L-778123 (hydrochloride)


CAS No. : 253863-00-2

253863-00-2
Price and Availability of CAS No. : 253863-00-2
Size Price Stock
5mg $77 In-stock
10mg $110 In-stock
50mg $319 In-stock
100mg $539 In-stock
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Cat. No. : HY-16273A
M.Wt: 442.34
Formula: C22H21Cl2N5O
Purity: >98 %
Solubility: DMSO : ≥ 25 mg/mL;H2O : 25 mg/mL (ultrasonic)
Introduction of 253863-00-2 :

L-778123 hydrochloride is a dual inhibitor of FPTase and GGPTase-I, with IC50 values of 2 nM and 98 nM respectively. In Vitro:L-778123 hydrochloride alone does not have obvious cytotoxicity on HT-29 and A549 cell lines (IC50: >100 μM), but can generate synergistic effects with Doxorubicin (HY-15142A), with the decreased IC50s of 1.72 and 1.52 μM respectively[2].
L-778123 hydrochloride inhibits myeloid leukemia cell proliferation with IC50 values of 0.2 μM-1.8 μM for cell lines, and 0.1 μM-161.8 μM in primary samples[3].
L-778123 (0-1 μM, 12 h; or 5 μM, 6 h) hydrochloride inhibits H-RAS prenylation in HL-60 cells, and inhibits phosphorylated MEK-1/2 level (5 μM, 24 h)[3].
L-778123 (0-100 μM, 72 h) hydrochloride inhibits lymphocyte activation (marker: CD71 or CD25) and function in human PBMCs[4].
In Vivo:L-778123 (50 mg/kg/day, infusion, 7 days) hydrochloride inhibits both HDJ2 and Rap1A prenylation in PBMCs of dogs, but without inhibition in Ki-Ras prenylation[1].

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