BMS-906024

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

BMS-906024 是一种高效、选择性的 γ-分泌酶介导的 Notch1/2/3/4 受体信号传导抑制剂，IC50 分别为 1.6/0.7/3.4/2.9 nM。

BMS-906024 is a highly potent, selective inhibitor of γ-secretase mediated signaling of Notch1/2/3/4 receptors with IC50 of 1.6/0.7/3.4/2.9 nM, respectively; exhibits >200-fold selectivity against a panel of diverse protein targets; inhibits both leukemia (TALL-1) and triple-negative breast cancer (MDA-MB-468) cells with IC50 of 0.4 nM, demonstrates broad-spectrum antineoplastic activity against a wide array of human cancer xenografts. Blood Cancer Phase 1 Clinical.

Western Blot Analysis Cell Line:NSCLC cell lines (A549, H358, H1975, H2444, H1792, HCC44).Concentration:5, 10, 25, 50, 100 nM.Incubation Time:72 hours Result:Reduced Notch1 ICD levels in all six lung cancer cell lines tested at concentrations as low as 5 nM, with maximal depletion at 50-100 nM.

Animal Model:Six to 12-week-old female NOD scid gamma (NSG) mice with KRAS- and BRAF-WT PDX-T42 xenograftsDosage:8.5 mg/kg Administration:oral gavage; days 1 through 4 of each week for 3 weeks Result: Significantly enhanced the tumor growth inhibition of Paclitaxel (36 mg/kg), but had no significant effect on Cisplatin (2 mg/kg) treatment.Animal Model:Mouse Dosage:1 mg/kg (Pharmacokinetic Analysis)Administration:IV or PO Result:Had a T1/2 of 4.6/5.3 hours, a Cmax of 1/0.3 μM and an AUC of 3.4/1.9 μM?hour for IV/PO.

BMS 906024 | BMS906024

Wnt/Notch/Hedgehog

Notch

Notch

Cancer

Blood cancer

1401066-79-2

556.5

C26H26F6N4O3

>98% (HPLC)

In Vitro:?DMSO : 9.5 mg/mL (17.07 mM)

CN1C2=CC=CC=C2C(=NC(C1=O)NC(=O)C(CCC(F)(F)F)C(CCC(F)(F)F)C(=O)N)C3=CC=CC=C3

(2R,3S)-N1-[(3S)-2,3-Dihydro-1-methyl-2-oxo-5-phenyl-1H-1,4-benzodiazepin-3-yl]-2,3-bis(3,3,3-trifluoropropyl)-butanediamide

(-20℃)

With Ice Pack

≥ 2 years