Cat. No.: HY-165280

BGC638

BGC638 is a thymidylate synthase inhibitor with a K_i value of 0.24 nM. BGC638 binds to α-FR with high affinity and enters cells via receptor-mediated endocytosis, thereby potently inhibiting thymidylate synthase to block DNA synthesis and ultimately induce apoptosis. BGC638 is applicable to studies related to α-FR-overexpressing tumors and epithelial carcinomas (ovarian cancer and endometrial cancer).

For research use only. We do not sell to patients.

CAS No.: 416852-27-2
Formula: C₃₂H₃₃N₅O₉
Molecular Weight:631.64

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Please store the product under the recommended conditions in the Certificate of Analysis.

BGC638 Chemical Structure

CAS No.: 416852-27-2

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
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Classifications
Bioz

Biological Activity

Description

All DNA/RNA Synthesis Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
L1210	IC₅₀	260 nM	Cell growth inhibition against mouse L1210 (RFC+/α-FR-) cells assessed via cell counting with continuous exposure until growth endpoint corresponding to ~4 population doublings. Cell growth inhibition against mouse L1210 (RFC+/α-FR-) cells assessed via cell counting with continuous exposure until growth endpoint corresponding to ~4 population doublings.	16357184
L1210 (1565)	IC₅₀	2100 nM	Cell growth inhibition against mouse L1210-1565 (RFC-/α-FR-) cells assessed via cell counting with continuous exposure until growth endpoint corresponding to ~4 population doublings. Cell growth inhibition against mouse L1210-1565 (RFC-/α-FR-) cells assessed via cell counting with continuous exposure until growth endpoint corresponding to ~4 population doublings.	16357184
L1210	IC₅₀	0.40 nM	Cell growth inhibition against mouse L1210-FBP (RFC-/α-FR+) cells assessed via cell counting with continuous exposure until growth endpoint corresponding to ~4 population doublings. Cell growth inhibition against mouse L1210-FBP (RFC-/α-FR+) cells assessed via cell counting with continuous exposure until growth endpoint corresponding to ~4 population doublings.	16357184
L1210	IC₅₀	300 nM	Cell growth inhibition against mouse L1210-FBP (RFC-/α-FR+) cells with co-addition of 1 μM folic acid, assessed via cell counting with continuous exposure until growth endpoint corresponding to ~4 population doublings. Cell growth inhibition against mouse L1210-FBP (RFC-/α-FR+) cells with co-addition of 1 μM folic acid, assessed via cell counting with continuous exposure until growth endpoint corresponding to ~4 population doublings.	16357184
A-431	IC₅₀	0.81 μM	Cell growth inhibition against human A431 (α-FR-negative) cells assessed via MTT assay with continuous 72-hour exposure in folate-free media supplemented with 20 nM leucovorin. Cell growth inhibition against human A431 (α-FR-negative) cells assessed via MTT assay with continuous 72-hour exposure in folate-free media supplemented with 20 nM leucovorin.	16357184
A-431	IC₅₀	0.97 μM	Cell growth inhibition against human A431 (α-FR-negative) cells with co-addition of 1 μM folic acid, assessed via MTT assay with continuous 72-hour exposure in folate-free media supplemented with 20 nM leucovorin. Cell growth inhibition against human A431 (α-FR-negative) cells with co-addition of 1 μM folic acid, assessed via MTT assay with continuous 72-hour exposure in folate-free media supplemented with 20 nM leucovorin.	16357184
A-431	IC₅₀	0.0028 μM	Cell growth inhibition against human A431-FBP (α-FR-overexpressing) cells assessed via MTT assay with continuous 96-hour exposure in folate-free media supplemented with 20 nM leucovorin. Cell growth inhibition against human A431-FBP (α-FR-overexpressing) cells assessed via MTT assay with continuous 96-hour exposure in folate-free media supplemented with 20 nM leucovorin.	16357184
A-431	IC₅₀	0.49 μM	Cell growth inhibition against human A431-FBP (α-FR-overexpressing) cells with co-addition of 1 μM folic acid, assessed via MTT assay with continuous 96-hour exposure in folate-free media supplemented with 20 nM leucovorin. Cell growth inhibition against human A431-FBP (α-FR-overexpressing) cells with co-addition of 1 μM folic acid, assessed via MTT assay with continuous 96-hour exposure in folate-free media supplemented with 20 nM leucovorin.	16357184
KB	IC₅₀	0.0036 μM	Cell growth inhibition against human KB (α-FR-overexpressing) cells assessed via cell counting with continuous 72-hour exposure in folate-free media supplemented with 20 nM leucovorin. Cell growth inhibition against human KB (α-FR-overexpressing) cells assessed via cell counting with continuous 72-hour exposure in folate-free media supplemented with 20 nM leucovorin.	16357184
KB	IC₅₀	0.39 μM	Cell growth inhibition against human KB (α-FR-overexpressing) cells with co-addition of 1 μM folic acid, assessed via cell counting with continuous 72-hour exposure in folate-free media supplemented with 20 nM leucovorin. Cell growth inhibition against human KB (α-FR-overexpressing) cells with co-addition of 1 μM folic acid, assessed via cell counting with continuous 72-hour exposure in folate-free media supplemented with 20 nM leucovorin.	16357184
IGROV-1	IC₅₀	0.070 μM	Cell growth inhibition against human IGROV-1 (low α-FR-expressing) cells assessed via MTT assay with continuous 96-hour exposure in folate-free media supplemented with 20 nM leucovorin. Cell growth inhibition against human IGROV-1 (low α-FR-expressing) cells assessed via MTT assay with continuous 96-hour exposure in folate-free media supplemented with 20 nM leucovorin.	16357184
IGROV-1	IC₅₀	0.93 μM	Cell growth inhibition against human IGROV-1 (low α-FR-expressing) cells with co-addition of 1 μM folic acid, assessed via MTT assay with continuous 96-hour exposure in folate-free media supplemented with 20 nM leucovorin. Cell growth inhibition against human IGROV-1 (low α-FR-expressing) cells with co-addition of 1 μM folic acid, assessed via MTT assay with continuous 96-hour exposure in folate-free media supplemented with 20 nM leucovorin.	16357184
JEG-3	IC₅₀	0.26 μM	Cell growth inhibition against human JEG-3 (very low α-FR-expressing) cells assessed via MTT assay with continuous 72-hour exposure in folate-free media supplemented with 20 nM leucovorin. Cell growth inhibition against human JEG-3 (very low α-FR-expressing) cells assessed via MTT assay with continuous 72-hour exposure in folate-free media supplemented with 20 nM leucovorin.	16357184
JEG-3	IC₅₀	0.61 μM	Cell growth inhibition against human JEG-3 (very low α-FR-expressing) cells with co-addition of 1 μM folic acid, assessed via MTT assay with continuous 72-hour exposure in folate-free media supplemented with 20 nM leucovorin. Cell growth inhibition against human JEG-3 (very low α-FR-expressing) cells with co-addition of 1 μM folic acid, assessed via MTT assay with continuous 72-hour exposure in folate-free media supplemented with 20 nM leucovorin.	16357184

In Vitro

BGC638 potently inhibits the growth of α-FR-overexpressing tumor cell lines in vitro, with an IC₅₀ of 3 nM^[1].
BGC 638 (72-96 h) inhibits cell proliferation in A431, A431-FBP, KB, IGROV-1, JEG-3, L1210, L1210-1565, and L1210-FBP cells^[2].
BGC638 potently inhibits isolated L1210 thymidylate synthase via a mixed non-competitive mechanism, with a K_i value of 0.24 nM. It binds to α-FR on mouse L1210-FBP cells, with a relative affinity of 66% that of folic acid^[2].
BGC 638 (30 nM; 1-16 h) inhibits thymidylate synthase activity in situ in KB cells^[2].
BGC 638 (0.03-1 µM; 120 h) significantly reduces the number of adherent cells, inhibits cell growth, and induces apoptosis in JEG-3 cells^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis^[2]

Cell Line:

JEG-3 cells
Concentration:

0.03, 0.2, 1 µM
Incubation Time:

120 h
Result:

Reduced the number of attached cells by slightly more than 50% at concentrations as low as 0.03 µM, and by approximately 90% at 0.2 µM, with 50% of the total cells detaching and displaying apoptotic morphology.

Parmacokinetics

Species	Dose	Route	AUC_last	C_max	T_1/2	CL	V_ss
Mice^[1]	3 μM	i.v.	149 μM·h	256 μM	4 h	1.05 L/h/kg	1.87 L/kg

In Vivo

BGC638 (100 mg/kg; i.p.; single dose; 24 h) specifically inhibits thymidylate synthase activity in tumor tissue and increases [¹²⁵I]dUrd incorporation in tumors in a nude mouse model bearing KB tumor xenografts^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

NCR nude mice (female, 6-10 weeks of age, folate-free diet for ≥14 days, KB tumor xenograft transplanted, tumor grown to ~250 mm³)^[2]
Dosage:

100 mg/kg
Administration:

i.p.; single dose; 24 h
Result:

Specifically and significantly increased the uptake of the marker [¹²⁵I]dUrd in KB tumor tissue (representing inhibition of thymidylate synthase).
Showed no significant increase in the uptake of [¹²⁵I]dUrd in normal tissues such as blood, liver, spleen, kidney, stomach, small bowel, and large bowel, demonstrating extremely high tumor selectivity.

Chemical Information

CAS No. 416852-27-2
Molecular Weight 631.64
Formula C₃₂H₃₃N₅O₉
SMILES

N(CC#C)([C@@H]1C=2C(=CC3=C(C2)C(=O)N=C(C)N3)CC1)C4=CC=C(C(N[C@@H](CCC(N[C@H](CCC(O)=O)C(O)=O)=O)C(O)=O)=O)C=C4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Wood N, et al. A liquid chromatographic-tandem mass spectrometric method for the determination of two selective thymidylate synthase inhibitors, BGC945 and BGC638, in mouse plasma. Journal of chromatography. B, Analytical technologies in the biomedical and life sciences. 2005 Sep 25;824(1-2):181-8.

[2]. Gibbs DD, et al. BGC 945, a novel tumor-selective thymidylate synthase inhibitor targeted to alpha-folate receptor-overexpressing tumors. Cancer research. 2005 Dec 15;65(24):11721-8. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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BGC638

All DNA/RNA Synthesis Isoforms