1. Protein Tyrosine Kinase/RTK
  2. VEGFR
  3. KRN-633

KRN-633 

Cat. No.: HY-12060 Purity: 99.06%
Handling Instructions

KRN-633 is a potent VEGFR inhibitor with IC50s of 170, 160 and 125 nM for VEGFR1, VEGFR2 and VEGFR3, respectively.

For research use only. We do not sell to patients.

KRN-633 Chemical Structure

KRN-633 Chemical Structure

CAS No. : 286370-15-8

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 119 In-stock
Estimated Time of Arrival: December 31
5 mg USD 108 In-stock
Estimated Time of Arrival: December 31
10 mg USD 174 In-stock
Estimated Time of Arrival: December 31
50 mg USD 414 In-stock
Estimated Time of Arrival: December 31
100 mg USD 648 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Description

KRN-633 is a potent VEGFR inhibitor with IC50s of 170, 160 and 125 nM for VEGFR1, VEGFR2 and VEGFR3, respectively.

IC50 & Target[1]

VEGFR1

170 nM (IC50)

VEGFR2

160 nM (IC50)

VEGFR3

125 nM (IC50)

In Vitro

KRN-633 inhibits tyrosine phosphorylation of VEGFR-1, VEGFR2, c-Kit, and PDGFR-β (IC50=11.7, 1.16, 8.01, 130 nM) in human umbilical vein endothelial cells. KRN-633 also inhibits the VEGF-driven proliferation of HUVECs (IC50=14.9 nM). KRN-633 suppresses capillary tube formation of endothelial cells[1].

In Vivo

KRN-633 inhibits tumor growth in several tumor xenograft models with diverse tissue origins, including lung, colon, and prostate, in athymic mice and rats. KRN-633 also causes the regression of some well-established tumors and those that have regrown after the cessation of treatment. KRN-633 is well tolerated and has no significant effects on body weight or the general health of the animals. Histologic analysis of tumor xenografts treated with KRN-633 reveals a reduction in the number of endothelial cells in non-necrotic areas and a decrease in vascular permeability[1].

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 8 mg/mL (19.19 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3989 mL 11.9944 mL 23.9889 mL
5 mM 0.4798 mL 2.3989 mL 4.7978 mL
10 mM 0.2399 mL 1.1994 mL 2.3989 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Kinase Assay
[1]

Cell-free kinase assays are done to obtain IC50 values against a variety of recombinant receptor and non-RTKs. KRN-633 is tested from 0.3 nM to 10 μM. All assays are done in quadruplicate with 1 μM ATP[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[1]

A549, Ls174T, HT29, DU145, LNCap, and PC-3 cells cancer cells are cultured for 24 hours before adding KRN-633 (0.01 to 10 μM) or vehicle (0.1% DMSO in medium) and then grow for a further 96 hours. Cell viability is measured using WST-1 reagent. The percentage viability is determined relative to the untreated control[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Rats: Human tumor xenografts are established in the hind flank of athymic rats (BALB/cA, Jcl-nu). Rats are randomized into groups of five at the point when the tumors reach the average size indicated (162 to 657 mm3) and are then treated with KRN-633 or vehicle, either once (qd) or twice (bid) per day, at the dosages shown. The percentage of tumor growth inhibition compared with the vehicle-treated group is calculated on the day after the last treatment (day 14)[1].

Mice: The mice are randomized into groups of five at the point when the tumors reached the average sizes: 103 to 260 mm3 or 500 to 667 mm3. They are then treated with KRN-633 or vehicle, either once (qd) or twice (bid) per day, at the dosages of 10-100 mg/kg. The percentage of tumor growth inhibition (TGI) compared with the vehicle-treated group is calculated on the day after the last treatment[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

416.86

Formula

C₂₀H₂₁ClN₄O₄

CAS No.

286370-15-8

SMILES

ClC1=CC(OC2=NC=NC3=CC(OC)=C(C=C32)OC)=CC=C1NC(NCCC)=O

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
KRN-633
Cat. No.:
HY-12060
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KRN-633

Cat. No.: HY-12060