ChemicalBook >> CAS DataBase List >>2-ButynaMide, N-[4-[(3-broMophenyl)aMino]-6-quinazolinyl]-

2-ButynaMide, N-[4-[(3-broMophenyl)aMino]-6-quinazolinyl]-

CAS No.
194423-06-8
Chemical Name:
2-ButynaMide, N-[4-[(3-broMophenyl)aMino]-6-quinazolinyl]-
Synonyms
785;CL-387;EKB 785;CS-1630;-387785;CL-38875;WAY-EKI 785;CL-387785, >=98%;EKI-785 CL-38875;CL-387785 (EKI-785)
CBNumber:
CB92626313
Molecular Formula:
C18H13BrN4O
Molecular Weight:
381.23
MDL Number:
MFCD02179194
MOL File:
194423-06-8.mol
Last updated:2023-06-08 17:06:36

2-ButynaMide, N-[4-[(3-broMophenyl)aMino]-6-quinazolinyl]- Properties

Melting point 276 °C
Density 1.577±0.06 g/cm3(Predicted)
storage temp. Sealed in dry,Store in freezer, under -20°C
solubility insoluble in EtOH; insoluble in H2O; ≥16.85 mg/mL in DMSO
pka 9.84±0.43(Predicted)
form Off-white to yellow solid.
color White to Orange to Green
FDA UNII B4W27J1Z8B

SAFETY

Risk and Safety Statements

HS Code  2933.59.5300

2-ButynaMide, N-[4-[(3-broMophenyl)aMino]-6-quinazolinyl]- price More Price(37)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich 233100 CL-387,785 - CAS 194423-06-8 - Calbiochem 194423-06-8 1MG $172 2024-03-01 Buy
TCI Chemical C3575 CL-387785 194423-06-8 25MG $166 2024-03-01 Buy
TCI Chemical C3575 CL-387785 194423-06-8 100MG $455 2024-03-01 Buy
Cayman Chemical 19081 CL-387785 ≥95% 194423-06-8 1mg $37 2024-03-01 Buy
Cayman Chemical 19081 CL-387785 ≥95% 194423-06-8 5mg $116 2024-03-01 Buy
Product number Packaging Price Buy
233100 1MG $172 Buy
C3575 25MG $166 Buy
C3575 100MG $455 Buy
19081 1mg $37 Buy
19081 5mg $116 Buy

2-ButynaMide, N-[4-[(3-broMophenyl)aMino]-6-quinazolinyl]- Chemical Properties,Uses,Production

Pharmacological activity

Overactivity of epidermal growth factor receptor (EGFR) tyrosine kinase activity has been associated with a number of cancers.CL 387,785 profoundly blocks the growth of EGFR-overexpressing tumors in nude mice when given orally at 80 mg/kg/day for 10 days.

Description

Overactivity of epidermal growth factor receptor (EGFR) tyrosine kinase activity has been associated with a number of cancers. CL 387,785 is a potent, irreversible inhibitor of EGFR kinase activity (IC50 = 370 pM). It blocks EGF-stimulated autophosphorylation of receptors in cells (IC50 = 5 nM) and halts cell cycling in cells that overexpress EGFR or c-ErbB2 (IC50s = 31-125 nM). CL 387,785 profoundly blocks the growth of EGFR-overexpressing tumors in nude mice when given orally at 80 mg/kg/day for 10 days.

Uses

CL-387785 (EKI-785) is an irreversible and selective EGFR inhibitor showing activity against mutations of the receptor. Potential therapeutic against various type of cancer, including lung cancer.

Definition

ChEBI: A member of the class of quinazolines that is 4,6-diaminoquinazoine in which the one of the hydrogens attached to the amino group at position 4 has been replaced by a m-bromophenyl group while one of the hydrogens attached to the amino group a position 6 has been replaced by a but-2-ynoyl group.

in vitro

cl-387785 covalently bound to egfr. it also specifically inhibited kinase activity of the protein, blocked egf-stimulated autophosphorylation of the receptor in cells, inhibited cell proliferation primarily in a cytostatic manner in cell lines that overexpress egf-r or c-erbb-2 [1].

in vivo

the effects of cl-387785 on tumor growth were assessed in human tumor xenografts implanted s.c. in the flanks of nude mice. cl-387785 inhibited the growth of tumors derived from a431 cells when the drug was administered i.p. or p.o.. inhibitory effects were observed within 7 days after the onset of therapy. no efficacy was observed with cl-387785 in tumors derived from cell lines that did not overexpress egf-r, including the human breast carcinoma mda-mb-435 [1].

IC 50

370 pm

References

[1] discafani cm, carroll ml, floyd mb jr, hollander ij, husain z, johnson bd, kitchen d, may mk, malo ms, minnick aa jr, nilakantan r, shen r, wang yf, wissner a, greenberger lm. irreversible inhibition of epidermal growth factor receptor tyrosine kinase with in vivo activity by n-[4-[(3-bromophenyl)amino]-6-quinazolinyl]-2-butynamide (cl-387,785). biochem pharmacol. 1999 apr 15;57(8):917-25.

2-ButynaMide, N-[4-[(3-broMophenyl)aMino]-6-quinazolinyl]- Preparation Products And Raw materials

Raw materials

Preparation Products

Global( 85)Suppliers
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ATK CHEMICAL COMPANY LIMITED
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View Lastest Price from 2-ButynaMide, N-[4-[(3-broMophenyl)aMino]-6-quinazolinyl]- manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
N-[4-(3-bromoanilino)quinazolin-6-yl]but-2-ynamide pictures 2019-12-24 N-[4-(3-bromoanilino)quinazolin-6-yl]but-2-ynamide
194423-06-8
US $1.00 / KG 1KG Min98% HPLC g/kg/ton Career Henan Chemical Co

2-ButynaMide, N-[4-[(3-broMophenyl)aMino]-6-quinazolinyl]- Spectrum

CL-387785 (EKI-785) N-(4-(3-bromophenylamino)quinazolin-6-yl)but-2-ynamide N-[4-[(3-broMophenyl)aMino]-6-quinazolinyl]-2-ButynaMide CL-387785 2-ButynaMide, N-[4-[(3-broMophenyl)aMino]-6-quinazolinyl]- CL-387785, >=98% CL-38875 EKB 785 WAY-EKI 785 EKI-785 CL-38875 CL-387 785 EKI-785; WAY-EKI 785; CL387785; CL 387785; EKI785; WAY-EKI785; EKI 785;CL-387;785 CS-1630 N-[4-(3-bromoanilino)quinazolin-6-yl]but-2-ynamide -387785 2-ButynaMide, N-[4-[(3-broMophenyl)aMino]-6-quinazolinyl]- USP/EP/BP CL-387785,ErbB-1,HER1,CL387785,EGFR,EKI785,inhibit,Inhibitor,CL 387785,EKI 785,Epidermal growth factor receptor 194423-06-8 Inhibitors