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ZT-12-037-01

Cat. No. M9586
ZT-12-037-01 Structure
Synonym:

ZT-1203701

Size Price Availability Quantity
10mg USD 135  USD135 In stock
25mg USD 315  USD315 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

ZT-12-037-01 is a potent, selective, ATP-competitive STK19 inhibitor with IC50 values of 23.96 nM and 27.94 nM for STK19 (WT) and STK19 (D89N), respectively. ZT-12-037-01 effectively blocks oncogenic NRAS-driven melanocyte malignant transformation and melanoma growth in vitro and in vivo. ZT-12-037-01 (3 μM; 14 days) significantly inhibits mutant NRAS-STK19-driven melanocyte colony formation and proliferation. 

In vivo, ZT-12-037-01 (25-50 mg/kg; injection subcutaneously; once daily) 21 days treatment inhibits growth of SK-MEL-2 xenograft melanoma and the sections of tumors indicates induction of apoptosis by increasing cleaved caspase-3.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 385.50
Formula C21H31N5O2
CAS Number 2328073-61-4
Purity >98%
Solubility DMSO ≥ 9 mg/mL
Storage at -20°C
References

[1] Chengqian Yin, et al. Cell. Pharmacological Targeting of STK19 Inhibits Oncogenic NRAS-Driven Melanomagenesis

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: ZT-12-037-01, ZT-1203701 supplier, Ras, inhibitors

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