ChemicalBook > CAS DataBase List > KRN 633

KRN 633

Product Name: KRN 633
CAS No.: 286370-15-8
Chemical Name: KRN 633
Synonyms: CS-463;KRN 633;KRN 633;KRN-633;KRN 633 USP/EP/BP;KRN-633, 10 mM in DMSO;KRN633; KRN-633; KRN 633;VEGFR Tyrosine Kinase Inhibitor III, KRN633;KRN 633 (This product is unavailable in the U.S.);1-(2-chloro-4-(6,7-diMethoxyquinazolin-4-yloxy)phenyl)-3-propylurea;N-[2-Chloro-4-(6,7-dimethoxyquinazolin-4-yloxy)phenyl]-N'-propylurea
CBNumber: CB42561482
Molecular Formula: C20H21ClN4O4
Formula Weight: 416.86
MOL File: 286370-15-8.mol

Less

KRN 633 Property

Melting point:: 231-232°C
Boiling point:: 545.6±50.0 °C(Predicted)
Density: 1.321
storage temp.: -20°C
solubility: DMSO: soluble3mg/mL, clear (warmed)
pka: 13.08±0.70(Predicted)
form: powder
color: white to beige

Less

Safety

Hazard Codes: Xn
Risk Statements: 22
WGK Germany: 3

Less

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

Precautionary statements

P280Wear protective gloves/protective clothing/eye protection/face protection.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

Less

N-Bromosuccinimide Price

Sigma-Aldrich

Product number: SML0957
Product name: KRN633
Purity: ≥98% (HPLC)
Packaging: 5mg
Price: $133
Updated: 2022/05/15

Cayman Chemical

Product number: 14871
Product name: KRN 633
Purity: ≥95%
Packaging: 1mg
Price: $51
Updated: 2024/03/01

Cayman Chemical

Product number: 14871
Product name: KRN 633
Purity: ≥95%
Packaging: 5mg
Price: $99
Updated: 2024/03/01

Cayman Chemical

Product number: 14871
Product name: KRN 633
Purity: ≥95%
Packaging: 10mg
Price: $184
Updated: 2024/03/01

Cayman Chemical

Product number: 14871
Product name: KRN 633
Purity: ≥95%
Packaging: 50mg
Price: $773
Updated: 2024/03/01

Less

KRN 633 Chemical Properties,Usage,Production

Uses

KRN 633 is an ATP-competitive inhibitor of VEGFR1/2/3 with IC50 of 170 nM/160 nM/125 nM and also inhibits PDGFRα/β with IC50 of 965 nM/9850 nM.

Uses

KRN 633 is an ATP-competitive inhibitor of vascular endothlial growth factor receptor tyrosine kinase (VEGFR). KRN 633 also suppresses VEGF-dependent activation of MAPK and cell proliferation and demonstrates antitumor and antiangiogenic activity by inhibiting vessel formation and vascular permeability in human tumor xenograft models.

Biological Activity

krn 633 is a selective inhibitor of vegfr-1, vegfr-2 and vegfr-3 with ic50 value of 170 nm, 160 nm and 125 nm [1].vascular endothelial growth factor receptor (vegfr) is a protein and plays an important role in tumor angiogenesis by cooperating with its ligand vegf [1].krn 633 is a potent vegfr inhibitor. when tested with huvecs, krn 633 inhibited the cell proliferation that mediated by vegf with the ic50 value of 14.9 nmol/l and suppressed the capillary tube formation by ~50% at the dose of 10 nmol/l [1].in mid-pregnant mice model, krn633 was used at the dose of 5 mg/kg once daily from embryonic day 13.5 until the day of delivery and the effect on vascular growth was slightly delayed on postnatal day 4 (p4) and on p8 it was observed that krn633 resulted in the decreased numbers of central arteries and veins and abnormal branching of the central arteries [2]. when tested with athymic mouse xenograft ht29 cells model, administration of krn633 inhibited tumor growth as ~90% from the initial tumor volume rangs from 500-667 mm3, while had less effect du145 xenograft mouse models by inhibiting tumor angiogenesis and vascular permeability [1].

Biochem/physiol Actions

KRN633 is a cell-permeable; reversible and ATP-competitive inhibitor of vascular endothelial growth factor receptor tyrosine kinase (VEGFR) with IC50 values of 170, 160, and 125 nM for VEGFR-1, -2, -3, respectively. Krn633 inhibits PDGFR-α and c-Kit only at higher concentrations (IC50 = 0.97 and 4.33 μM, respectively) and is inactive towards a panel of 17 other kinases (IC50 >/= 10 μM).

Synthesis

286371-63-9

32315-10-9

144-55-8

286370-15-8

Example 62 N-[2-chloro-4-[(6,7-dimethoxy-4-quinazolinyl)oxy]phenyl]-N'-propylurea was synthesized as follows: 2-chloro-4-[(6,7-dimethoxy-4-quinazolinyl)oxy]aniline (5.13 g) was dissolved in a solvent mixture of chloroform (100 mL) and triethylamine (50 mL). Subsequently, a solution of chloroform (3 mL) of triphosgene (4.59 g) was slowly added to this solution. The reaction mixture was stirred at room temperature for 30 minutes. Next, n-propylamine (2.74 g) was added to the reaction system and stirring was continued for 2 hours. Upon completion of the reaction, saturated aqueous sodium bicarbonate solution was added to the reaction solution for neutralization, followed by extraction with chloroform. The organic phase was dried with anhydrous sodium sulfate, filtered and concentrated under reduced pressure to remove the solvent. The crude product was purified by silica gel column chromatography with chloroform/methanol (50:1, v/v) as eluent to afford the target product N-[2-chloro-4-[(6,7-dimethoxy-4-quinazolinyl)oxy]phenyl]-N'-propylurea in 4.14 g in 64% yield. The structure of the product was confirmed by 1H-NMR (DMSO-d6, 400 MHz) and mass spectrometry (ESI-MS).1H-NMR data: δ 0.91 (t, J = 7.3 Hz, 3H), 1.41-1.53 (m, 2H), 3.05-3.12 (m, 2H), 3.97 (s, 3H), 3.99 (s, 3H). 6.99 (t, J = 5.4 Hz, 1H), 7.22 (dd, J = 2.7 Hz, 9.0 Hz, 1H), 7.38 (s, 1H), 7.46 (d, J = 2.9 Hz, 1H), 7.54 (s, 1H), 8.04 (s, 1H), 8.20 (d, J = 9.3 Hz, 1H), 8.55 (s, 1H). Mass spectral data: m/z 417 (M++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].

target

VEGFR3

IC 50

VEGFR1: 170 nM (IC₅₀); VEGFR2: 160 nM (IC₅₀); VEGFR3: 125 nM (IC₅₀)

References

[1]. nakamura, k., et al., krn633: a selective inhibitor of vascular endothelial growth factor receptor-2 tyrosine kinase that suppresses tumor angiogenesis and growth. mol cancer ther, 2004. 3(12): p. 1639-49.
[2]. morita, a., et al., treatment of mid-pregnant mice with krn633, an inhibitor of vascular endothelial growth factor receptor tyrosine kinase, induces abnormal retinal vascular patterning in their newborn pups. birth defects res b dev reprod toxicol, 2014. 101(4): p. 293-9.

KRN 633 Preparation Products And Raw materials

Raw materials

Preparation Products

Less

KRN 633 Suppliers

China 118 Europe 1 India 3 Japan 1 United States 19 Global 142

Shanghai Boyle Chemical Co., Ltd.

Tel
Fax: 86-21-57758967
Email: sales@boylechem.com
Country: China
ProdList: 2922
Advantage: 55

WUHAN SUN-SHINE BIO-TECHNOLOGY Co., Ltd.

Tel: 17702719238 18971495150;
Email: sales@sun-shinechem.com
Country: China
ProdList: 1077
Advantage: 64

Jinan Trio PharmaTech Co., Ltd.

Tel: 0531-88811783
Fax: +86 (531) 55696010 QQ 1762738062
Email: sales@trio-pharmatech.com
Country: China
ProdList: 1856
Advantage: 62

Dalian Meilun Biotech Co., Ltd.

Tel: 0411-62910999 13889544652
Email: sales@meilune.com
Country: China
ProdList: 4747
Advantage: 58

Haoyuan Chemexpress Co., Ltd.

Tel: 021-58950125
Fax: (86) 21-58955996
Email: info@chemexpress.com
Country: China
ProdList: 7552
Advantage: 61

Shanghai Aladdin Bio-Chem Technology Co.,LTD

Tel: 400-6206333 13167063860
Fax: 021-50323701
Email: anhua.mao@aladdin-e.com
Country: China
ProdList: 25003
Advantage: 65

The future of Shanghai Industrial Co., Ltd.

Tel: 021-61552785
Fax: 021-55660885
Email: sales@shshiji.com
Country: China
ProdList: 9546
Advantage: 55

CEG Chemical Science&Technology Co., Ltd.

Tel: Mobile:13665161512
Fax: +86-510-68873513
Country: China
ProdList: 1785
Advantage: 58

ShangHai Caerulum Pharma Discovery Co., Ltd.

Tel: 18149758185
Email: sales-cpd@caerulumpharma.com
Country: China
ProdList: 3506
Advantage: 58

Suzhou yacoo science co.,Ltd

Tel: 0512-87182056 18013166090
Fax: 0512-87182056
Email: lingling.qi@yacoo.com.cn
Country: China
ProdList: 6295
Advantage: 60

ShangHai KenEn Chemical Technology Co., Ltd.

Tel: 13120367189
Fax: 021-50315529
Email: mychess007@163.com
Country: China
ProdList: 1994
Advantage: 55

Nanjing Chalf-Pharm Technology Co., Ltd.

Tel: 025-57018978 18251899859
Fax: 025-57018008
Email: sales@chalf-pharm.com
Country: China
ProdList: 5674
Advantage: 50

AdooQ Bioscience CHINA

Tel: 025-58849295 18951903616;
Fax: 025-68650336
Email: info@adooq.cn
Country: China
ProdList: 2990
Advantage: 60

Hotechem Shanghai Co., Ltd.,

Tel: 021-34621078 13120882795
Fax: 021-34622517
Email: 465106944@qq.com
Country: China
ProdList: 857
Advantage: 56

Hubei Jusheng Technology Co.,Ltd

Tel: 027-59599241 18871490274
Fax: 027-59599241
Email: 1400878000@qq.com
Country: China
ProdList: 9858
Advantage: 58

LETOPHARM LIMITED

Tel: +86-21-5821 5861
Fax: +86-21-5106 2861
Email: sales@letopharm.com
Country: China
ProdList: 2384
Advantage: 58

Sigma-Aldrich

Tel: 021-61415566 800-8193336
Email: orderCN@merckgroup.com
Country: China
ProdList: 51395
Advantage: 80

Shanghai Lollane Biological Technology Co.,Ltd.

Tel: 021-52996696，15000506266 15000506266
Fax: +86-21-52996696
Country: China
ProdList: 4769
Advantage: 55

Shanghaizehan biopharma technology co., Ltd.

Tel: 021-61350663 13052117465
Fax: 021-61350662
Email: sales@zehanbiopharma.com
Country: China
ProdList: 984
Advantage: 55

Shanghai Synchem Pharma Co., ltd

Tel: 21-619849051-1 18521059765
Email: synchempharma@aliyun.com
Country: China
ProdList: 6468
Advantage: 55

SPIRO PHARMA

Tel
Fax: -
Email: eric_feng1954@126.com
Country: China
ProdList: 9248
Advantage: 55

Codow Chemical Co.,Ltd.

Tel: 18620099427
Fax: +86-20-62619665
Email: amy@howeipharm.com
Country: China
ProdList: 6687
Advantage: 55

Guangzhou QiYun Biotechnology Co., Ltd.

Tel: 020-61288194 61288195
Fax: 020-61288700
Email: 505721671@qq.com
Country: China
ProdList: 3866
Advantage: 58

Shanghai YuanYe Biotechnology Co., Ltd.

Tel: 021-61312847; 18021002903
Fax: QQ:3008007432
Email: 3008007409@qq.com
Country: China
ProdList: 71826
Advantage: 60

Raw material medicin reagent co.,Ltd

Tel
Email: sales@njromanme.com
Country: China
ProdList: 4529
Advantage: 58

Chengdu Huachun Technology Co., Ltd

Tel: 400-1166-196 15982826727
Fax: QQ：800101999
Email: cdhxsj@163.com
Country: China
ProdList: 14603
Advantage: 60

Shanghai Rechem science Co., Ltd.

Tel: 021-31433387 15618786686
Fax: QQ:1369748377
Email: sales@rechemscience.com
Country: China
ProdList: 2991
Advantage: 58

Beijing Solarbio Science & Tecnology Co., Ltd.

Tel: 010-50973130 18101056239
Email: 3193328036@qq.com
Country: China
ProdList: 29760
Advantage: 68

Amadis Chemical Company Limited

Tel: 571-89925085
Fax: 0086-571-89925065
Email: sales@amadischem.com
Country: China
ProdList: 131957
Advantage: 58

Beijing Jin Ming Biotechnology Co., Ltd.

Tel: 010-60605840 18892239720
Fax: 010-60605840
Email: psaitong@jm-bio.com
Country: China
ProdList: 12306
Advantage: 58

Medi-tech Bioscientific Co., Ltd.

Tel: 0519-83246372 13585352506
Fax: 0519-83246372
Country: China
ProdList: 1844
Advantage: 58

Heze Development Zone chuangli Chemical Co., Ltd.

Tel: 0530-+86-530-529 6766，+86-15666160102 15666160102
Fax: 0530-529 6766
Email: info@chuangli-chem.com
Country: China
ProdList: 836
Advantage: 55

Shanghai Biopharmaleader Co., Ltd.

Tel: +86 18721201413
Fax: +86 (21) 5775-8967
Email: sales@biopharmaleader.com
Country: China
ProdList: 1720
Advantage: 58

Amatek Scientific Co. Ltd.

Tel: 0512-56316828
Fax: 0512-56316826
Email: info@amateksci.com
Country: China
ProdList: 28785
Advantage: 58

Shanghai Zhen Li Biological Technology Co., Ltd

Tel: 021-16621358918; 18516310516
Fax: 13045646768
Email: zhenlipharma888@163.com
Country: China
ProdList: 19035
Advantage: 58

Wuhan Sun-shine Bio-technology Corporation Limited

Tel: +86-027-6552-2453
Email: sales@sun-shinechem.com
Country: China
ProdList: 727
Advantage: 58

Aikon International Limited

Tel: 025-58859352 18068836627
Fax: 02557626880
Email: sales01@aikonchem.com
Country: China
ProdList: 16027
Advantage: 58

Wuhan FengyaoTonghui Chemical Products Co., Ltd.

Tel: 027-87466105 15377573527
Email: 2678564200@qq.com
Country: China
ProdList: 17987
Advantage: 58

Zhengzhou Ruke Biological Co., Ltd.

Tel: 15981811963
Fax: QQ：1410472904
Email: 1410472904@qq.com
Country: China
ProdList: 5825
Advantage: 58

Henan Alfachem Co.,Ltd.

Tel: 0371-55051623 18137891487
Fax: QQ：2853979817
Email: 2853979817@qq.com
Country: China
ProdList: 9988
Advantage: 58

Angel Pharmatech, Ltd.

Tel: 17317130613
Fax: QQ3358272972
Email: 3358272972@qq.com
Country: China
ProdList: 3277
Advantage: 58

Shanghai Jizhi Biochemical Technology Co. Ltd.

Tel: 4009004166/18616739031 18616739031
Email: 3007523370@qq.com
Country: China
ProdList: 52687
Advantage: 58

Shanghai Medicil Biomedical Co., Ltd.

Tel: 021-50822001
Email: marketing@medicilon.com.cn
Country: China
ProdList: 1152
Advantage: 58

Guangzhou Tomums Life Science Co., Ltd.

Tel: 020-31155029 18902330969
Fax: 020-31155029
Email: sales@tomums.cn
Country: China
ProdList: 4696
Advantage: 58

Nanjing Meihao Pharmaceutical Technology Co., Ltd.

Tel: meitaochem@126.com
Email: meitaochem@126.com
Country: China
ProdList: 19103
Advantage: 58

Henan Alfa Chemical Co., Ltd

Tel: +8615838112936
Email: alfa10@alfachem.cn
Country: China
ProdList: 12921
Advantage: 58

Zhejiang J&C Biological Technology Co.,Limited

Tel: +1-2135480471
Email: sales@sarms4muscle.com
Country: China
ProdList: 10473
Advantage: 58

Dayang Chem (Hangzhou) Co.,Ltd.

Tel: +86-0571-88938639 +8617705817739
Fax: +86-571-88938652，+86-571- 88492614
Email: info@dycnchem.com
Country: China
ProdList: 52846
Advantage: 58

Dideu Industries Group Limited

Tel: +86-29-89586680 +86-15129568250
Email: 1026@dideu.com
Country: China
ProdList: 20284
Advantage: 58

Chemwill Asia Co.,Ltd.

Tel: 86-21-51086038
Fax: 86-21-51861608
Email: chemwill_asia@126.com
Country: CHINA
ProdList: 23912
Advantage: 58

Less

View Lastest Price from KRN 633 manufacturers

Career Henan Chemical Co

Product: KRN 633 286370-15-8
Price: US $1000.00-950.00/KG
Min. Order: 1G
Purity: 98%
Supply Ability: 100kg
Release date: 2018-08-04

286370-15-8, KRN 633Related Search:

2-Cyclopropyl-4-(4-fluorophenyl)-quinolyl-3-methanol N-ACETYLLACTOSAMINE Deionized water Sulfanilamide Dapagliflozin MK-2206 2HCl Ki8751 SU 11274 Lenvatinib Olaparib

KRN 633

N-[2-Chloro-4-[(6,7-dimethoxy-4-quinazolinyl)oxy]phenyl]-N'-propylurea

1-(2-chloro-4-(6,7-diMethoxyquinazolin-4-yloxy)phenyl)-3-propylurea

N-[2-Chloro-4-[(6,7-dimethoxy-4-quinazolinyl)oxy]phenyl]-N'-propylurea KRN633

VEGFR Tyrosine Kinase Inhibitor III, KRN633

KRN 633;KRN-633

CS-463

KRN633; KRN-633; KRN 633

Urea, N-[2-chloro-4-[(6,7-dimethoxy-4-quinazolinyl)oxy]phenyl]-N'-propyl-

KRN 633 (This product is unavailable in the U.S.)

KRN 633 USP/EP/BP

N-[2-Chloro-4-(6,7-dimethoxyquinazolin-4-yloxy)phenyl]-N'-propylurea

KRN-633, 10 mM in DMSO

286370-15-8

Inhibitors