BMS-754807

Product Name: BMS-754807
CAS No.: 1001350-96-4
Chemical Name: BMS-754807
Synonyms: CS-466;BMS-754807;BMS-754807, >=98%;MS-754807 USP/EP/BP;BMS-754807;BMS 754807;(2S)-1-[4-[(5-Cyclopropyl;(S)-1-(4-((5-Cyclopropyl-1H-pyrazol-3-yl)amino)pyrrolo[2,1-f][1,2,4]triazin-2-yl)-N-(6-fluorop;(S)-1-(4-(5-cyclopropyl-1H-pyrazol-3-ylamino)pyrrolo[1,2-f][1,2,4]triazin-2-yl)-N-(6-fluoropyridin-3-yl)-2-methylpyrrolidine-2-carboxamide;(S)-1-(4-((5-cyclopropyl-1H-pyrazol-3-yl)aMino)pyrrolo[2,1-f][1,2,4]triazin-2-yl)-N-(6-fluoropyridin-3-yl)-2-Methylpyrrolidine-2-carboxaMide;(2S)-1-[4-[(5-Cyclopropyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]-N-(6-fluoro-3-pyridinyl)-2-methyl-2-pyrrolidinecarboxamide
CBNumber: CB02500939
Molecular Formula: C23H24FN9O
Formula Weight: 461.49
MOL File: 1001350-96-4.mol

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BMS-754807 Property

Density: 1.58
storage temp.: room temp
solubility: ≥23.05 mg/mL in DMSO; insoluble in H2O; ≥27.75 mg/mL in EtOH
form: powder
color: white to beige
optical activity: [α]/D -86 to -96°, c = 1 in methanol

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 17505
Product name: BMS 754807
Purity: ≥98%
Packaging: 1mg
Price: $44
Updated: 2024/03/01

Cayman Chemical

Product number: 17505
Product name: BMS 754807
Purity: ≥98%
Packaging: 5mg
Price: $202
Updated: 2024/03/01

Cayman Chemical

Product number: 17505
Product name: BMS 754807
Purity: ≥98%
Packaging: 10mg
Price: $321
Updated: 2024/03/01

TRC

Product number: B596315
Product name: BMS754807
Packaging: 1mg
Price: $55
Updated: 2021/12/16

ApexBio Technology

Product number: A1185
Product name: BMS-754807
Packaging: 5mg
Price: $65
Updated: 2021/12/16

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BMS-754807 Chemical Properties,Usage,Production

Description

BMS 754807 is a reversible, orally bioavailable dual inhibitor of insulin-like growth factor 1 receptor (IGF-1R) and insulin receptor (InsR) tyrosine kinases (IC₅₀s = 1.8 and 1.7 nM, respectively). It has minimal effect against an array of other tyrosine and serine/threonine kinases. BMS 754807 inhibits cell proliferation or induces apoptosis in a variety of cancer cells in vitro. It inhibits the growth of tumor xenografts in mice and this effect is often enhanced by combination therapy with other chemotherapeutics. Predictive biomarkers, including elevated IGF-1R expression, for effectiveness of BMS 754807 have been delineated.

Uses

BMS-754807 has been used in the embryo drug treatment.

Uses

An IGF-1R inhibitor with an IC50 of 13 nM.

Uses

BMS 754807 is a reversible, orally bioavailable dual inhibitor of insulin-like growth factor 1 receptor (IGF-1R) and insulin receptor (InsR) tyrosine kinases (IC50s = 1.8 and 1.7 nM, respectively). It has minimal effect against an array of other tyrosine and serine/threonine kinases. BMS 754807 inhibits cell proliferation or induces apoptosis in a variety of cancer cells in vitro. It inhibits the growth of tumor xenografts in mice and this effect is often enhanced by combination therapy with other chemotherapeutics. Predictive biomarkers, including elevated IGF-1R expression, for effectiveness of BMS 754807 have been delineated.[Cayman Chemical]

Definition

ChEBI: BMS-754807 is a pyrrolotriazine that is pyrrolo[2,1-f][1,2,4]triazine which is substituted at position 2 by the pyrrolidine nitrogen of (2S)-N-(6-fluoropyridin-3-yl)-2-methylprolinamide, and at position 4 by a (5-cyclopropyl-1H-pyrazol-3-yl)amino group. It is a potent, reversible inhibitor of the insulin-like growth factor 1 receptor/insulin receptor family kinases. It has a role as an EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor and an antineoplastic agent. It is a pyrrolotriazine, a member of pyrazoles, a member of pyridines and a member of pyrrolidines.

General Description

BMS-754807 is a pyrrolotriazine, which is a potent dual inhibitor of insulin-like growth factor-1 receptor (IGF-1R) and insulin receptor (InsR) tyrosine kinase. It has been reported that BMS-754807 also acts as a reversible ATP-competitive antagonist of IGF-1R by restricting the catalytic domain of the IGF-1R.

Biochem/physiol Actions

BMS-754807 is an orally available and potent dual insulin-like growth factor factor-1 receptor (IGF-1R)/ insulin receptor (InsR) tyrosine kinase inhibitor that synergistically enhances antiproliferative effects of 4-hydroxytamoxifen, letrozole, and fulvestrant in MCF-7/AC-1 cells.

References

[1] q.s. chu，s.w. kim，p.m. ellis，l. mileshkin，r.h. de boer，j.s. park，t. pellas，f. huang，f. graf finckenstein，a. dhar. bms-754807, an oral dual igf-1r/insulin receptor (ir) inhibitor: initial results from a phase 1 dose- and schedule-ﬁnding study in combination with carboplatin/paclitaxel in subjects with solid tumors. european journal of cancer supplements. november 2010, 8(7): 131.
[2] vattoly j. majo, victoria arango, norman r. simpson, jaya prabhakaran, suham a. kassir, mark d. underwood, mihran bakalian, peter canoll, j. john mann, j.s. dileep kumar. synthesis and in vitro evaluation of [18f]bms-754807: a potential pet ligand for igf-1r. bioorganic & medicinal chemistry letters. july 2013, 23(14): 4191-4194.
[3] joan m. carboni, mark wittman, zheng yang, et al.. bms-754807, a small molecule inhibitor of insulin-like growth factor-1r/ir. mol cancer ther. 2009;8:3341-3349.

BMS-754807 Preparation Products And Raw materials

Raw materials

Preparation Products

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BMS-754807 Suppliers

China 116 India 2 United States 17 Global 135

AdooQ BioScience, LLC

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Target molecule Corp.

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Musechem

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TargetMol Chemicals Inc.

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InvivoChem

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Cckinase, Inc.

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Aladdin Scientific

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Aceschem Inc.

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Cayman Chemical Company

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View Lastest Price from BMS-754807 manufacturers

Career Henan Chemical Co

Product: BMS-754807 1001350-96-4
Price: US $2.00/kg
Min. Order: 1kg
Purity: 99%
Supply Ability: 100kg
Release date: 2018-12-24

1001350-96-4, BMS-754807Related Search:

ABT-199 Linsitinib Saracatinib AVP-AEW541 BI 2536 Olaparib

(2S)-1-[4-[(5-Cyclopropyl-1H-pyrazol-3-yl)aMino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]-N-(6-fluoropyridin-3-yl)-2-Methylpyrrolidine-2-carboxaMide

(S)-1-(4-((5-cyclopropyl-1H-pyrazol-3-yl)aMino)pyrrolo[2,1-f][1,2,4]triazin-2-yl)-N-(6-fluoropyridin-3-yl)-2-Methylpyrrolidine-2-carboxaMide

BMS-754807

(2S)-1-[4-[(5-Cyclopropyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]-N-(6-fluoro-3-pyridinyl)-2-methyl-2-pyrrolidinecarboxamide

(S)-1-(4-(5-cyclopropyl-1H-pyrazol-3-ylamino)pyrrolo[1,2-f][1,2,4]triazin-2-yl)-N-(6-fluoropyridin-3-yl)-2-methylpyrrolidine-2-carboxamide

(2S)-1-[4-[(5-Cyclopropyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]-N-(6-fluoro-3-pyridinyl)-2-methyl-2-pyrrolidinecarboxamide BMS 754807

BMS 754807 (2S)-1-[4-[(5-Cyclopropyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]-N-(6-fluoro-3-pyridinyl)-2-methyl-2-pyrrolidinecarboxamide

(S)-1-(1-(4-((5-cyclopropyl-1H-pyrazol-3-yl)amino)pyrrolo[2,1-f][1,2,4]triazin-2-yl)-2-methylpyrrolidin-2-yl)-2-((6-fluoropyridin-3-yl)amino)ethanone

(2S)-1-[4-[(5-Cyclopropyl

(S)-1-(4-((5-Cyclopropyl-1H-pyrazol-3-yl)amino)pyrrolo[2,1-f][1,2,4]triazin-2-yl)-N-(6-fluorop

BMS-754807, >=98%

BMS-754807;BMS 754807

CS-466

2-Pyrrolidinecarboxamide, 1-[4-[(5-cyclopropyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]-N-(6-fluoro-3-pyridinyl)-2-methyl-, (2S)-

MS-754807 USP/EP/BP

1001350-96-4

C23H24FN9O

Inhibitors