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Afatinib (dimaleate)

(CAS: 850140-73-7)

Suppliers of Afatinib (dimaleate)

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AbMole BioScience [email protected] 1-800-660-8580 USA

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Active Biochem [email protected]; [email protected] 1-800-857-0985 (USA Toll Free#) USA

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AdooQ BioScience, LLC [email protected] 855-GO-ADOOQ (855-462-3667) (US & Canada Toll Free) 866-930-6790 (US & Canada Toll Free) +1-323-389-9269 (Outside of US & Canada) USA

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Apexbio Technology LLC [email protected] +1-832-696-8203 USA

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Price and Availability: USD39/10mg ()

Ark Pharm, Inc. [email protected] +1 (847) 367-3680 USA

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BOC Sciences [email protected] 1-631-504-6093

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Biochempartner Co., Ltd [email protected] 0086-13720134139; 0086-15971444841 China

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CHEMSCENE, LLC [email protected] 732-484-9848 USA

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Price and Availability: USD60/10mg () USD132/50mg ()

Cayman Chemical Company [email protected] Toll Free (USA and Canada Only): (800) 364-9897; Direct: (734) 971-3335;Technical Support Toll Free (USA and Canada Only): (888) 526-5351;Technical Support Direct: (734) 975-3888 USA

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Jinan Chuancheng Pharmaceutical Co., Ltd. [email protected] +86 (531) 8890-2485 China

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MedChemexpress Co., Ltd. [email protected] 609-228-6898 USA

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Price and Availability: USD60/10mg () USD132/50mg ()
Quality Control & MSDS Files: HNMR LCMS HNMR HNMR LCMS LCMS MSDS

MedKoo Biosciences, Inc. [email protected] 919-279-0682 USA

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ProbeChem [email protected] 86-21-80183644

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Selleck Chemicals LLC [email protected] +1-832-582-8158 USA

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Shanghai Haoyuan Chemexpress Co., Ltd. [email protected] +86 (21) 5187-0955 / +86 (21) 5895-5995 China

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Price and Availability: USD60/10mg () USD132/50mg ()

Target Molecule Corp. [email protected] (857) 239-0968 USA

Fax: 857-239-8801Purity: .98 Brand: TargetMol

Price and Availability: USD98/20mg () USD168/50mg () USD318/100mg ()

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Background Information of Afatinib (dimaleate)

Afatinib (BIBW2992) irreversibly inhibits EGFR/HER2 including EGFR(wt), EGFR(L858R), EGFR(L858R/T790M) and HER2 with IC50 of 0.5 nM, 0.4 nM, 10 nM and 14 nM, respectively; 100-fold more active against Gefitinib-resistant L858R-T790M EGFR mutant. IC50 value: 0.5 nM/0.4 nM/10 nM/14 nM (EGFR(wt)/EGFR(L858R)/EGFR(L858R/T790M) /HER2) [1] Target: EGFR;EGFR mutant forms; HER2 in vitro: BIBW2992 shows potent activity against both wild-type and mutant forms of EGFR and HER2.

Solubility of Afatinib (dimaleate)

Solubility Sources
DMSO MedChemexpress Co., Ltd.

Storage Condition of Afatinib (dimaleate)

Storage Condition Sources

MSDS Information

MSDS Sources
MedChemexpress Co., Ltd.

Quality Control and Spectral Data

QC Reports Sources
[HNMR] [LCMS] MedChemexpress Co., Ltd.

Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
Afatinib (dimaleate) Boehringer Ingelheim Corp; ICON Clinical Research Metastatic non small cell lung cancer 2012/3/31 2015/1/31 Phase 3 Clinical
Afatinib (dimaleate) Boehringer Ingelheim Corp Metastatic non small cell lung cancer 2013/9/30 2015/12/31 Phase 3 Clinical
Afatinib (dimaleate) Boehringer Ingelheim Corp Metastatic head and neck cancer 2013/5/31 2016/4/30 Phase 3 Clinical
Afatinib (dimaleate) Boehringer Ingelheim Pharmaceuticals Inc Metastatic non small cell lung cancer 2013/7/31 2015/7/31 Phase 3 Clinical
Afatinib (dimaleate) Boehringer Ingelheim Pharmaceuticals Inc Diarrhea 2013/4/30 2015/2/28 Phase 3 Clinical
Afatinib (dimaleate) - Launched

Chemical Information

M.Wt Formula CAS No. Synonyms
718.08 C32H33ClFN5O11 850140-73-7 BIBW 2992MA2;BIBW-2992;BIBW2992;BIBW 2992;Afatinib; (S,E)-N-(4-((3-chloro-4-fluorophenyl)amino)-7-((tetrahydrofuran-3-yl)oxy)quinazolin-6-yl)-4-(dimethylamino)but-2-enamide dimaleate

Structure Information of Afatinib (dimaleate)

Smiles O=C(NC1=C(C=C2C(C(NC3=CC(Cl)=C(C=C3)F)=NC=N2)=C1)O[[email protected]]4CCOC4)/C=C/CN(C)C.O=C(O)/C=CC(O)=O.O=C(O)/C=CC(O)=O
InChI InChI=1S/C24H25ClFN5O3.2C4H4O4/c1-31(2)8-3-4-23(32)30-21-11-17-20(12-22(21)34-16-7-9-33-13-16)27-14-28-24(17)29-15-5-6-19(26)18(25)10-15;2*5-3(6)1-2-4(7)8/h3-6,10-12,14,16H,7-9,13H2,1-2H3,(H,30,32)(H,27,28,29);2*1-2H,(H,5,6)(H,7,8)/b4-3+;2*2-1-/t16-;;/m0../s1

Related Products

Other Form Products of Afatinib (dimaleate)

Name CAS Formula Suppliers
Afatinib (BIBW 2992) 439081-18-2 C24H25ClFN5O3 20
2-Butenamide, N-[4-[(3-chloro-4-fluorophenyl)amino]-7-[[(3S)-tetrahydro-3-furanyl]oxy]-6-quinazolinyl]-4-(dimethylamino)- 439081-18-2 C24H25ClFN5O3 15
Afatinib (D6) 1313874-96-2 C24H19D6ClFN5O3 3

Recommended Products in Same Target

Name CAS Formula Suppliers
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Mutated EGFR-IN-1 1421372-66-8 C25H31N7O 10
AZD-9291 (mesylate) 1421373-66-1 C29H37N7O5S 11
Mutant EGFR inhibitor 1421373-62-7 C27H30ClN7O2 10
AZD-9291 1421373-65-0 C28H33N7O2 21
WHI-P180 (hydrochloride) 153437-55-9 C16H16ClN3O3 6
WHI-P180 211555-08-7 C16H15N3O3 13
Gefitinib (hydrochloride) 184475-55-6 C22H25Cl2FN4O3 13
Erlotinib (mesylate) 248594-19-6 C23H27N3O7S 9
BGB-102 807640-87-5 C22H25BrN4O2 6
Poziotinib 1092364-38-9 C23H21Cl2FN4O3 17
CO-1686 (hydrobromide) 1446700-26-0 C27H29BrF3N7O3 14
CO-1686 1374640-70-6 C27H28F3N7O3 19
CNX-2006 1375465-09-0 C26H27F4N7O2 13
PD168393 194423-15-9 C17H13BrN4O 17
AG 18 118409-57-7 C10H6N2O2 21
Chrysophanol 481-74-3 C15H10O4 28
AG-1478 153436-53-4 C16H14ClN3O2 15
Mubritinib 366017-09-6 C25H23F3N4O2 26
AST-1306 (TsOH) 1050500-29-2 C31H26ClFN4O5S 15

Recommended Products in the Same Indication

Name CAS Formula Suppliers
LDK378 1032900-25-6 C28H36ClN5O3S 19
Pemetrexed (disodium) 150399-23-8 C20H19N5Na2O6 22
Volasertib 755038-65-4 C34H50N8O3 17
ALK inhibitor 1 761436-81-1 C23H28BrN7O3S 8
Olaparib 763113-22-0 C24H23FN4O3 20
MGCD-265 analog 875337-44-3 C26H20FN5O2S2 14
AT-101 90141-22-3 C30H30O8 16
Tivantinib 905854-02-6 C23H19N3O2 10
Sunitinib 557795-19-4 C22H27FN4O2 19
Motesanib (Diphosphate) 857876-30-3 C22H29N5O9P2 20
Racecadotril 81110-73-8 C21H23NO4S 26
LY2603618 911222-45-2 C18H22BrN5O3 15
Crizotinib 877399-52-5 C21H22Cl2FN5O 25
Ganetespib 888216-25-9 C20H20N4O3 17
Axitinib 319460-85-0 C22H18N4OS 27
Carboplatin 41575-94-4 C6H12N2O4Pt 29
Lenvatinib 417716-92-8 C21H19ClN4O4 19
AXL1717 477-47-4 C22H22O8 20
Afatinib (BIBW 2992) 439081-18-2 C24H25ClFN5O3 20
Vandetanib (hydrochloride) 524722-52-9 C22H25BrClFN4O2 8

Chemical and Physical Properties

Appearance:White to off-white solid Melting point:
Boiling point: Flash Point:
Water Solubility: Solubility:In vitro:DMSO,100 mg/mL(139.43 mM);In vitro:Water,Insoluble;In vitro:Ethanol,Insoluble;In vivo:Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):5% DMSO+30% PEG 300+ddH2OFor best results, use promptly a
Density: Merck:
BRN: Refractive Index:
Vapour: EINECS:
Optical Rotation: alpha:

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