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453562-69-1 (Motesanib)

1

Identification

Motesanib Motesanib
Name Motesanib
Formula C22H23N5O
MW 373.45
CAS No. 453562-69-1
EINECS
Smiles O=C(C1=CC=CN=C1NCC2=CC=NC=C2)NC3=CC(NCC4(C)C)=C4C=C3
Synonyms AMG 706; AMG-706; N-(3,3-dimethylindolin-6-yl)-2-((pyridin-4-ylmethyl)amino)nicotinamide
InChI InChI=1S/C22H23N5O/c1-22(2)14-26-19-12-16(5-6-18(19)22)27-21(28)17-4-3-9-24-20(17)25-13-15-7-10-23-11-8-15/h3-12,26H,13-14H2,1-2H3,(H,24,25)(H,27,28)
2

Introduction

Motesanib (AMG-706) is a potent ATP-competitive inhibitor of VEGFR1/2/3 with IC50 of 2 nM/3 nM/6 nM, respectively; similar activity against Kit, ~10-fold more selective for VEGFR than PDGFR and Ret. IC50 value: 2 nM/3 nM/6 nM/8 nM(VEGFR1/2/3/c-Kit) [1] Target: pan-VEGFR; Kit in vitro: Motesanib Diphosphate has broad activity against the human VEGFR family, and displays >1000 selectivity against EGFR, Src, and p38 kinase.

Background Information

An orally bioavailable inhibitor of a multiple-receptor tyrosine kinase inhibitor with potential antineoplastic activity ......by AOBIOUS INC
Motesanib (AMG706) is a multikinase inhibitor that selectively targets VEGF receptors, platelet-derived growth factor receptors (PDGFRs), and Kit receptors with IC?? values of 2 nM (VEGFR1), 3 nM (VEGFR2), 6 nM (VEGFR3), 84 nM (PDGFR), and 8 nM (Kit). ......by AdooQ BioScience, LLC
Description ......by Apexbio Technology LLC
Motesanib is a multikinase inhibitor that selectively targets VEGF receptors, platelet-derived growth factor receptors (PDGFRs), and Kit receptors. It also potently inhibits angiogenesis and induces regression in tumor xenografts. ......by BOC Sciences
Cell-permeable. Motesanib, also known as AMG-706, is a multikinase inhibitor that selectively targets VEGF receptors, platelet-derived growth factor receptors (PDGFRs), and Kit receptors with IC₅₀ values of 2 nM (VEGFR1), 3 nM (VEGFR2), 6 nM (VEGFR3), 84 nM (PDGFR), and 8 nM (Kit). It also potently inhibits angiogenesis and induces regression in tumor xenografts. ......by BioVision, Inc.,
Motesanib is a potent ATP-competitive inhibitor of VEGFR1/2/3 with IC50s of 2 nM/3 nM/6 nM, respectively, and has similar activity against Kit, and is appr 10-fold more selective for VEGFR than PDGFR and Ret.  ......by MedChemexpress Co., Ltd.
Motesanib, also known as AMG-706, is the orally bioavailable multiple-receptor tyrosine kinase inhibitor with potential antineoplastic activity. Motesanib selectively targets and inhibits vascular endothelial growth factor (VEGFR), platelet-derived growth factor (PDGFR), kit, and Ret receptors, thereby inhibiting angiogenesis and cellular proliferation. ......by MedKoo Biosciences, Inc.
A potent, orally bioavailable, multikinase inhibitor inhibitor of VEGFR1/2/3, PDGFR and c-Kit with IC50 of 2-6 nM, 84 nM and 8 nM, respectively; also displays activity against Ret (IC50=59 nM), no activities against EGFR, Src, and p38; inhibits human endothelial cell proliferation induced by VEGF, but not by bFGF in vitro; potently inhibits VEGF-induced angiogenesis in the rat models.Lung CancerPhase 3 Discontinued ......by ProbeChem
Motesanib is an orally bioavailable receptor tyrosine kinase inhibitor with potential antineoplastic activity. AMG 706 selectively targets and inhibits vascular endothelial growth factor (VEGFR), platelet-derived growth factor (PDGFR), Kit, and Ret receptors, thereby inhibiting angiogenesis and cellular proliferation. ......by Target Molecule Corp.
3

Protocol(Only for Reference)

Cell Experiment

Animal Experiment

4

Physical and Chemical Properties

Appearance:White to off-white solid EBNumber:EB000029137

Storage condition

Store at or below -20 oC. by LC Laboratoies

Solubility

Soluble in DMSO at 200 mg/mL; soluble in ethanol at 40 mg/mL; very poorly soluble in water; maximum solubility in plain water is estimated to be about 50-100 μM; buffers, serum, or other additives may increase or decrease the aqueous solubility. by LC Laboratoies
DMSO by MedChemexpress Co., Ltd.
5

Mechanism and Indication

6

Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
Motesanib Amgen Inc Metastatic non small cell lung cancer 2007/7/31 2013/2/28 Phase 3 Clinical
Motesanib Amgen Inc Non-small-cell lung cancer 2007/7/31 2011/8/31 Phase 2 Clinical
Motesanib Amgen Inc Solid tumor 2005/12/31 2012/7/31 Phase 2 Clinical
Motesanib Amgen Inc Fallopian tube cancer 2007/7/31 2013/12/31 Phase 2 Clinical
Motesanib Amgen Inc Peritoneal tumor 2007/7/31 2013/12/31 Phase 2 Clinical
Motesanib Amgen Inc Metastatic ovary cancer 2007/7/31 2013/12/31 Phase 2 Clinical
Motesanib - Phase 3
7

Safety Data of Motesanib

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Spectral Information

9

Suppliers List

Company Price and Availability Country/Region
AOBIOUS INC 1mg/USD11() USA
Adipogen Corporation USA
AdooQ BioScience, LLC USA
Apexbio Technology LLC USA
Ark Pharm, Inc. USA
BOC Sciences
BioVision, Inc., USA
Biochem Tek(Shanghai) Co., ltd. China
Biochempartner Co., Ltd China
CHEMSCENE, LLC 10mg/USD60();50mg/USD192() USA
LC Laboratoies 10mg/USD36(In stock);25mg/USD75(In stock);50mg/USD112(In stock);100mg/USD198(In stock);200mg/USD367(In stock);500mg/USD860(In stock);1g/USD1590(In stock) USA
MedChemexpress Co., Ltd. 10mg/USD60();50mg/USD192() USA
MedKoo Biosciences, Inc. USA
ProbeChem
Shanghai Haoyuan Chemexpress Co., Ltd. 10mg/USD60();50mg/USD192() China
Target Molecule Corp. 1mg/USD56();5mg/USD168();10mg/USD299();25mg/USD538();50mg/USD968() USA
10

Related Products

Other Forms of 453562-69-1

Name CAS No Formula MW
Motesanib (Diphosphate) 857876-30-3 C22H29N5O9P2 569.44

Recommended Compounds in VEGFR c-Kit

Name CAS No Formula MW
BIBF 1202 894783-71-2 C30H31N5O4 525.6
SKLB1002 1225451-84-2 C13H12N4O2S2 320.39
Vandetanib (hydrochloride) 524722-52-9 C22H25BrClFN4O2 511.81
Vandetanib (trifluoroacetate) 338992-53-3 C24H25BrF4N4O4 589.38
WHI-P154 211555-04-3 C16H14BrN3O3 376.2
ZM323881 (hydrochloride) 193000-39-4 C22H19ClFN3O2 411.86
ZM 306416 690206-97-4 C16H13ClFN3O2 333.74
Tanshinone IIA 568-72-9 C19H18O3 294.34
R1530 882531-87-5 C18H14ClFN4O 356.78
Oglufanide 38101-59-6 C16H19N3O5 333.34
SKLB610 1125780-41-7 C21H16F3N3O3 415.37
AZD2932 883986-34-3 C24H25N5O4 447.4864
Toceranib (phosphate) 874819-74-6 C22H28FN4O6P 494.45
Sunitinib 557795-19-4 C22H27FN4O2 398.47
Regorafenib (monohydrate) 1019206-88-2 C21H17ClF4N4O4 500.83
Tyrphostin A9 10537-47-0 C18H22N2O 282.38
TAK-593 1005780-62-0 C23H23N7O3 445.47
ZM323881 193001-14-8 C22H18FN3O2 375.4
SAR131675 1433953-83-3 C18H22N4O4 358.39
JI-101 900573-88-8 C22H20BrN5O2 466.33

Recommended Compounds in Same Indication

Name CAS No Formula MW
LDK378 1032900-25-6 C28H36ClN5O3S 558.14
Pemetrexed (disodium) 150399-23-8 C20H19N5Na2O6 471.37
AZD1152 722543-31-9 C26H31FN7O6P 587.54
Volasertib 755038-65-4 C34H50N8O3 618.81
ALK inhibitor 1 761436-81-1 C23H28BrN7O3S 562.48
Olaparib 763113-22-0 C24H23FN4O3 434.46
Afatinib (dimaleate) 850140-73-7 C32H33ClFN5O11 718.08
PU-H71 873436-91-0 C18H21IN6O2S 512.37
BMS-599626 (Hydrochloride) 873837-23-1 C27H28ClFN8O3 567.01
MGCD-265 analog 875337-44-3 C26H20FN5O2S2 517.5977
Crizotinib 877399-52-5 C21H22Cl2FN5O 450.34
AT9283 896466-04-9 C19H23N7O2 381.43
KX2-391 897016-82-9 C26H29N3O3 431.53
AT-101 90141-22-3 C30H30O8 518.55
Tivantinib 905854-02-6 C23H19N3O2 369.42
SNX-2112 908112-43-6 C23H27F3N4O3 464.48
IDO5L 914471-09-3 C9H7ClFN5O2 271.6356
Dovitinib 405169-16-6 C21H21FN6O 392.43
Tivozanib 475108-18-0 C22H19ClN4O5 454.86
Nordihydroguaiaretic acid 500-38-9 C18H22O4 302.36
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Route of Synthesis

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References

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More Information

Motesanib

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