Free shipping on all orders over $ 500

CL-387785

Cat. No. M4871
CL-387785 Structure
Synonym:

EKI-785

Size Price Availability Quantity
10mM*1mL in DMSO USD 75  USD75 In stock
5mg USD 70  USD70 In stock
10mg USD 105  USD105 In stock
50mg USD 340  USD340 In stock
100mg USD 540  USD540 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control & Documentation
Biological Activity

CL-387785 blocks EGF-stimulated autoposphorylation of the receptor in cells (IC50, 5 nM), In cell lines that overexpress EGF-R or c-erbB-2, CL-387785 inhibits cell proliferation (IC50, 31 nM) primarily in a cytostatic manner.Doses of CL-387785 as low as 25 mg/kg reduces the growth of HCA-7-induced xenograft tumor, and a dose of 100 mg/kg prevents tumor growth entirely. Dose of 50 mg/kg CL-387785 is effective at reducing the growth of HCT-116-induced xenograft tumor.

Chemical Information
Molecular Weight 381.23
Formula C18H13BrN4O
CAS Number 194423-06-8
Solubility (25°C) DMSO 63 mg/mL
Water <1 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Discafani CM, et.al Biochem Pharmacol. Irreversible inhibition of epidermal growth factor receptor tyrosine kinase with in vivo activity by N-[4-[(3-bromophenyl)amino]-6-quinazolinyl]-2-butynamide (CL-387,785).

Related EGFR/HER2 Products
BBT-207

BBT-207 is a reversible, mutant-specific EGFR inhibitor with antitumor activity.

VRN-11

VRN-11 is an EGFR C797S inhibitor.

TRX-221

TRX-221 is an EGFR C797S inhibitor.

TAS-3351

TAS-3351 is an EGFR C797S inhibitor.

Larotinib mesylate hydrate

Larotinib mesylate hydrate is a potent, broad-spectrum, orally active tyrosine kinase inhibitor (TKI) that primarily targets EGFR with an IC50 of 0.6 nM.

  Catalog
Abmole Inhibitor Catalog




Keywords: CL-387785, EKI-785 supplier, EGFR/HER2, inhibitors, activators


Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.