [Content Brief]
- [5]. Mehta R, et al. Preclinical efficacy of the novel PIM2 kinase inhibitor, JP11646 in triple negative breast cancer models [abstract]. In: Proceedings of the 2016 San Antonio Breast Cancer Symposium; 2016 Dec 6-10; San Antonio, TX. Philadelphia (PA): AACR; Cancer Res 2017;77(4 Suppl):Abstract nr P6-11-10.
Keywords
