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抑制剂/激活剂

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Silmitasertib CX-4945

Silmitasertib (CX-4945) 是一种有效、可口服、高度选择性的 CK2 抑制剂，对 CK2α 和 CK2α' 的 IC50值均为 1 nM。

货号：
TK0197
规格：

2mg

5mg

10mg
价格：
￥0.00

产品参数

CAS No.	1009820-21-6
生物活性	Silmitasertib (CX-4945) is an orally bioavailable, highly selective and potent CK2 inhibitor, with IC50 values of 1 nM against CK2α and CK2α'.
分子式	C19H12ClN3O2
分子量	349.77
运输条件	Room temperature in continental US; may vary elsewhere.
储存条件	Powder -20°C 3 years
溶解性数据	DMSO : ≥ 35 mg/mL (100.07 mM) 0.1 M NaOH : 33.33 mg/mL (95.29 mM; ultrasonic and adjust pH to 9 with NaOH)
体内研究	Silmitasertib (CX-4945) (25 or 75 mg/kg, p.o.) is well tolerated and demonstrated robust antitumor activity with concomitant reductions of the mechanism-based biomarker phospho-p21 (T145) in murine xenograft models.
体外研究	Silmitasertib (CX-4945) causes cell-cycle arrest and selectively induces apoptosis in cancer cells relative to normal cells, attenuates PI3K/Akt signalingand, and the antiproliferative activity of Silmitasertib (CX-4945) is correlated with expression levels of the CK2α catalytic subunit, Attenuation of PI3K/Akt signaling. Silmitasertib (CX-4945) with PS-341 treatment prevents leukemic cells from engaging a functional UPR in order to buffer the PS-341-mediated proteotoxic stress in ER lumen, and decreases pro-survival ER chaperon BIP/Grp78 expression. Silmitasertib (CX-4945) induces cytotoxicity and apoptosis, and exerts anti-proliferative effects in hematological tumors by downregulating CK2 expression and suppressing activation of CK2-mediated PI3K/Akt/mTOR signaling pathways.
文献	•Science. 2017 Dec 1;358(6367):eaan4368. •Nat Cell Biol. 2021 Mar;23(3):257-267. •Sci Transl Med. 2018 Jul 18;10(450). pii: eaaq1093. •EMBO Mol Med. 2020 Aug 7;12(8):e11987. •Oncogene. 2021 Nov 16. •Oncogene. 2017 Aug 24;36(34):4943-4950. •Cancers (Basel). 2021, 13(5), 1127. •Cells. 2021 Jan 18;10(1):E181. •Int J Mol Sci. 2021 Jan 15;22(2):E819. •Int J Mol Sci. 2020 Mar 3;21(5):1718. •Oncol Rep. 2017 Feb;37(2):1141-1147. •Biochem Biophys Res Commun. 2020 Oct 20;531(3):409-415. •Patent. US20180263995A1. •Oncotarget. 2016 Aug 16;7(33):53191-53203.
纯度及产品资料	98%

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