MYCi361

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

MYCi361 是 MYC 的抑制剂（与 MYC 结合，Kd 为 3.2 μM）。 MYCi361 是一种小分子 MYC 抑制剂，可抑制 MYC 依赖性癌细胞的活力，包括前列腺癌（MycCaP、LNCaP 和 PC3）、白血病（MV4-11）、淋巴瘤（HL-60 和 P493-6）和神经母细胞瘤(SK-N-B2) 具有低微摩尔 IC50 值。

MYCi361 is an inhibitor of MYC (binding to MYC with Kd of 3.2 μM). MYCi361 is a small-molecule MYC inhibitors that inhibits the viability of MYC-dependent cancer cells including prostate cancer (MycCaP, LNCaP, and PC3), leukemia (MV4-11), lymphoma (HL-60 and P493-6), and neuroblastoma (SK-N-B2) with low-micromolar IC50 values.MYC inhibitor 361 (MYCi361), suppressed in vivo tumor growth in mice, increased tumor immune cell infiltration, upregulated PD-L1 on tumors, and sensitized tumors to anti-PD1 immunotherapy.

MYCi361 inhibits the viability of MYC-dependent cancer cells including prostate cancer (MycCaP, LNCaP, and PC3), leukemia (MV4-11), lymphoma (HL-60 and P493-6), and neuroblastoma (SK-N-B2) with low-micromolar IC50 values. Cell Proliferation Assay Cell Line:The prostate cancer (MycCaP, LNCaP, and PC3), leukemia (MV4-11), lymphoma (HL-60 and P493-6), and neuroblastoma (SK-N-B2).Concentration:1.4-5.0 μM Incubation Time:5 days Result:IC50s of 2.9, 1.4, 1.6, 2.6, 5.0, 2.1, and 4.9 μM for prostate cancer (MycCaP, LNCaP, and PC3), leukemia (MV4-11), lymphoma (HL-60 and P493-6), and neuroblastoma (SK-N-B2), respectively.

MYCi361 inhibits MYC-dependent tumor growth in vivo. MYCi361 treatment (100 mg/kg/day for 2 days; then 70 mg/kg/day for 9 days) induces tumor regression in FVB or NSG male mice.?MYCi361 has moderate terminal elimination half-life of 44 and 20 h for intraperitoneal (i.p.) or oral (p.o.) dosing in mice, respectively.?MYCi361 suppresses tumor growth in mice, increases tumor immune cell infiltration, upregulates PD-L1 on tumors, and sensitizes tumors to anti-PD1 immunotherapy. However, MYCi361 demonstrates a narrow therapeutic index. An improved analog, MYCi975 shows better tolerability. Animal Model:FVB or NSG male mice of 6-8 weeks of age and 25 g bearing established MycCaP tumors Dosage:50 mg/kg and 70 mg/kg Administration:Treatment i.p. initially at 50 mg/kg twice daily for 2 days, then 70 mg/kg/day for 9 days Result:Induced tumor regression.Animal Model:C57BL/6 mice Dosage:50 mg/kg (Pharmacokinetic analysis) Administration:Treated p.o. or i.p.; 24 hours Result:Intraperitoneal (i.p.) or oral (p.o.) dosing in mice indicated plasma half-lives of 44 and 20 h, respectively, with maximum plasma concentrations (Cmax) of 27,200 ng/mL (46 μM) i.p. and 13,867 ng/mL (23 μM) p.o..

NUCC-0196361

Cell Cycle/DNA Damage

c-Myc

MYC

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2289690-31-7

594.86

C26H16ClF9N2O2

>98% (HPLC)

DMSO:100 mg/mL (168.1 mM; Need ultrasonic)

Cn1nc(cc1-c1ccc(OCc2ccc(Cl)cc2)c(-c2cc(cc(c2)C(F)(F)F)C(F)(F)F)c1O)C(F)(F)F

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(-20℃)

With Ice Pack

≥ 2 years